| 产品标题 |
产品货号 |
产品规格 |
厂家 |
| AB 1010 - Masitinib mesylate | Axon 1419
CAS [1048007-93-7]
MF C28H30N6OS.CH4O3SMW 594.75
Purity:
99%
Soluble in water and DMSO
Description
A potent oral tyrosine kinase inhibitor, targeting c-KIT, PDGFR and FGFR3; oncology drug under clinical trial
References
Certificates
Categories
Extra info
P Dubreuil et al. Masitinib (AB1010), a Potent and Selective Tyrosine Kinase Inhibitor Targeting KIT. Plos ONE 2009, 4(9), e7258.
BN Bui et al. Preliminary efficacy and safety results of masitinib administered, front line in patients with advanced GIST. A phase II study. J. Clin. Onco. 2007, 25(18S), 10025.
G Giamas et al. Protein kinases as targets for cancer treatment. Pharmacogenomics. 2007, 8(8), 1005-1016.
KA Hahn et al. Masitinib is safe and effective for the treatment of canine mast cell tumors. J. Vet. Intern. Med. 2008, 22(6), 1301-1309.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
PDGFR
c-KIT
RTK class III and V; EC 2.7.10.1
FGFR
PDGFR, c-KIT and FGFR3 tyrosine kinase inhibitor
Chemical name
4-(4-Methyl-piperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl-thiazol-2-ylamino)-phenyl]-benzamide methanesulfonate
Parent CAS No.
[790299-79-5]
Order
Size
Unit Price
Stock
5 mg
€70.00
In Stock | | axonmedchem |
| Apilimod - STA 5326 | Axon 1369
CAS [541550-19-0]
MF C23H26N6O2MW 418.49
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Potent and orally active inhibitor of the cytokines interleukin-12 (IL-12), and interleukin-23 (IL-23) production; potential regulators of certain autoimmune and inflammatory diseases.The water-soluble dimesylate salt is available as well (Axon 2500).
Note: | | axonmedchem |
| Imatinib mesylate - CGP 57148B | STI 571 | Gleevec | Axon 1394
CAS [220127-57-1]
MF C29H31N7O.CH4O3SMW 589.71
Purity:
99%
Soluble in DMSO
Description
Protein kinase inhibitor, targeting Bcr-Abl/c-kit/PDGF-R.
KEYWORDS: Imatinib mesylate | supplier | Bcr-Abl inhibitor | CGP 57148B | STI 571 | Gleevec | CGP57148B | STI571 | CGP-57148B | STI-571 | CAS [220127-57-1] | [152459-95-5] | Non Selective (Phosphorylation Substrates) | BCR-ABL | c-KIT | PDGFR | Inhibitor | Enzymes | | axonmedchem |
| PD 161570 | Axon 2098
CAS [192705-80-9]
MF C26H35Cl2N7OMW 532.51
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Selective FGFR inhibitor; with IC50 values to be 40, 262 and 3700 nM for FGFR1, PDGFR and EGFR tyrosine kinases, respectively. PD 161570 suppressed constitutive phosphorylation of FGFR1 in both human ovarian carcinoma cells (A121(p)) and Sf9 insect cells overexpressing the human FGFR1 and blocked the growth of A121(p) cells in culture.
KEYWORDS: PD 161570 | supplier | FGFR inhibitor | PD161570 | CAS [192705-80-9] | FGF | FGFR | Inhibitor | Receptors | | axonmedchem |
| DCC 2036 - Rebastinib | Axon 2123
CAS [1020172-07-9]
MF C30H28FN7O3MW 553.59
Purity:
99%
Soluble in DMSO
Description
An orally active Bcr-ABL inhibitor; being a ABL Switch-control inhibitor that potently inhibits BCR-ABL1 gatekeeper mutant T315I (IC50: 0.8 nM for native ABL1 and 4 nM in a ABL1T3151 kinase assay). DCC-2036 has efficacy in a mouse model of T315I-induced CML and against cells of patients with CML. In addition, DCC-2036 also inhibited the SRC family kinases SRC, LYN, FGR, and HCK, and the receptor TKs KDR, FLT3, and TIE2, but not c-KIT (IC50 of 34 nM, 29 nM, 38 nM, 40 nM, 4 nM, 2 nM, 6 nM, and 481 nM respectively)
References
Certificates
Categories
Extra info
WW Chan et al. Conformational Control Inhibition of the BCR-ABL1 Tyrosine Kinase, Including the Gatekeeper T315I Mutant, by the Switch-Control Inhibitor DCC-2036. Cancer Cell 2011, 19(4), 556–568.
