| 产品标题 |
产品货号 |
产品规格 |
厂家 |
| Difluprednate - DFBA | Durezol | Axon 1428
CAS [23674-86-4]
MF C27H34F2O7MW 508.55
Purity:
99%
Soluble in DMSO
Description
A corticosteroid used for the treatment of post-operative ocular inflammation and pain
References
Certificates
Categories
Extra info
Certificate of Analysis
Material Safety Data Sheet
Miscellaneous
Pain & Inflammation
NR3C
Glucocorticoid (GR)
Corticosteroid
Chemical name
Butyric acid (6S,9R,10S,11S,13S,14S,17R)-17-(2-acetoxy-acetyl)-6,9-difluoro-11-hydroxy-10,13-dimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-17-yl ester
Parent CAS No.
[23674-86-4]
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Size
Unit Price
Stock
10 mg
€75.00
In Stock | | axonmedchem |
| Diflorasone Diacetate | Axon 1427
CAS [33564-31-7]
MF C26H32F2O7MW 494.52
Purity:
99%
Soluble in DMSO
Description
A corticosteroid used as anti-inflammatory and anti-itching agent
References
Certificates
Categories
Extra info
Certificate of Analysis
Material Safety Data Sheet
Miscellaneous
Pain & Inflammation
Endocrinology
NR3C
Glucocorticoid (GR)
Corticosteroid
Chemical name
Acetic acid (6S,9R,10S,11S,13S,16S,17R)-17-(2-acetoxy-acetyl)-6,9-difluoro-11-hydroxy-10,13,16-trimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-17-yl ester
Parent CAS No.
[33564-31-7]
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Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| Fluticasone furoate - GW 685698X | Axon 1172
CAS [397864-44-7]
MF C27H29F3O6SMW 538.58
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO and Ethanol
Description
Selective high affinity glucocorticoid agonist, MRP4 inhibitor; a Fluticasone derivative as corticosteroid with potent anti-inflammatory activity
References
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Extra info
M. Salter et al. Pharmacological properties of the enhanced-affinity glucocorticoid fluticasone furoate in vitro and in an in vivo model of respiratory inflammatory disease. Am. J. Physiol. - Lung Physiol. 2007, 293(3), L660-L667.
Certificate of Analysis
Material Safety Data Sheet
Immunology
Miscellaneous
Pain & Inflammation
Endocrinology
NR3C
Glucocorticoid (GR)
Glucocorticoid agonist; MRP4 inhibitor
Chemical name
Furan-2-carboxylic acid (6S,9R,10S,11S,13S,16R,17R)-6,9-difluoro-17-fluoromethylsulfanylcarbonyl-11-hydroxy-10,13,16-trimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-17-yl ester
Parent CAS No.
[397864-44-7]
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Size
Unit Price
Stock
10 mg
€115.00
In Stock | | axonmedchem |
| SKL 2001 | Axon 2084
CAS [909089-13-0]
MF C14H14N4O3MW 286.29
Purity:
99%
Soluble in DMSO
Description
Wnt/β-catenin signaling pathway agonist or activator, having effects of regulating the differentiation of mesenchumal stem cells
References
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Extra info
J Gwak et al. Small molecule-based disruption of the Axin/β-catenin protein complex regulates mesenchymal stem cell differentiation. Cell Res. 2012, 22(1), 237-247.
EM Felipe De Sousa & JP Medema. Axing Wnt signals. Cell Res. 2012, 22(1), 9-11.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Stem Cell
β-Catenin
Wnt-β-Catenin
Cell-Cell Adhesion Protein
Stem Cell Differentiator
Wnt
Wnt/β-catenin signaling pathway agonist or activator
Chemical name
N-(3-(1H-imidazol-1-yl)propyl)-5-(furan-2-yl)isoxazole-3-carboxamide
Parent CAS No.
[909089-13-0]
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Size
Unit Price
Stock
10 mg
€90.00
In Stock | | axonmedchem |
| OG-L002 hydrochloride | Axon 2077
CAS [1357298-75-9]
MF C15H15NO.HClMW 261.75
Purity:
100%
Soluble in water and DMSO
Description
Highly specific inhibitor of lysine specific demethylase 1 (LSD1, also known as KDM1A, or H3K9 demethylase) (IC50, ~0.02 µM).
OG-L002 potently repressed herpes simplex virus (HSV) IE gene expression, genome replication, and reactivation from latency. It suppressed primary lytic infection of HSV in vivo in a mouse model. This highlights the potential for drugs that inhibit a virus’ ability to modify chromatin for treating or even preventing viral diseases like herpes, chicken pox, and shingles.
References
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Extra info
Y Liang et al. A Novel Selective LSD1/KDM1A Inhibitor Epigenetically Blocks Herpes Simplex Virus Lytic Replication and Reactivation from Latency. MBio. 2013, 4, e00558-12.
Inhibiting key protein halts herpes lytic cycle. mBioSphere on Feb 6, 2013.
Z Watson et al. Role of Polycomb Proteins in Regulating HSV-1 Latency. Viruses 2013, 5, 1740-1757.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Epigenetics
Immunology
EC 1.14.11
Histone demethylase
Inhibitor of lysine specific demethylase 1 (LSD1 aka KDM1A)
Chemical name
4'-((trans)-2-aminocyclopropyl)biphenyl-3-ol hydrochloride
Parent CAS No.
[1357300-15-2]
Order
Size
Unit Price
Stock
5 mg
€125.00
In Stock | | axonmedchem |
| Axon 1170 - Androsta-1,4-diene-17-carboxylic acid, 6,9-difluoro-11,17-dihydroxy-16-methyl-3-oxo-, (6a,11b,16a,17a)- | Axon 1170
CAS [28416-82-2]
MF C21H26F2O5MW 396.42
Purity:
98%
No solubility data
Description
Steroid derivative; precursor for e.g. fluticasone
References
Certificates
Categories
Extra info
Liao, Y. et al. Synthesis and pharmacological evaluation of triflate-substituted analogues of Clozapine: Identification of a novel atypical neuroleptic. J. Med. Chem. 1997, 40, 4146-4153.
Y. Liao et al. New sulfonyloxy piperazinyldibenzazapines as potential atypical antipsychotics: chemistry and pharmacological evaluation. J. Med. Chem. 1999,42, 2235-2244.
Jackson, D; Wikström, H; Liao, Y. Is clozapine an (partial) agonist at both dopamine D1 and D2 receptors? Psychopharm. 1998, 138, 213-214.
Certificate of Analysis
Material Safety Data Sheet
Endocrinology
Non Selective
Building Block; unknown pharmacology
Chemical name
(6S,9R,10S,11S,13S,16R,17R)-6,9-Difluoro-11,17-dihydroxy-10,13,16-trimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthrene-17-carboxylic acid
Parent CAS No.