CA Eide et al. The ABL switch control inhibitor DCC-2036 is active against the chronic myeloid leukemia mutant BCR-ABLT315I and exhibits a narrow resistance profile. Cancer Res. 2011, 71(9), 3189-95.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
BCR-ABL
EC 2.7.10.1
An orally active Bcr-ABL inhibitor
Chemical name
4-(4-(3-(3-tert-butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl)ureido)-3-fluorophenoxy)-N-methylpicolinamide
Parent CAS No.
[1020172-07-9]
Order
Size
Unit Price
Stock
5 mg
€125.00
In Stock | | axonmedchem |
| NVP-BGJ398 phosphate - BGJ 398 phosphate | Infigratinib phosphate | Axon 1944
CAS [1310746-10-1]
MF C26H34Cl2N7O7PMW 658.47
Purity:
99%
Soluble in DMSO
Description
Potent and selective inhibitor of fibroblast growth factor receptor (FGFR) tyrosine kinases 1, 2, 3 and 4 (with IC50 values of 0.9, 1.4, 1.0 and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4 respectively); it showed siginificant antitumor activity in RT112 bladder cancer xenografts models overexpressing wild-type FGFR3. Phosphate salt of Axon 1775
KEYWORDS: NVP-BGJ398 phosphate | supplier | FGFR inhibitor | BGJ 398 phosphate | Infigratinib phosphate | NVPBGJ398 | NVP-BGJ 398 | CAS [1310746-10-1] | [872511-34-7] | FGF | RTK | fibroblast growth factor | tyrosine kinases | FGFR1 | FGFR2 | FGFR3 | FGFR4 | antitumor activity | RT112 xenograft | | axonmedchem |
| INNO 406 - Bafetinib | Axon 2121
CAS [859212-16-1]
MF C30H31F3N8OMW 576.62
Purity:
99%
Optical purity:
Optically pure
Soluble in 0.1N HCl(aq) and DMSO
Description
Orally bioavailable dual Bcr-Abl and Lyn kinase inhibitor with anti-CML efficacy; orally bioavailable; more potent (>10 times) than Imatinib; highly recommended Abl inhibitor in treating chronic myeloid leukaemia (CML)
References
Certificates
Categories
Extra info
A Yokota et al. INNO-406, a novel BCR-ABL/Lyn dual tyrosine kinase inhibitor, suppresses the growth of Ph+ leukemia cells in the central nervous system, and cyclosporine A augments its in vivo activity. Blood, 2007, 109(1), 306-314.
H Kantarjian et al. Phase 1 study of INNO-406, a dual Abl/Lyn kinase inhibitor, in Philadelphia chromosome-positive leukemias after imatinib resistance or intolerance. Cancer, 2010, 116(11), 2665-72.
JC Uitdehaag et al. A guide to picking the most selective kinase inhibitor tool compounds for pharmacological validation of drug targets. Br. J. Pharmacol. 2012, 166, 858–876.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
BCR-ABL
Lyn
Oncogene Fusion Proteins
EC 2.7.10.1
Dual Bcr-Abl and Lyn kinase inhibitor
Chemical name
(S)-N-(3-(4,5'-bipyrimidin-2-ylamino)-4-methylphenyl)-4-((3-(dimethylamino)pyrrolidin-1-yl)methyl)-3-(trifluoromethyl)benzamide
Parent CAS No.
[859212-16-1]
Order
Size
Unit Price
Stock
2 mg
€85.00
In Stock | | axonmedchem |
| AP 24534 - Ponatinib | Axon 1857
CAS [943319-70-8]
MF C29H27F3N6OMW 532.56
Purity:
98%
Soluble in DMSO
Description
Potent and orally active tyrosine kinase inhibitor, targeting BCR-ABL and multiple RTK
References
Certificates
Categories
Extra info
T O'Hare et al. AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance. Cancer Cell. 2009, 16(5), 401-412.
WS Huang et al. Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of (...). J. Med. Chem. 2010, 53(12), 4701-4719.
T Zhou et al. Structural mechanism of the Pan-BCR-ABL inhibitor ponatinib (AP24534): lessons for overcoming kinase inhibitor resistance. Chem. Biol. Drug Des. 2011, 77(1), 1-11.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
BCR-ABL
Oncogene Fusion Proteins
EC 2.7.10.1
BCR-ABL kinase inhibitor (including T315I mutation)
Chemical name
3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide
Parent CAS No.
[943319-70-8]
Order
Size
Unit Price
Stock
5 mg
€90.00
In Stock | | axonmedchem |
| GNF 2 | Axon 1882
CAS [778270-11-4]
MF C18H13F3N4O2MW 374.32
Purity:
99%
Soluble in DMSO
Description
Selective and allosteric inhibitor of Bcr-Abl tyrosine kinase, with IC50 of 267 nM and inactive at a panel of 63 other kinases, including native c-Abl; A new class of Bcr-Abl inhibitor to treat resistant Chronic myelogenous leukemia (CML)
References
Certificates
Categories
Extra info
FJ Adrián et al. Allosteric inhibitors of Bcr-abl–dependent cell proliferation. Nature Chem. Biol. 2006, 2, 95-102.
J Zhang, FJ Adrián et al. Targeting Bcr–Abl by combining allosteric with ATP-binding-site inhibitors. Nature 2010, 463, 501-506.
O Hantschel. Allosteric BCR-ABL inhibitors in Philadelphia chromosome-positive acute lymphoblastic leukemia: novel opportunities for drug combinations to overcome resistance. Haematol. 2012, 97(2), 157-159.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
BCR-ABL
Oncogene Fusion Proteins
EC 2.7.10.1
Inhibitor of Bcr-Abl tyrosine kinase
Chemical name
3-(6-(4-(trifluoromethoxy)phenylamino)pyrimidin-4-yl)benzamide
Parent CAS No.
[778270-11-4]
Order
Size
Unit Price
Stock
10 mg
€125.00
In Stock | | axonmedchem |
| PD 180970 | Axon 1137
CAS [287204-45-9]
MF C21H15Cl2FN4OMW 429.27
Purity:
99%
Soluble in DMSO
Description
PD180970 inhibits p210(Bcr-Abl) tyrosine kinase and induces apoptosis in Bcr-Abl-expressing leukemic cells
References
Certificates
Categories
Extra info
P La Rosée et al. Activity of the Bcr-Abl kinase inhibitor PD180970 against clinically relevant Bcr-Abl isoforms that cause resistance to imatinib mesylate (Gleevec, STI571). Cancer Res. 2002, 62 (24), 7149-53.
TS May. Gleevec: tailoring to fit. Drug Discovery Today (DDT), 2003, 8 (5), 188-189.
M Huang et al. Inhibition of Bcr-Abl kinase activity by PD180970 blocks constitutive activation of Stat5 and growth of CML cells. Oncogene. 2002, 21(57), 8814-8816.
JM Goldman, JV Melo. BCR-ABL in Chronic Myelogenous Leukemia - How Does It Work? Acta Haematol 2008, 119, 212-217.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
BCR-ABL
Oncogene Fusion Proteins
EC 2.7.10.1
Bcr-Abl tyrosine kinase inhibitor (p210 specific)
Chemical name
6-(2,6-Dichloro-phenyl)-2-(4-fluoro-3-methyl-phenylamino)-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one
Parent CAS No.
[287204-45-9]
Order
Size
Unit Price
Stock
10 mg
€120.00
In Stock | | axonmedchem |
| Nilotinib - AMN 107 | Tasigna | Axon 1396
CAS [641571-10-0]
MF C28H22F3N7OMW 529.52
Purity:
99%
Soluble in DMSO
Description
A highly selective inhibitor of Bcr-Abl, the definitive cause of Ph+ CML, and its mutations
References
Certificates
Categories
Extra info
H Kantarjian et al. Nilotinib in imatinib-resistant CML and Philadelphia chromosome-positive ALL. N. Engl. J. Med. 2006, 354 (24), 2542–51.
E Weisberg et al. AMN107 (nilotinib): a novel and selective inhibitor of BCR-ABL. Br. J. Cancer 2006, 94, 1765-1769.
JM Goldman, JV Melo. BCR-ABL in Chronic Myelogenous Leukemia - How Does It Work? Acta Haematol. 2008, 119, 212-217.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
BCR-ABL
Oncogene Fusion Proteins
EC 2.7.10.1
BCR-ABL inhibitor
Chemical name
4-methyl-N-[3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino] benzamide
Parent CAS No.
[641571-10-0]
Order
Size
Unit Price
Stock
5 mg
€70.00
In Stock | | axonmedchem |
| LY 2874455 - LM 1476 | Axon 1981
CAS [1254473-64-7]
MF C21H19Cl2N5O2MW 444.31
Purity:
99%
Soluble in DMSO
Description
Potent and selective FGFR inhibitor; LY2874455 inhibits autophosphorylation of FGFR-1, FGFR-2, FGFR-3, and FGFR-4 (with in vitro IC50 values of 2.8, 2.6, 6.4, and 6 nM, respectively), which is required for activation of FGF-induced downstream signaling
References
Certificates
Categories
Extra info
G Zhao et al. A Novel, Selective Inhibitor of Fibroblast Growth Factor Receptors That Shows A Potent Broad-spectrum of Anti-tumor Activity in Several Tumor Xenograft Models. Mol. Cancer Ther. 2011, 10, 2200.