[28416-82-2]
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Size
Unit Price
Stock
500 mg
€330.00
In Stock | | axonmedchem |
| KY 02111 | Axon 2036
CAS [1118807-13-8]
MF C18H17ClN2O3SMW 376.86
Purity:
98%
Soluble in DMSO
Description
A canonical Wnt signaling pathway inhibitor that promotes differentiation of human pluripotent stem cells (hPSCs), including ESCs and iPSCs, to cardiomyocytes. KY02111 acts downstream of APC and GSK-3β to inhibit Wnt signaling; KY02111 and Wnt inhibitors, such as XAV 939 (Axon 1527), cooperatively enhance hPSC cardiomyogenesis; KY 02111 and WNT modulators, CHIR 99021 (Axon 1386) and/or BIO (Axon 1693) permit cytokine and xeno-free hPSC cardiomyogenesis
References
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Extra info
I Minami et al. A Small Molecule that Promotes Cardiac Differentiation of Human Pluripotent Stem Cells under Defined, Cytokine- and Xeno-free Conditions. Cell Reports 2012, 2(5), 1448–1460.
W Li et al. Chemical approaches to studying stem cell biology. (review article). Cell Res. 2013, 23, 81–91.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Stem Cell
Wnt-β-Catenin
Wnt
Canonical Wnt signaling pathway inhibitor
Chemical name
N-(6-chlorobenzo[d]thiazol-2-yl)-3-(3,4-dimethoxyphenyl)propanamide
Parent CAS No.
[1118807-13-8]
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Size
Unit Price
Stock
10 mg
€80.00
In Stock | | axonmedchem |
| CGI 1746 | Axon 2018
CAS [910232-84-7]
MF C34H37N5O4MW 579.69
Purity:
99%
Soluble in DMSO
Description
Potent and highly selective inhibitor of Bruton's tyrosine kinase (Btk) (IC50: 1.9 nM); CGI1746 inhibits B cell signaling and functional effects
References
Certificates
Categories
Extra info
JA Di Paolo et al. Specific Btk inhibition suppresses B cell- and myeloid cell-mediated arthritis. Nat. Chem. Biol. 2011, 7(1), 41-50.
Y Lou et al. Bruton's tyrosine kinase inhibitors: approaches to potent and selective inhibition, preclinical and clinical evaluation for inflammatory diseases and B cell malignancies. J. Med. Chem. 2012, 55(10), 4539-4350.
SL Tamn et al. Targeting the SYK–BTK axis for the treatment of immunological and hematological disorders: Recent progress and therapeutic perspectives. Pharmacol. & Ther. 2013, 138(2), 294-309.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
BTK
EC 2.7.10.2
Inhibitor of Bruton's tyrosine kinase (BTK)
Chemical name
4-tert-butyl-N-(2-methyl-3-(4-methyl-6-(4-(morpholine-4-carbonyl)phenylamino)-5-oxo-4,5-dihydropyrazin-2-yl)phenyl)benzamide
Parent CAS No.
[910232-84-7]
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Size
Unit Price
Stock
2 mg
€85.00
In Stock | | axonmedchem |
| AZD 8330 | Axon 1999
CAS [869357-68-6]
MF C16H17FIN3O4MW 461.23
Purity:
98%
Soluble in DMSO
Description
Potent, highly specific non-ATP-competitive MEK inhibitor; AZD8330 specifically inhibits mitogen-activated protein kinase kinase 1 (MEK or MAP/ERK kinase1), resulting in inhibition of growth factor-mediated cell signaling and tumor cell proliferation
References
Certificates
Categories
Extra info
JI Trujillo. MEK inhibitors: a patent review 2008-2010. Exp. Opin. Ther. Patents. 2011, 21(7), 1045-1069.
MS Chapman & JN Miner. Novel mitogen-activated protein kinase kinase inhibitors. Exp. Opin. Invest. Drugs. 2011, 20(2), 209-220.
C Frémin and S Meloche. From basic research to clinical development of MEK1/2 inhibitors for cancer therapy. J. Hematol. Oncol. 2010, 3, 8.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
MAPK
EC 2.7.12.2
MEK
MEK 1 inhibitor
Chemical name
2-(2-fluoro-4-iodophenylamino)-N-(2-hydroxyethoxy)-1,5-dimethyl-6-oxo-1,6-dihydropyridine-3-carboxamide
Parent CAS No.
[869357-68-6]
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Size
Unit Price
Stock
5 mg
€105.00
In Stock | | axonmedchem |
| CH 5424802 - Alectinib | Axon 1884
CAS [1256580-46-7]
MF C30H34N4O2MW 482.62
Purity:
99%
Moderately soluble in DMSO
Description
Potent, orally available and selective anaplastic lymphoma kinase (ALK) inhibitor capable of blocking the resistant gatekeeper mutant
References
Certificates
Categories
Extra info
H Sakamoto et al. CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant. Cancer Cell. 2011, 19(5), 679-90.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
ALK
TGF-β
RTK class XIX; 2.7.10.1
Orally available and selective ALK inhibitor
Chemical name
9-ethyl-6,6-dimethyl-8-(4-morpholinopiperidin-1-yl)-11-oxo-6,11-dihydro-5H-benzo[b]carbazole-3-carbonitrile
Parent CAS No.
[1256580-46-7]
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Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| LY 2228820 | Axon 1895
CAS [862505-00-8]
MF C24H29FN6MW 420.53
Purity:
99%
Soluble in DMSO
Description
Potent p38 MAPK inhibitor (IC50: 7 and 3 nM for p38α and p38β MAPKs respectively); antitumor agent for the treatment of multiple myeloma (MM) patients by reducing skeletal events and enhancing cytotoxicity of bortezomib (Axon 1810)
References
Certificates
Categories
Extra info
K Ishitsuka et al. p38 mitogen-activated protein kinase inhibitor LY2228820 enhances bortezomib-induced cytotoxicity and inhibits osteoclastogenesis in multiple myeloma; therapeutic implications. Br. J. Haematol. 2008, 141(5), 598-606.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
MAPK (p38)
MAPK
EC 2.7.11.24
Inhibitor of p38 MAPK
Chemical name
5-(2-tert-butyl-4-(4-fluorophenyl)-1H-imidazol-5-yl)-3-neopentyl-3H-imidazo[4,5-b]pyridin-2-amine
Parent CAS No.
[862505-00-8]
Order
Size
Unit Price
Stock
5 mg
€105.00
In Stock | | axonmedchem |
| PCI 32765 - Ibrutinib | Axon 1858
CAS [936563-96-1]
MF C25H24N6O2MW 440.50
Purity:
99%
Soluble in DMSO
Description
Orally bioavailable and highly selective inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity; inhibiting BTK activity, B-cell-mediated signaling and the growth of malignant B cells that overexpress BTK; an experimental drug candidate for chronic lymphocytic leukemia (CLL), mantle cell lymphoma, diffuse large B-cell lymphoma, and multiple myeloma etcBTK, a member of the BTK/Tec family of non-recetor cytoplasmic tyrosine kinases, is required for B cell receptor (BCR) signaling, plays a key role in B-cell maturation, and is overexpressed in a number of B-cell malignancies
References
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Extra info
Z Pan et al. Discovery of selective irreversible inhibitors for Bruton's tyrosine kinase. ChemMedChem 2007, 2(1), 58–61.
LA Honigberg et al. The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy. Proc. Nat. Acad. Sci. USA 2010, 107(29), 13075–80.
ES Winer et al. PCI-32765: a novel Bruton's tyrosine kinase inhibitor for the treatment of lymphoid malignancies. Expert Opin. Investig. Drugs. 2012, 21(3), 355-61.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Immunology
BTK
EC 2.7.10.2
Inhibitor of Bruton's tyrosine kinase (BTK)
Chemical name
(R)-1-(3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one
Parent CAS No.