AN Brooks et al. Molecular Pathways: Fibroblast Growth Factor Signaling: A New Therapeutic Opportunity in Cancer. Clin. Cancer Res. 2012, 18, 1855.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
RTK class V; EC 2.7.10.1
FGFR
Potent and selective FGFR inhibitor
Chemical name
(R,E)-2-(4-(2-(5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazol-3-yl)vinyl)-1H-pyrazol-1-yl)ethanol
Parent CAS No.
[1254473-64-7]
Order
Size
Unit Price
Stock
2 mg
€110.00
In Stock | | axonmedchem |
| AZD 4547 | Axon 1917
CAS [1035270-39-3]
MF C26H33N5O3MW 463.57
Purity:
99%
Soluble in DMSO
Description
Orally available, potent and selective FGFR inhibitor
References
Certificates
Categories
Extra info
PR Gavine et al. AZD4547: an orally bioavailable, potent, and selective inhibitor of the fibroblast growth factor receptor tyrosine kinase family. Cancer Res. 2012, 72(8), 2045-2056.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
RTK class V; EC 2.7.10.1
FGFR
Potent and selective FGFR inhibitor
Chemical name
N-(5-(3,5-dimethoxyphenethyl)-1H-pyrazol-3-yl)-4-((3R,5S)-3,5-dimethylpiperazin-1-yl)benzamide, rel-
Parent CAS No.
[1035270-39-3]
Order
Size
Unit Price
Stock
5 mg
€85.00
In Stock | | axonmedchem |
| PD 173074 | Axon 1673
CAS [219580-11-7]
MF C28H41N7O3MW 523.67
Purity:
99%
Soluble in DMSO and Ethanol
Description
Potent and selective FGFR inhibitor with IC50 to be 21.5 and 5 nM for FGRF1 and FGFR3 inhibition respectively
References
Certificates
Categories
Extra info
OE Pardo et al. The Fibroblast Growth Factor Receptor Inhibitor PD173074 Blocks Small Cell Lung Cancer Growth In vitro and In vivo. Cancer Res. 2009, 69, 8645.
M Miyake et al. 1-tert-butyl-3-[6-(3,5-dimethoxy-phenyl)-2-(4-diethylamino-butylamino)-pyrido[2,3-d]pyrimidin-7-yl]-urea (PD173074), a selective tyrosine kinase inhibitor of FGFR3 (...). J. Pharmacol. Exp. Ther. 2010, 332 795.
L Zaragosi et al. Autocrine fibroblast growth factor 2 signaling is critical for self-renewal of human multipotent adipose-derived stem cells. Stem Cells 2006, 24 2412-2419.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
Stem Cell
RTK class V; EC 2.7.10.1
Stem Cell Differentiator
FGFR
Pfizer Licensed Products
FGFR1 and FGFR3 inhibitor
Chemical name
1-tert-butyl-3-(2-(4-(diethylamino)butylamino)-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl)urea
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[219580-11-7]
Order
Size
Unit Price
Stock
5 mg
€75.00
In Stock | | axonmedchem |
| NVP-BGJ398 - BGJ 398 | Infigratinib | Axon 1775
CAS [872511-34-7]
MF C26H31Cl2N7O3MW 560.48
Purity:
99%
Soluble in DMSO
Description
Potent and selective inhibitor of fibroblast growth factor receptor (FGFR) tyrosine kinases 1, 2, 3 and 4 (with IC50 values of 0.9, 1.4, 1.0 and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4 respectively); it showed siginificant antitumor activity in RT112 bladder cancer xenografts models overexpressing wild-type FGFR3.The phosphate salt of NVP-BGJ398 (Axon 1944) is available as well.
KEYWORDS: NVP-BGJ398 | supplier | FGFR inhibitor | BGJ 398 | Infigratinib | NVP-BGJ398 | BGJ398 | CAS [872511-34-7] | FGF | RTK | fibroblast growth factor | tyrosine kinases | FGFR1 | FGFR2 | FGFR3 | FGFR4 | antitumor activity | RT112 xenograft | | axonmedchem |
| UNC 569 | Axon 2086
CAS [1350547-65-7]
MF C22H29FN6MW 396.50
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Potent, reversible and ATP-competitive inhibitor of Mer receptor tyrosine kinase (RTK) (IC50: 2.9 nM). UNC 569 inhibits Mer activation and downstream signaling through ERK1/2 and AKT and was capable of inducing >50% reduction in tumor burden compared to references. Potential therapeutic for acute lymphoblastic leukemia (ALL) and atypical teratoid/rhabdoid tumors (ATRT).
KEYWORDS: UNC 569 | supplier | Mer Inhibitor | UNC569 | CAS [1350547-65-7] | Gas6 | Mer | Inhibitor | Receptors | RTK | | axonmedchem |
| OTX 008 - PTX 008 | Calixarene 0118 | Axon 2332
CAS [286936-40-1]
MF C52H72N8O8MW 937.18
Purity:
99%
Soluble in DMSO and Ethanol
Description
Selective allosteric inhibitor of galectin-1, downregulates cancer cell proliferation, invasion and tumor angiogenesis. OTX008 inhibited galectin-1 expression and ERK1/2 and Akt-dependent survival pathways, and induced G2/M cell cycle arrest through CDK1.
References
Certificates
Categories
Extra info
L. Astorgues-Xerri et al. OTX008, a selective small-molecule inhibitor of galectin-1, downregulates cancer cell proliferation, invasion and tumour angiogenesis. Eur. J. Cancer. 2014, 50, 2463-2477.
M. Zucchetti et al. Pharmacokinetics and antineoplastic activity of galectin-1-targeting OTX008 in combination with sunitinib. Cancer Chemother. Pharmacol. 2013, 72, 879-887.
R.O. Dings et al. Polycationic calixarene PTX013, a potent cytotoxic agent against tumors and drug resistant cancer. Invest. New Drugs. 2013, 31, 1142-1150.
R.P. Dings et al. Antitumor agent calixarene 0118 targets human galectin-1 as an allosteric inhibitor of carbohydrate binding. J. Med. Chem. 2012, 55, 5121-5129.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Immunology
PI3K-Akt-mTOR
Galectin
Selective allosteric inhibitor of galectin-1
Chemical name
2,2',2'',2'''-[Pentacyclo[19.3.1.13,7.19,13.115,19]octacosa-1(25),3,5,7(28),9,11,13(27),15,17,19(26),21,23-dodecaene-5,11,17,23-tetrayltetrakis(oxy)]tetrakis[N-[2-(dimethylamino)ethyl]-acetamide
Parent CAS No.
[286936-40-1]
Order
Size
Unit Price
Stock
5 mg
€125.00
In Stock | | axonmedchem |
| SSR 128129E | Axon 2234
CAS [848318-25-2]
MF C18H15N2NaO4MW 346.31
Purity:
99%
Soluble in water and DMSO
Description
Extracellularly acting, small-molecule, allosteric inhibitor of FGF receptor signaling with oral bioavailability. SSR 128129E inhibits responses mediated by FGFR1-4 (IC50 values 15-28 nM for FGF2 induced FGFR stimulation), but not by other related RTKs.SSR 128129E does not inhibit all FGFR signaling pathways indiscriminatively but selectively blocks particular signaling pathways, dependent on the cellular context. Capable of inhibiting angiogenesis, inflammation, and bone resorption in arthritis, and delays tumor growth and metastasis.
References
Certificates
Categories
Extra info
C. Herbert et al. Molecular mechanism of SSR128129E, an extracellularly acting, small-molecule, allosteric inhibitor of FGF receptor signaling. Cancer Cell. 2013, 23, 489-501.
F. Bono et al. Inhibition of tumor angiogenesis and growth by a small-molecule multi-FGF receptor blocker with allosteric properties. Cancer Cell. 2013, 23, 477-488.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
Pain & Inflammation
RTK class V; EC 2.7.10.1
FGFR
Allosteric inhibitor of FGF receptor signaling
Chemical name
sodium 2-amino-5-(1-methoxy-2-methylindolizine-3-carbonyl)benzoate
Parent CAS No.
[848463-13-8]
Order
Size
Unit Price
Stock
10 mg
€99.00
In Stock | | axonmedchem |
| CT 53518 - MLN 518 | Tandutinib | Axon 1415
CAS [387867-13-2]
MF C31H42N6O4MW 562.70
Purity:
99%
Soluble in DMSO
Description
An oral tyrosine kinase inhibitor (TKI), targeting FLT3 (FMS-Like Tyrosine kinase-3), c-KIT and PDGFR, thereby inhibiting cellular proliferation and inducing apoptosis.