[936563-96-1]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| PF 06463922 - Lorlatinib | Axon 2600
CAS [1454846-35-5]
MF C21H19FN6O2MW 406.41
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Potent, orally available and brain-penetrant ALK/ROS1 selective inhibitor (mean Ki value of <0.07 nM for inhibition of recombinant human wild-type ALK) displaying superior potency against all known clinically acquired ALK mutations (all displaying sub-nanomolar Ki values), including the highly resistant G1202R mutant. PF 06463922 (Lorlatinib) is capable of blocking Crizotinib-resistant ROS1 mutations and treatment with PF 06463922 led to superior regression of EML4-ALK-driven brain metastases compared with other clinically available ALK inhibitors.
KEYWORDS: PF 06463922 | supplier | ALK/ROS1 inhibitor | Lorlatinib | PF06463922 | CAS [1454846-35-5] | ALK | ROS | Inhibitor | RTK | receptor tyrosine kinase | c-ROS | G1202R | mutant | Crizotinib | EML4-ALK | oncogene | fusion protein | Anaplastic Lymphoma Kinase | insulin receptor | | axonmedchem |
| NT 157 | Axon 2238
CAS [1384426-12-3]
MF C16H14BrNO5SMW 412.26
Purity:
99%
Soluble in DMSO
Description
Unique allosteric inhibitor of IGF1R. NT 157 promotes ERK-MAPK dependent inhibitory Ser-phosphorylation and degradation of insulin receptor substrate 1 and 2 (IRS1/2) by shifting IGF1R complexation from IRS1/2 to Shc, which results in long-term inhibition of IGF1R signaling and powerful inhibition of tumor cell growth.
References
Certificates
Categories
Extra info
H. Reuveni et al. Therapeutic Destruction of Insulin Receptor Substrates for Cancer Treatment. Cancer Res. 2013, 73, 4383-4394.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
IGF1R
Endocrinology
MAPK
PI3K-Akt-mTOR
RTK class II; EC 2.7.10.1
Unique allosteric inhibitor of IGF1R signaling
Chemical name
(E)-3-(3-bromo-4,5-dihydroxyphenyl)-N-(3,4,5-trihydroxybenzyl)prop-2-enethioamide
Parent CAS No.
[1384426-12-3]
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Size
Unit Price
Stock
2 mg
€95.00
In Stock | | axonmedchem |
| KRCA 0008 | Axon 2294
CAS [1472795-20-2]
MF C30H37ClN8O4MW 609.12
Purity:
100%
Soluble in DMSO
Description
Potent and selective dual ALK (anaplastic lymphoma kinase ) and ACK1 inhibitor (IC50 values 12 nM and 4 nM for ALK and Ack1, respectively) with good drug-like properties: good water-solubility with moderate plasma protein binding and low brain exposure. It has good liver microsomal stability and little to no CYP inhibition. KRCA0008 also shows promising pharmacokinetic parameters in both mice and rat (oral bioavailability = 66-94.5%) and a modest tumor growth inhibition in vivo activity in H3122 human lung cancer bearing mice model comparable to Crizotinib (Axon 1660) without significant body weight change.
References
Certificates
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Extra info
C.H. Park et al. Novel bis-ortho-alkoxy-para-piperazinesubstituted-2,4-dianilinopyrimidines (KRCA-0008) as potent and selective ALK inhibitors for anticancer treatment. Bioorg Med Chem Lett. 2013 Nov 15;23(22):6192-6.
H.J. Lee et al. ALK inhibitors of bis-ortho-alkoxy-para-piperazinesubstituted-pyrimidines and -triazines for cancer treatment. Arch Pharm Res. 2014 Sep;37(9):1130-8.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Endocrinology
ACK1
TGF-β
EC 2.7.10.1
ALK
ALK
Potent and selective dual ALK/ACK1 inhibitor with good drug-like properties
Chemical name
1,1'-(4,4'-(4,4'-(5-chloropyrimidine-2,4-diyl)bis(azanediyl)bis(3-methoxy-4,1-phenylene))bis(piperazine-4,1-diyl))diethanone
Parent CAS No.
[1472795-20-2]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| GSK 1838705A - GSK 1838705 | Axon 2267
CAS [1116235-97-2]
MF C27H29FN8O3MW 532.57
Purity:
99%
Soluble in DMSO
Description
Potent and selective insulin-like growth factor-1 receptor (IGF-IR) and insulin receptor (IR) kinase inhibitor with additional affinity for anaplastic lymphoma kinase (ALK) with IC50 values of 2.0 nM, 1.6 nM, and 0.6 nM, for IGF1R, IR, and ALK respectively, and >800-fold selectivity over related kinases, including RSK1, JNK3, and B-Raf V600EGSK 1838705A inhibits the proliferation of cancer cell lines, comprises the growth of human tumor xenografts in vivo, and causes complete regression of ALK-dependent tumors in vivo at well-tolerated doses.
References
Certificates
Categories
Extra info
S.D. Chamberlain et al. Optimization of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine IGF-1R tyrosine kinase inhibitors towards JNK selectivity. Bioorg. Med. Chem. Lett. 2009, 19, 360-364.
P. Sabbatini et al. GSK1838705A inhibits the insulin-like growth factor-1 receptor and anaplastic lymphoma kinase and shows antitumor activity in experimental models of human cancers. Mol. Cancer Ther. 2009, 8, 2811-20.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
ALK
IGF1R
Endocrinology
RTK class II; EC 2.7.10.1
IR
Potent IGF-IR and insulin receptor (IR) kinase inhibitor with additional affinity for ALK
Chemical name
2-(2-(1-(2-(dimethylamino)acetyl)-5-methoxyindolin-6-ylamino)-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-6-fluoro-N-methylbenzamide
Parent CAS No.
[1116235-97-2]
Order
Size
Unit Price
Stock
5 mg
€110.00
In Stock | | axonmedchem |
| XMD 8-87 | Axon 2762
CAS [1234480-46-6]
MF C24H27N7O2MW 445.52
Purity:
98%
Soluble in 0.1N HCl(aq) and DMSO
Description
XMD 8-87 is a potent and selective inhibitor of Ack1 (activated CDC42-associated kinase) also known as tyrosine kinase nonreceptor 2 (TNK2). XMD8-87 has IC50 values of 38 and 113 nM for the D163E and R806Q mutations, respectively.
KEYWORDS: XMD 8-87 | supplier | Ack1 inhibitor | XMD8-87 | CAS [1234480-46-6] | Ack1-AR-ATM signaling | ACK1 | Inhibitor | Enzymes | TNK2 | | axonmedchem |
| LDK 378 - Ceritinib | Axon 2224
CAS [1032900-25-6]
MF C28H36ClN5O3SMW 558.14
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Potent, bioavailable, and selective anaplastic lymphoma kinase (ALK) inhibitor (IC50 value 0.2 nM) with >35 fold selectivity over InsR, IGF-1R. LDK 378 induced a dose-dependent tumor growth inhibition and tumor regression in multiple rat xenograft models.