References
Certificates
Categories
Extra info
L Kelly et al. CT53518, a novel selective FLT3 antagonist for the treatment of acute myelogenous leukemia (AML). Cancer Cell , 2003, 1(5), 421 - 432. [online abstract]
IJ Griswold et al. Effects of MLN518, a dual FLT3 and KIT inhibitor, on normal and malignant hematopoiesis. Blood 2004, 104(9), 2912-8. [online abstract]
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Apoptosis
Cell Signaling & Oncology
FLT3
PDGFR
c-KIT
RTK class III; EC 2.7.10.1
PDGFR, c-KIT and FLT3 tyrosine kinase inhibitor
Chemical name
4-[7-(3-Piperidin-1-yl-propoxy)-quinazolin-4-yl]-piperazine-1-carboxylic acid (4-isopropoxy-phenyl)-amide
Parent CAS No.
[387867-13-2]
Order
Size
Unit Price
Stock
5 mg
€75.00
In Stock | | axonmedchem |
| RIPA-56 | Axon 2677
CAS [1956370-21-0]
MF C13H19NO2MW 221.30
Purity:
99%
Soluble in DMSO
Description
Highly potent, selective, and metabolically stable inhibitor of receptor-interacting protein 1 (RIP1; IC50 value 13 nM) for the treatment of systemic inflammatory response syndrome (SIRS). RIPA-56 efficiently reduced TNFα-induced mortality and multiorgan damage.
KEYWORDS: RIPA-56 | supplier | RIP1 inhibitor | RIPA56 | RIPA 56 | CAS [1956370-21-0] | Axon Medchem | Axon 2677 | RIP kinase | SIRS | necrotic cell death pathway | inflammation | | axonmedchem |
| DRI-C21045 | Axon 2887
CAS [2101765-81-3]
MF C32H24N2O7SMW 580.61
Purity:
98%
Soluble in DMSO
Recently added | | axonmedchem |
| SGX 523 | Axon 1914
CAS [1022150-57-7]
MF C18H13N7SMW 359.41
Purity:
99%
Soluble in DMSO
Description
ATP-competitive kinase inhibitor remarkable for its exquisite selectivity for MET (IC50: 4 nM)
References
Certificates
Categories
Extra info
SG Buchanan et al. SGX523 is an exquisitely selective, ATP-competitive inhibitor of the MET receptor tyrosine kinase with antitumor activity in vivo. Mol. Cancer Ther. 2009, 8(12), 3181-3190.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
c-MET
RTK class X; EC 2.7.10.1
ATP-competitive inhibitor of c-MET
Chemical name
6-(6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-ylthio)quinoline
Parent CAS No.
[1022150-57-7]
Order
Size
Unit Price
Stock
10 mg
€120.00
In Stock | | axonmedchem |
| GSK481 - GSK'481 | Axon 2608
CAS [1622849-58-4]
MF C21H19N3O4MW 377.39
Purity:
98%
Soluble in DMSO
Description
Potent inhibitor of Receptor-interacting serine/threonine-protein kinase 1 (RIPK1 or RIP1; IC50 value 2.8 nM for inhibition of S166 phosphorylation of hWT RIP1) exhibiting a remarkable specificity over >450 other kinases. GSK'481 protects against TNF-induced inflammation and lethal shock.
KEYWORDS: GSK481 | supplier | RIP1 kinase inhibitor | GSK'481 | CAS [1622849-58-4] | Phosphorylation | RIP | inflammation | TNF | RIPK1 | | axonmedchem |
| Necrostatin-1 | Axon 1258
CAS [4311-88-0]
MF C13H13N3OSMW 259.33
Purity:
99%
Soluble in DMSO
Description
A cell-permeable, potent, and selective inhibitor of necroptosis; Acts as a selective and ATP-competitive inhibitor of RIP1 kinase with negligible effect of RIP2 kinase activity
References
Certificates
Categories
Extra info
A. Degterev et al. Identification of RIP1 kinase as a specific cellular target of necrostatins. Nature Chem. Biol. 2008, 4, 313-321.
A. Degterev et al. Chemical inhibitor of nonapoptotic cell death with therapeutic potential for ischemic brain injury. Nature Chem. Biol. 2005, 1, 112.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
Immunology
Pain & Inflammation
NF-κB
MAPK
DNA-damage Response
EC 2.7.11.1
RIP
RIP1 inhibitor
Chemical name
5-((1H-indol-3-yl)methyl)-3-methyl-2-thioxoimidazolidin-4-one
Parent CAS No.
[4311-88-0]
Order
Size
Unit Price
Stock
25 mg
€95.00
In Stock | | axonmedchem |
| LBH 589 - NVP-LBH 589 | Panobinostat | Axon 1548
CAS [404950-80-7]
MF C21H23N3O2MW 349.43
Purity:
98%
Soluble in DMSO
Description
Highly potent and oral inhibitor of histone deacetylase (HDAC) with IC50 of HDAC1 to be 0.23 nM; an investigational drug against human pancreatic cancer, T cell lymphoma and other types of malignant diseases. In vitro LBH 589 induces cell cycle arrest and apoptosis through both caspase dependent and caspase independent pathways in various tumor cell types at nanomolar concentrations. In vivo LBH 589 inhibits tumor angiogenesis as evidenced by blocking new blood vessel formation in human prostate carcinoma cell PC 3 xenografts
References
Certificates
Categories
Extra info
P Maiso et al. The Histone Deacetylase Inhibitor LBH589 Is a Potent Antimyeloma Agent that Overcomes Drug Resistance. Cancer Res. 2006, 66(11), 5781-5789.
AA Lane and BA Chabner. Histone Deacetylase Inhibitors in Cancer Therapy. J. Clin. Oncol. 2009, 27(32), 5459 - 5468.
L Ellis et al. The histone deacetylase inhibitors LAQ824 and LBH589 do not require death receptor signaling or a functional apoptosome to mediate tumor cell death or therapeutic efficacy. Blood, 2009, 114(2), 380 - 393.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
DNA-damage Response
EC 3.5.1.98
HDAC
HDAC1 Inhibitor
Chemical name
(E)-N-Hydroxy-3-(4-{[2-(2-methyl-1H-indol-3-yl)-ethylamino]-methyl}-phenyl)-acrylamide
Parent CAS No.
[404950-80-7]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| GSK 2982772 | Axon 2713
CAS [1622848-92-3]
MF C20H19N5O3MW 377.40
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
GSK2982772 potently binds to RIP1 with exquisite kinase specificity (IC50 value of 1.0 nM; ADP-Glo activity assay) and has excellent activity in blocking many TNF-dependent cellular responses (IC50 value of 6.3 nM; human monocytic U937 cellular assay). The inhibitor was also able to reduce spontaneous production of cytokines from human ulcerative colitis explants. First-in-class RIP1 inhibitor to enter clinical trials for psoriasis, rheumatoid arthritis, and ulcerative colitis.
KEYWORDS: GSK 2982772 | supplier | RIP1 inhibitor | GSK-2982772 | GSK2982772 | CAS [1622848-92-3] | Non Selective (Phosphorylation Substrates) | RIP | Inhibitor | Enzymes | | axonmedchem |
| ARQ 197 - Tivantinib | Axon 1838
CAS [905854-02-6]
MF C23H19N3O2MW 369.42
Purity:
98%
Soluble in DMSO
Description
Selective, non-ATP-competitive and orally bioavailable inhibitor of c-MET receptor tyrosine kinase (RTK)
References
Certificates
Categories
Extra info
N Munshi et al. ARQ 197, a Novel and Selective Inhibitor of the Human c-Met Receptor Tyrosine Kinase with Antitumor Activity. Mol. Cancer Ther. 2010, 9, 1544-1553.
R Bagai et al. ARQ-197, an oral small-molecule inhibitor of c-Met for the treatment of solid tumors. IDrugs. 2010, 13(6), 404-414.
AA Adjei et al. Early clinical development of ARQ 197, a selective, non-ATP-competitive inhibitor targeting MET tyrosine kinase for the treatment of advanced cancers. Oncologist. 2011, 16(6), 788-799.
S Eathiraj et al. Discovery of a novel mode of protein kinase inhibition characterized by the mechanism of inhibition of human mesenchymal-epithelial transition factor (c-Met) protein autophosphorylation (...). J. Biol. Chem. 2011, 286(23), 20666-20676.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
c-MET
RTK class X; EC 2.7.10.1
c-MET tyrosine kinase Inhibitor
Chemical name
(3R,4R)-3-(2,3-dihydro-1H-pyrrolo[3,2,1-ij]quinolin-6-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione
Parent CAS No.
[905854-02-6]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| PF 04217903 mesylate | Axon 1583
CAS [956906-93-7]
MF C19H16N8O.CH4O3SMW 468.49
Purity:
99%
Soluble in 0.1N HCl(aq)
Description
An orally bioavailabe tyrosine kinase inhibitor, targeting MET (or c-MET); it selectively binds to and inhibits mesenchymal epithelial transition (low nM Ki values and >1000 fold selective relative to 208 kinases) with potential antineoplastic activity
References
Certificates
Categories
Extra info
SL Timofeevski et al. Enzymatic characterization of c-Met receptor tyrosine kinase oncogenic mutants and kinetic studies with aminopyridine and triazolopyrazine inhibitors. Biochemistry. 2009, 48(23), 5339-49.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
c-MET
RTK class X; EC 2.7.10.1
c-MET tyrosine kinase Inhibitor
Chemical name
2-(4-(1-(quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl)-1H-pyrazol-1-yl)ethanol methanesulfonate
Parent CAS No.