References
Certificates
Categories
Extra info
J. Chen et al. LDK378: a promising anaplastic lymphoma kinase (ALK) inhibitor. J. Med. Chem. 2013, 56, 5673-5674.
T.H. Marsilje et al. Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(...). J. Med. Chem. 2013, 56, 5675-5690.
E. Ardini et al. ALK Inhibitors, a Pharmaceutical Perspective. Front Oncol. 2012, 2, 17.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
ALK
TGF-β
RTK class XIX; 2.7.10.1
Potent, bioavailable, and selective anaplastic lymphoma kinase (ALK) inhibitor
Chemical name
5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine
Parent CAS No.
[1032900-25-6]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| AIM 100 | Axon 2031
CAS [873305-35-2]
MF C23H21N3O2MW 371.43
Purity:
99%
Optical purity:
98.1% e.e.
Soluble in DMSO
Description
Specific inhibitor of Ack1 tyrosine kinase (also known as TNK2); AIM-100 inhibits Ack1 activity and also suppresses androgen receptor (AR) Tyr(267) phosphorylation and its recruitment to the ATM enhancer (Ack1/AR/ATM signaling)
References
Certificates
Categories
Extra info
K Mahajan et al. Effect of Ack1 tyrosine kinase inhibitor on ligand-independent androgen receptor activity. Prostate. 2010, 70(12), 1274-1285.
K Mahajan et al. Ack1 mediated androgen receptor phosphorylation modulates radiation resistance in castration resistant prostate cancer. J. Biol. Chem. 2012, 287(26), 22112-22122.
K Mahajan, NP Mahajan. Shepherding AKT and androgen receptor by Ack1 tyrosine kinase. J. Cell. Physiol. 2010, 224, 327–333.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Endocrinology
ACK1
EC 2.7.10.2
Specific inhibitor of Ack1 tyrosine kinase (also known as TNK2)
Chemical name
(S)-5,6-diphenyl-N-((tetrahydrofuran-2-yl)methyl)furo[2,3-d]pyrimidin-4-amine
Parent CAS No.
[873305-35-2]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| AZD 3463 | Axon 2153
CAS [1356962-20-3]
MF C24H25ClN6OMW 448.95
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Potent inhibitor of Anaplastic Lymphoma Kinase (ALK) and IGF1R; AZD3463 is potent in ALK-driven preclinical models and in a variety of crizotinib-resistant models
References
Certificates
Categories
Extra info
Discovery of AZD3463 as a Novel ALK/IGFR Dual Inhibitor and its Ability in Overcoming Acquired Resistance to Crizotinib. Presented by B Yang at 8th Protein Kinases in Drug Discovery 2013, Boston USA.
Concurrent roles for IGF1R and EGFR in driving acquired resistance to crizotinib and ability to overcome with a combination of the ALK/IGF1R inhibitor AZD3463 and Iressa. Abstr. 4465 presented by L Drew et al. AACR Annual Meeting 2013 Washington DC USA.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
ALK
Endocrinology
TGF-β
RTK class II and XIX; EC 2.7.10.1
Potent inhibitor of ALK and IGF1R
Chemical name
N-(4-(4-aminopiperidin-1-yl)-2-methoxyphenyl)-5-chloro-4-(1H-indol-3-yl)pyrimidin-2-amine
Parent CAS No.
[1356962-20-3]
Order
Size
Unit Price
Stock
5 mg
€105.00
In Stock | | axonmedchem |
| OSI 906 - Linsitinib | Axon 1702
CAS [867160-71-2]
MF C26H23N5OMW 421.49
Purity:
99%
Soluble in DMSO
Description
Highly potent, orally efficacious and highly selective, dual ATP-competitive tyrosine kinase inhibitor of insulin-like growth factor-1 receptor (IGF-1R) (IC50: 35 nM) and insulin receptor (IR) (IC50: 75 nM)
References
Certificates
Categories
Extra info
MJ Mulvihill et al. Discovery of OSI-906: a selective and orally efficacious dual inhibitor of the IGF-1 receptor and insulin receptor. Fut. Med. Chem. 2009, 1(6), 1153-1171.
CP Carden et al. Phase I study of intermittent dosing of OSI-906, a dual tyrosine kinase inhibitor of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR) in patients with advanced solid tumors. J. Clin. Oncol. 2010, 28,15s
V. M. Macaulay et al. Phase I study of OSI-906, dual tyrosine kinase inhibitor of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR) in combination with erlotinib (E) in patients with advanced (...). J. Clin. Oncol. 2010, 28,15s
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
IGF1R
Endocrinology
RTK class II; EC 2.7.10.1
IGF1R tyrosine kinase inhibitor
Chemical name
3-[8-Amino-1-(2-phenyl-quinolin-7-yl)-imidazo[1,5-a]pyrazin-3-yl]-1-methyl-cyclobutanol
Parent CAS No.
[867160-71-2]
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Size
Unit Price
Stock
2 mg
€85.00
In Stock | | axonmedchem |
| NVP-TAE684 - TAE 684 | Axon 1416
CAS [761439-42-3]
MF C30H40ClN7O3SMW 614.20
Purity:
99%
Soluble in DMSO
Description
Potent, selective and efficacious inhibitor of NPM-ALK.
KEYWORDS: NVP-TAE684 | supplier | ALK inhibitor | TAE 684 | NVPTAE684 | TAE684 | TAE-684 | CAS [761439-42-3] | NPM-ALK | fusion protein | anaplastic large-cell lymphoma | ALCL | apoptosis | cell cycle arrest | nucleophosmin | | axonmedchem |
| AVL 292 - CC 292 | Axon 2226
CAS [1202757-89-8]
MF C22H22FN5O3MW 423.44
Purity:
98%
Soluble in DMSO
Description
A potent, selective, orally bioavailable, covalent Bruton's tyrosine kinase (Btk) inhibitor with potential antineoplastic activity (IC50 value 1400 selective over a number of Src family kinases and B cell signaling components in full length recombinant Btk protein assay). More specific for BTK than PCI 32765 (Ibrutinib, Axon 1858) is, and with a shorter half-life.AVL 292 reduces migration of CLL cells towards CXCL12 and CXCL13, and reduces viability as well as markers of BCR activation, such as CCL3 and CCL4 chemokine production, in primary CLL cells cultured with Nurse-like Cells (NLC).
References
Certificates
Categories
Extra info
E.K. Evans et al. Inhibition of Btk with CC-292 provides early pharmacodynamic assessment of activity in mice and humans. J. Pharmacol. Exp. Ther. 2013, 346, 219-228.
H. Eda et al. A novel Bruton′s tyrosine kinase inhibitor CC-292 in combination with the proteasome inhibitor carfilzomib impacts multiple myeloma bone microenviroment with resultant anti-myeloma activity. Blood 2013, 122, 682.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Immunology
BTK
EC 2.7.10.2
Potent, selective, covalent BTK inhibitor
Chemical name
N-(3-(5-Fluoro-2-(4-(2-methoxyethoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide
Parent CAS No.
[1202757-89-8]
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Size
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5 mg
€120.00
In Stock | | axonmedchem |
| ASP 3026 | Axon 2005
CAS [1097917-15-1]
MF C29H40N8O3SMW 580.74
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Selective inhibitor of the oncogenic fusion kinase EML4-ALK; ASP3026 has a broad safety margin and inhibitory activity at the gatekeeper mutation; potential agent in EML4-ALK fusion positive NSCLC patients, that have relapsed to Crizotinib (Axon 1660)
References
Certificates
Categories
Extra info
S Kuromitsu et al. Abstract A227: Antitumor activities of ASP3026 against EML4-ALK-dependent tumor models. Mol. Cancer Ther. 2011, 10, 11, S1.
J de Lartigue. ALK Inhibitors: Moving Rapidly From Discovery to Clinical Approval and Beyond. Onclive 2013.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Oncogene Fusion Proteins
TGF-β
EC 2.7.10.1
ALK
ALK
Inhibitor of the oncogenic fusion kinase EML4-ALK
Chemical name
N2-(2-(isopropylsulfonyl)phenyl)-N4-(2-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)-1,3,5-triazine-2,4-diamine
Parent CAS No.
[1097917-15-1]
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Unit Price
Stock
2 mg
€80.00
In Stock | | axonmedchem |
| Stemregenin 1 - SR1 | Axon 1865
CAS [1227633-49-9]
MF C24H23N5OSMW 429.54
Purity:
99%
Soluble in DMSO
Description
Aryl hydrocarbon receptor (AHR) antagonist that promotes the self-renewal of human hematopoietic stem cells (HSC) in culture. SR1 promotes the ex vivo expansion of CD34+ cells. Culture of HSCs with SR1 led to a 50-fold increase in cells expressing CD34 and a 17-fold increase in cells that retain the ability to engraft immunodeficient mice
References
Certificates
Categories
Extra info
AE Boitano et al. Aryl hydrocarbon receptor antagonists promote the expansion of human hematopoietic stem cells. Science 2010, 329, 1345-1348.
G Sauvageau and RK Humphries. The blood stem cell Holy Grail? Science 2010, 329, 1291-1292.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Signaling & Oncology
Diabetes & Metabolism
Immunology
Stem Cell
AHR
Transcription Factors
TF class 1.2
Aryl hydrocarbon receptor (AHR) antagonist
Chemical name
4-(2-(2-(benzo[b]thiophen-3-yl)-9-isopropyl-9H-purin-6-ylamino)ethyl)phenol
Parent CAS No.
[1227633-49-9]
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Size
Unit Price
Stock
10 mg
€105.00
In Stock | | axonmedchem |
| LFM-A13 | Axon 2862
CAS [244240-24-2]
MF C11H8Br2N2O2MW 360.00
Purity:
99%
Soluble in DMSO
Description
LFM-A13 is a potent and specific inhibitor of BTK (IC50 value of 2.5 µM). LFM-A13 did not affect the enzymatic activity of other protein tyrosine kinases, including Janus kinases JAK1 and JAK2, Src family kinase HCK, and receptor family tyrosine kinases E.
KEYWORDS: LFM-A13 | suppplier | BTK inhibitor | LFM A13 | LFMA13 | CAS [244240-24-2] | B-Cell Transformation | BTK | Inhibitor | Enzymes | | axonmedchem |
| VX 745 | Axon 1811
CAS [209410-46-8]
MF C19H9Cl2F2N3OSMW 436.26
Purity:
99%
Soluble in DMSO
Description
Highly potent and selective inhibitor of p38α MAP kinase (IC50: 10 nM); being 1000 fold selective over closely related kinases
References
Certificates
Categories
Extra info
JP Duffy et al. The discovery of VX-745: a novel and selective p38α kinase inhibitor. ACS Med. Chem. Lett. 2011, 2, 758.
MC Bagley et al. Rapid synthesis of VX-745: p38 MAP kinase inhibition in Werner syndrome cells. Bioorg. Med. Chem. Lett. 2007, 17(8), 5107-5110.
JJ Haddad. VX-745. Vertex Pharmaceuticals. Curr. Opin. Investig. Drugs. 2001, 2(8), 1070-1076.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
MAPK (p38)
MAPK
EC 2.7.11.24
Inhibitor of p38α MAP kinase
Chemical name
5-(2,6-dichlorophenyl)-2-(2,4-difluorophenylthio)-6H-pyrimido[1,6-b]pyridazin-6-one
Parent CAS No.
[209410-46-8]
Order
Size
Unit Price
Stock
5 mg
€90.00
In Stock | | axonmedchem |
| PH 797804 | Axon 1837
CAS [586379-66-0]
MF C22H19BrF2N2O3MW 477.30
Purity:
99%
Soluble in DMSO and ethanol
Description
Highly potent, selective and metabolically stable inhibitor of p38 MAPK (p38α cascade IC50: 2.3 nM); an ATP-competitive, readily reversible inhibitor of the α isoform of human p38 MAP kinase, exhibiting a Ki of 5.8 nM; clinical candidate.
*PH 797804 is an (-)-atropisomer, which is 100-fold more potent than its (+)-atropisomer. Be careful that racemate of PH 797804 is wrongly provided by other supplier as drug PH 797804 itself. The less potent (+)-rotating atropisomer is also available (inquire). Be right about your drug.
The racemate, (±)-PH797804 (Axon 2786) is also available. | | axonmedchem |
| GSK 1120212 - Trametinib | JTP 74057 | Axon 1761
CAS [871700-17-3]
MF C26H23FIN5O4MW 615.39
Purity:
99%
Soluble in DMSO
Description
Highly potent and selective MEK inhibitor, with IC50 values to be 0.7 and 0.9 nM for MEK1 and MEK2 respectively and with long circulating half-life
References
Certificates
Categories
Extra info
AG Gilmartin et al. GSK1120212 (JTP-74057) is an inhibitor of MEK activity and activation with favorable pharmacokinetic properties for sustained in vivo pathway inhibition. Clin. Cancer Res. 2011, 17(5), 989-1000.
T Yamaguchi et al. Antitumor activities of JTP-74057 (GSK1120212), a novel MEK1/2 inhibitor, on colorectal cancer cell lines in vitro and in vivo. Int J Oncol. 2011, 39(1), 23-31.
H Abe et al. Discovery of a Highly Potent and Selective MEK Inhibitor: GSK1120212 (JTP-74057 DMSO Solvate). ACS Med. Chem. Lett., 2011, 2(4), 320–324.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
MAPK
EC 2.7.12.2
MEK
MEK1 and MEK2 inhibitor
Chemical name
N-(3-(3-cyclopropyl-5-(2-fluoro-4-iodophenylamino)-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydropyrido[4,3-d]pyrimidin-1(2H)-yl)phenyl)acetamide
Parent CAS No.
[871700-17-3]
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Size
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5 mg
€95.00
In Stock | | axonmedchem |
| Shz-1 | Axon 1701
CAS [326886-05-9 ]
MF C13H11BrN2O3SMW 355.21
Purity:
99%
Soluble in DMSO
Description
Stem cell differentiating agent that induce differentiation of stem cells into cells of cardiac fate; Cardiogenic small molecule that enhance myocardial repair by stem cells; Potently induces Nkx2.5 and a subset of other cardiac markers
References
Certificates
Categories
Extra info
H Sadek et al. Cardiogenic small molecules that enhance myocardial repair by stem cells. PNAS 2008, 105(16), 6063-6068.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Cycle Regulation
Cell Signaling & Oncology
Stem Cell
Nkx2.5
TF class 3.1.1
Stem cell differentiating agent; Nkx2.5 inducer
Chemical name
(E/Z)-N'-(5-bromo-2-hydroxybenzylidene)benzenesulfonohydrazide
Parent CAS No.
[326886-05-9 ]
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Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| SCIO 469 - Talmapimod | Axon 1671
CAS [309913-83-5]
MF C27H30ClFN4O3MW 513.00
Purity:
98%
Soluble in DMSO
Description
Orally available and selective inhibitor of p38 mitogen-activated protein (MAP) kinase (MAPK), with a 10-fold selectivity for p38α over p38β and 2000-fold over 20 other kinases; potential agent with immunomodulating, anti-inflammatory and antineoplastic activities
References
Certificates
Categories
Extra info
SN Nikas and AA Drosos. SCIO-469 Scios Inc. Curr Opin Investig Drugs. 2004, 5(11), 1205-1212.
SN Nikas and AA Drosos. SCIO-469 Scios Inc. Curr Opin Investig Drugs. 2004, 5(11), 1205-1212.
T Navas et al. The p38 MAPK inhibitor SCIO-469 enhances the apoptotic and anti-proliferative effects of proteasome inhibitors MG132 and PS341 (Velcade) in multiple myeloma cells. Proc. Amer. Assoc. Cancer Res, 2004, Vol. Abs. #3350.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Immunology
Pain & Inflammation
MAPK (p38)
MAPK
EC 2.7.11.24
MAPK inhibitor (p38 specific)
Chemical name
2-(6-chloro-5-((2R,5S)-4-(4-fluorobenzyl)-2,5-dimethylpiperazine-1-carbonyl)-1-methyl-1H-indol-3-yl)-N,N-dimethyl-2-oxoacetamide
Parent CAS No.
[309913-83-5]
Order
Size
Unit Price
Stock
5 mg
€105.00
In Stock | | axonmedchem |
| AC 220 dihydrochloride - Quizartinib dihydrochloride | Axon 1696
CAS [1132827-21-4]
MF C29H32N6O4S.2HClMW 633.59
Purity:
98%
Soluble in DMSO
Description
A uniquely potent, selective and efficacious inhibitor of FMS-Like Tyrosine kinase-3 (FLT3) for the treatment of AML; Second-generation FLT3 inhibitor that is highly potent with low nanomolar potency both in vitro and in cellular assays, and has a highly focused and selective interaction pattern across the human protein kinome.
References
Certificates
Categories
Extra info
PP Zarrinkar et al. AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). Blood 2009, 114 (14), 2984-2992.
PH Wiernik. FLT3 inhibitors for the treatment of acute myeloid leukemia. Clin. Adv. Hematol. Oncol. 2010, 8(6), 429-444.
Q Chao et al. Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and (...). J. Med. Chem. 2009, 52(23), 7808-7816.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
FLT3
RTK class III; EC 2.7.10.1
FLT3 inhibitor
Chemical name
1-(5-tert-Butyl-isoxazol-3-yl)-3-{4-[7-(2-morpholin-4-yl-ethoxy)-benzo[d]imidazo[2,1-b]thiazol-2-yl]-phenyl}-urea dihydrochloride
Parent CAS No.
[950769-58-1]
Order
Size
Unit Price
Stock
5 mg
€90.00
In Stock | | axonmedchem |
| Zaleplon | Axon 1646
CAS [151319-34-5]
MF C17H15N5OMW 305.33
Purity:
99%
Soluble in DMSO
Description
Zaleplon selectively binds with high efficacy to the benzodiazepine site (ω1) on the α1 containing GABAA receptors; a nonbenzodiazepine hypnotic agent used in the treatment of insomnia
References
Certificates
Categories
Extra info
D.J. Sanger et al. Comparison of the pharmacological profiles of the hypnotic drugs, zaleplon and zolpidem. Eur. J. Pharmacol. 1996, 313, 35-42.
S.M. Stahl et al. Selective actions on sleep or anxiety by exploiting GABA-A/benzodiazepine receptor subtypes. J. Clin. Psychiatry. 2002, 63, 179-180.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
GABA-A
Unclassified
GABAA-α1 agonist
Chemical name
N-(3-(3-cyanopyrazolo[1,5-a]pyrimidin-7-yl)phenyl)-N-ethylacetamide
Parent CAS No.
[151319-34-5]
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Size
Unit Price
Stock
10 mg
€65.00
In Stock | | axonmedchem |
| JQ-1, (+)- - JQ1 | Axon 1989
CAS [1268524-70-4]
MF C23H25ClN4O2SMW 456.99
Purity:
99%
Optical purity:
99% ee
Soluble in DMSO
Description
Potent and selective BET bromodomain inhibitor (IC50 values of 77 nM and 33 nM for inhibition of binding of a tetra-acetylated histone H4 peptide to BRD4 with the first and second bromodomain, respectively). (+)-JQ1 is capable of blocking the macrophage inflammatory responses via inhibition of BET proteins in mice, and activating HIV latency through antagonizing Brd4 inhibition of Tat-transactivation. Cotreatment with JQ1 and the FLT3 inhibitor AC220 (Axon 1696) synergistically induce apoptosis of cultured and primary CD34(+) human AML blast progenitor cells (BPC) expressing FLT3-ITD.
KEYWORDS: (+)-JQ-1 | BET inhibitor | JQ1 | JQ-1 | JQ1 | CAS [1268524-70-4] | Histone | BET (BRD) | Inhibitor | Proteins | Bromodomain | inflammatory | HIV latency | | axonmedchem |
| PK 11195, N-Desmethyl- | Axon 2833
CAS [124236-61-9]
MF C20H19ClN2OMW 338.83
Purity:
99%
Soluble in DMSO
Description
Precursor for [N-methyl-11C]PK 11195 for PET studies. Radioligand precursor of the peripheral benzodiazepine antagonist PK 11195 (Axon 1208).
KEYWORDS: N-Desmethyl-PK 11195 | supplier | PK 11195 radioligand precursor | N-Desmethyl-PK11195 | N-Desmethyl-PK-11195 | CAS [124236-61-9] | GABA | GABA-A | Antagonist | Ion Channels | PET | | axonmedchem |
| CD161 | Axon 2776
CAS [1627716-22-6]
MF C26H21N5O2MW 435.48
Purity:
98%
Soluble in DMSO
Description
CD161 is a potent, orally active and selective BET bromodomain inhibitor (Ki values of 8.2 nM and 1.4 nM for BRD4 BD1 and BD2, respectively). CD161 inhibits cell growth in acute leukemia cell lines and breast cancer cell lines. Moreover, CD161 has an excellent oral pharmacokinetic profile and, orally administered, effectively inhibits tumor growth in mice.
KEYWORDS: CD161 | supplier | BET inhibitor | CD-161 | CD 161 | CAS [1627716-22-6] | Histone | BET (BRD) | Inhibitor | Proteins | BRD4 | Leukemia | Breast Cancer | Bioavailable | | axonmedchem |
| PF 02341066 - Crizotinib | PF 2341066 | Axon 1660
CAS [877399-52-5]
MF C21H22Cl2FN5OMW 450.34
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Potent, selective and ATP-competitive inhibitor of c-Met/HGF receptor and the nucleophosmin-anaplastic lymphoma kinase (NPM-ALK), with IC50 values to be 4 and 25 nM for c-Met and ALK respectively. (R)-Crizotinib is superior to standard chemotherapy in patients with previously treated, advanced non-smal-cell lung cancer with ALK rearrangement. Notably, (S)-Crizotinib (Axon 2296) was recently found to potently inhibit the MTH1 phosphatase enzyme, whereas the (R) enantiomer is inactive (IC50 values of 72 nM and 1375 nM resp.).
References
Certificates
Categories
Extra info
A.T. Shaw et al. Crizotinib versus chemotherapy in advanced ALK-positive lung cancer. N. Engl. J. Med. 2013, 368, 2385-2394.
HY Zou et al. An Orally Available Small-Molecule Inhibitor of c-Met, PF-2341066, Exhibits Cytoreductive Antitumor Efficacy through Antiproliferative and Antiangiogenic Mechanisms. Cancer Res. 2007, 67, 4408.
SH Ou et al. Activity of Crizotinib (PF02341066), a Dual Mesenchymal-Epithelial Transition (MET) and Anaplastic Lymphoma Kinase (ALK) Inhibitor, in a Non-small Cell Lung Cancer Patient with De Novo MET Amplification. J. Thor. Oncol. 2011, 6(5), 942-946.
K.V. Huber et al. Stereospecific targeting of MTH1 by (S)-crizotinib as an anticancer strategy. Nature. 2014, doi: 10.1038/nature13194. [Epub ahead of print]
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
c-MET
p53-Tumor Suppression
RTK class X; EC 2.7.10.1
ALK
Pfizer Licensed Products
ALK
c-MET Inhibitor; NPM-ALK inhibitor
Chemical name
(R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[877399-52-5]
Order
Size
Unit Price
Stock
10 mg
€80.00
In Stock | | axonmedchem |
| CPI 0610 | Axon 2594
CAS [1380087-89-7]
MF C20H16ClN3O2MW 365.81
Purity:
99%
Soluble in DMSO
Description
Selective and metabolically stable inhibitor of the BET family of bromodomains (BET-BRD; IC50 values 0.12 - 0.17 µM and 0.22 µM for inhibition of BD-1 of BRD2-4 and BRDT, respectively), demonstrating a correlation between BET-driven reduction in MYC gene expression and tumor growth inhibition in a xenograft study. CPI 0610 displays essentially no activity in TR-FRET- or AlphaLisabased assays against the bromodomains of CBP, BRD9, BRPF1, PCAF, BRG1, ATAD2, TRIM24, BRD8 (IC50 value > 15 µM), and no meaningful inhibition in a CEREP express panel of about 50 GPCRs, ion channels, and transporters.
*Constellation Pharmaceuticals Inc compound; sold under agreement with Constellation Pharmaceuticals Inc. | | axonmedchem |
| OF-1 | Axon 2442
CAS [919973-83-4]
MF C17H18BrN3O4SMW 440.31
Purity:
99%
Soluble in DMSO
Description
Potent Bromodomain inhibitor with selectivity for BRPF1 and BRPF2 (Kd values 100 nM, 500 nM, and 2.4 μM for BRPF1B, BRPF2, and BRPF3, respectively). Selectivity against other bromodomains is very good, in general >100-fold. The closest off-target effects are against BRD4 (39-fold selectivity) and TIF1a (50% inhibition at 20 µM. OF-1 increases thermal stability in the cellular thermal shift assay (CETSA) of full length BRPF1B at 1 µM and also demonstrates accelerated FRAP recovery at 5 µM in the BRPF2 FRAP assay.
KEYWORDS: OF1 | supplier | BRPF inhibitor | OF-1 supplier | CAS [919973-83-4] | Histone | BRPF (BRD) | Inhibitor | SGC | Bromodomain | Chromatin | BRPF1 | BRPF1B | BRPF2 | BRD4 | TIF1a | FRAP | epigenetic | DNA | | axonmedchem |
| OTX 015 | Axon 2530
CAS [202590-98-5]
MF C25H22ClN5O2SMW 491.99
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO and ethanol
Description
Potent inhibitor of BRD2, BRD3, and BRD4 (Ki values ranging from 3.2 to 24.7 nM, considering BDs 1 and 2), with clear anti-proliferative activity on a large number of diffuse large B-cell lymphoma (DLBCL) cell lines. OTX 015 inhibits the growth of hematologic malignances through directly regulating MYC expression and activity.
KEYWORDS: OTX 015 | supplier | BET-BRD inhibitor | OTX015 | CAS [202590-98-5] | Histone | BET (BRD) | Inhibitor | BRD2 | BRD3 | BRD4 | tumor | apoptosis | G1 | cell cycle | diffuse large B-cell lymphoma | DLBCL | MYC | | axonmedchem |
| CHR 6494 trifluoroacetate | Axon 2250
CAS [1458630-17-5]
MF C16H16N6.C2HF3O2MW 406.36
Purity:
99%
Soluble in DMSO
Description
Specific, first-in-class inhibitor of histone kinase Haspin, which blocks H3T3 phosphorylation in association with a characteristic spindle and centrosome phenotype (IC50 values are 500 nM, 473 nM and 752 nM for apoptosis induction in HCT-116, HeLa and MDA-MB-231 cells, respectively). CHR 6494 causes arrest in G2/M, induces apoptosis and possesses ex vivo anti-angiogenesis features and antitumoral properties in a nude mice xenograft model. Haspin function is critical in mitosis, favouring chromosome cohesion, metaphase alignment and progression through the cell cycle.
References
Certificates
Categories
Extra info
Huertas, D. et al. Antitumor activity of a small-molecule inhibitor of the histone kinase Haspin. Oncogene (2012), 31(11), 1408-1418.
Cuny, Gregory D. et al. Structure-activity relationship study of beta-carboline derivatives as haspin kinase inhibitors. Bioorg. Med. Chem. Lett. 2012, 22, 2015-2019.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
DNA-damage Response
Haspin
EC 2.7.11.1
Specific, first-in-class inhibitor of histone kinase Haspin
Chemical name
3-(1H-Indazol-5-yl)-N-propylimidazo[1,2-b]pyridazin-6-amine trifluoroacetate
Parent CAS No.
[1333377-65-3]
Order
Size
Unit Price
Stock
10 mg
€120.00
In Stock | | axonmedchem |
| GSK 5959 | Axon 2410
CAS [901245-65-6]
MF C22H26N4O3MW 394.47
Purity:
99%
Soluble in DMSO
Description
Potent, cell permeable inhibitor of BRPF1 bromodomain with excellent selectivity over other bromodomains (pIC50 values 7.1 (BRPF1), 5.1 (BRPF2), and <4.3 (BRD4-BD1).
References
Certificates
Categories
Extra info
E.H. Demont et al. 1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain. ACS Med Chem Lett. 2014 Sep 10;5(11):1190-5.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
BRPF (BRD)
Potent, cell permeable inhibitor of BRPF1 bromodomain
Chemical name
N-(1,3-dimethyl-2-oxo-6-(piperidin-1-yl)-2,3-dihydro-1H-benzo[d]imidazol-5-yl)-2-methoxybenzamide
Parent CAS No.
[901245-65-6]
Order
Size
Unit Price
Stock
10 mg
€135.00
In Stock | | axonmedchem |
| PFI-1 - PF 06405761 | Axon 1887
CAS [1403764-72-6]
MF C16H17N3O4SMW 347.39
Purity:
98%
Soluble in DMSO
Description
BET bromodomain inhibitor; chemical probe developed by SGC and Pfizer.
KEYWORDS: PFI-1 | supplier | BETinhibitor | PF 06405761 | PFI1 | PF06405761 | CAS [1403764-72-6] | Histone | BET(BRD) | Inhibitor | bromodomain | SGC| Pfizer | | axonmedchem |
| PK 11195, (R)-(-)-N-Desmethyl- | Axon 2784
CAS [157809-85-3]
MF C20H19ClN2OMW 338.83
Purity:
99%
Optical purity:
99% ee
Soluble in DMSO
Description
Precursor for (R)-[N-methyl-11C]PK 11195 for PET studies. Radioligand precursor of the peripheral benzodiazepine antagonist (R)-[N-methyl-11C]PK 11195.
KEYWORDS: (R)-(-)-N-Desmethyl-PK 11195 | supplier | (R)-(-)-PK 11195 radioligand precursor | (R)-(-)-N-Desmethyl-PK11195 | (R)-(-)-N-Desmethyl-PK-11195 | CAS [157809-85-3] | GABA | GABA-A | Antagonist | Ion Channels | PET | | axonmedchem |
| PK 11195, (R)-(-)- | Axon 2785
CAS [205934-46-9]
MF C21H21ClN2OMW 352.86
Purity:
99%
Optical purity:
98% ee
Soluble in DMSO
Description
(R)-enantiomer of PK 11195 (Axon 1208), a peripheral benzodiazepine antagonist. It is a drug reference standard of [11C](R)-PK 11195 that is used for PET study.
KEYWORDS: (R)-(-)-PK 11195 | BZD antagonist | supplier | (R)-(-)-PK11195 | (R)-(-)-PK-11195 | CAS [205934-46-9] | GABA | GABA-A | Antagonist | Ion Channels | | axonmedchem |
| GS 39783 | Axon 1820
CAS [39069-52-8]
MF C15H23N5O2SMW 337.44
Purity:
99%
Moderately soluble in DMSO
Description
Positive allosteric modulator at GABAB receptor
References
Certificates
Categories
Extra info
S Urwyler et al. N,N'-Dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine (GS39783) and structurally related compounds: novel allosteric enhancers of gamma-aminobutyric acidB receptor function. J. Pharmacol. Exp. Ther. 2003, 307(1), 322-330.
C Mombereau et al. Genetic and pharmacological evidence of a role for GABA(B) receptors in the modulation of anxiety- and antidepressant-like behavior. Neuropsychopharmacol. 2004, 29(6), 1050-1062.
P Maccioni et al. Reducing effect of the positive allosteric modulator of the GABA(B) receptor, GS39,783, on alcohol self-administration in alcohol-preferring rats. Psychopharmacology (Berlin). 2007, 193(2), 171-178.
NE Paterson et al. Positive modulation of GABA(B) receptors decreased nicotine self-administration and counteracted nicotine-induced enhancement of brain reward function in rats. J. Pharmacol. Exp. Ther. 2008, 326(1), 306-314.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
GABA-B
C2
PAM of GABA-B Receptor
Chemical name
N4,N6-dicyclopentyl-2-(methylthio)-5-nitropyrimidine-4,6-diamine
Parent CAS No.
[39069-52-8]
Order
Size
Unit Price
Stock
10 mg
€99.00
In Stock | | axonmedchem |
| CP 615003 mesylate | Axon 1604
CAS [1259477-42-3]
MF C20H24FN3O3.CH4O3SMW 469.53
Purity:
99%
Soluble in water and DMSO
Description
A potent and subtype selective GABAA receptor partial agonist potentially useful in treating generalized anxiety disorder; the Mdr1 P-glycoprotein (P-gp) substrate
References
Certificates
Categories
Extra info
CL Shaffer et al. Metabolism and disposition of a g-aminobutyric acid type A receptor partial agonist in humans. Drug Metab. Disp. (2008), 36(4), 655-662.
K Venkatakrishnan et al. Central nervous system pharmacokinetics of the Mdr1 P-glycoprotein substrate CP-615,003. Drug Metab. Disp. (2007), 35(8), 1341-1349
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
GABA-A
Unclassified
GABAA agonist
Chemical name
N-(3-fluoro-4-(2-(propylamino)ethoxy)phenyl)-4-oxo-4,5,6,7-tetrahydro-1H-indole-3-carboxamide methanesulfonate
Parent CAS No.
[329016-45-7]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| Pagoclone, (+)- - CI 1043 | Axon 1594
CAS [133737-32-3]
MF C23H22ClN3O2MW 407.89
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Subtype selective partial agonist at GABAA receptor, which binds primarily to the α2/α3 subtypes which are responsible for the anti-anxiety effects of these kind of drugs, but has relatively little efficacy at the α1 subtype which produces the sedative and memory loss effects; nonbenzodiazepine anxiolytic
References
Certificates
Categories
Extra info
JR Atack. The benzodiazepine binding site of GABA(A) receptors as a target for the development of novel anxiolytics. Exp. Opin. Invest. Drugs. 2005, 14(5), 601-618.
DJ Nutt. Alcohol alternatives - a goal for psychopharmacology? J. Psychopharmacol. 2006, 20(3), 318–320.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
GABA-A
Unclassified
GABAA-α2 and GABAA-α3 agonist
Chemical name
2-(7-chloro-1,8-naphthyridin-2-yl)-3-(5-methyl-2-oxohexyl)isoindolin-1-one
Parent CAS No.
[133737-32-3]
Order
Size
Unit Price
Stock
5 mg
€135.00
In Stock | | axonmedchem |
| NS 11394 | Axon 1457
CAS [951650-22-9]
MF C23H19N3OMW 353.42
Purity:
99%
Soluble in DMSO
Description
A unique subtype-selective GABAA receptor positive allosteric modulator (PAM); with a subtype selectivity profile at GABAA receptors of α5 > α3 > α2 > α1. Compared with other subtype-selective ligands, NS11394 is unique in having superior efficacy at GABAA-α3 receptors while maintaining low efficacy at GABAA-α1 receptors, which might be attributed for its significantly reduced side effect profile in rat.
KEYWORDS: NS 11394 | supplier | 951650-22-9 | GABAA PAM | NS11394 | GABA-A | γ-aminobutyric acid | gamma-aminobutyric acid | positive allosteric modulator | agonist | | axonmedchem |
| TP 003 | Axon 1422
CAS [628690-75-5]
MF C23H16F3N3OMW 407.39
Purity:
99%
Soluble in DMSO and Ethanol
Description
Subtype selective partial agonist at GABAA receptor, showing significant efficacy at α3; nonbenzodiazepine anxiolytic.
KEYWORDS: TP 003 | supplier | GABAA-α3 agonist | TP003 | TP-003 | CAS [628690-75-5] | GABA | GABA-A | Ion Channel | receptor | alfa-3 | anxiolytic | non-benzodiazepine | anticonvulsant | | axonmedchem |