[956905-27-4]
Order
Size
Unit Price
Stock
5 mg
€80.00
In Stock | | axonmedchem |
| Tucidinostat - Chidamide | HBI-8000 | CS 055 | Epidaza | Axon 2893
CAS [1616493-44-7]
MF C22H19FN4O2MW 390.41
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Tucidinostat (Chidamide) is an orally bioavailable inhibitor of HDAC1, HDAC2, HDAC3, and HDAC10 with IC50 values of 0.095, 0.160, 0.067, 0.078 µM, respectively. Tucidinostat exhibits a significant and broad spectrum in vitro and in vivo antitumor activity, including a wide therapeutic index.
Keywords: Tucidinostat | supplier | HDAC inhibitor | Chidamide | HBI-8000 | CS 055 | Epidaza | HBI8000 | HBI 8000 | CS055 | CS-055 | CAS [1616493-44-7] | Histone | HDAC | Inhibitor | Enzymes | | axonmedchem |
| UF 010 | Axon 2518
CAS [537672-41-6]
MF C11H15BrN2OMW 271.15
Purity:
98%
Soluble in DMSO and Ethanol
Description
Class I selective HDAC inhibitor (IC50 values 0.5 μM, 0.1 μM, 0.06 μM, and 1.5 μM for HDAC1, HDAC2, HDAC3, and HDAC8 respectively) that inhibits cancer cell proliferation. Consistently induced the accumulation of acetylated histones (H2B, H3, and H4 but no effect on H2A) and p53 in vitro, without affecting α-tubulin.
KEYWORDS: UF 010 | supplier | HDAC inhibitor | UF010 | CAS [537672-41-6] | Histone | deacetylase | HDAC | Inhibitor | HDAC1 | HDAC2 | HDAC3 | HDAC8 | tubulin | epigenetic | inflammation | tumor suppressor | antiproliferative | | axonmedchem |
| AR-42 | Axon 2394
CAS [935881-37-1]
MF C18H20N2O3MW 312.36
Purity:
99%
Optical purity:
optically pure
Soluble in DMSO
Description
AR-42 is a novel HDAC inhibitor (IC50 value of 16 nM) with potent anticancer effects in pancreatic cancer cells at submicromolar concentrations by inducing cell cycle arrest, stimulating apoptosis, and regulating expression of several miRNAs. Also demonstrated anticancer activity in many other cancers, including acute myeloid leukemia, multiple myeloma, prostate cancer, ovarian cancer, human glioma cells, and bladder cancer.
KEYWORDS: AR-42 | supplier | HDAC inhibitor | AR 42 | AR42 | CAS [935881-37-1] | Histone | HDAC | Inhibitor | Enzymes | | axonmedchem |
| Mocetinostat - MGCD 0103 | MG 0103 | Axon 2505
CAS [726169-73-9]
MF C23H20N6OMW 396.44
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Class I selective HDAC inhibitor (sub-micromolar IC50 values for HDAC1, HDAC2, and HDAC11, ca 2 μM for HDAC3, and >10 μM for HDAC4-8) with broad spectrum antitumor activity in vitro and in vivo. MGCD 0103 induced hyperacetylation of histones, selectively induced apoptosis, caused cell cycle blockade, and exhibited potent and selective antiproliferative activities against a broad spectrum of human cancer cell lines in vitro.
KEYWORDS: Mocetinostat | Supplier | HDAC inhibitor | MGCD 0103 | MG 0103 | MG0103 | MGCD0103 | CAS [726169-73-9] | Histone | HDAC1 | HDAC2 | HDAC3 | HDAC11 | deacetylase | antitumor | hyperacetylation | apoptosis | cell cycle | blockade | isotype-selective | | axonmedchem |
| Santacruzamate A - CAY 10683 | Axon 2495
CAS [1477949-42-0]
MF C15H22N2O3MW 278.35
Purity:
99%
Soluble in DMSO
Description
Picomolar level Class I HDAC2 inhibitor (IC50 value 0.11 nM) with relatively little inhibition of HDAC4 or HDAC6 (IC50 values >1000 nM and 433 nM, respectively). Cytotoxin with several structural features in common with Vorinostat, a clinically approved HDAC inhibitor used to treat refractory cutaneous T-cell lymphoma.
Note: Potency of synthetic Santacruzamate A is questioned due to lack of cytotoxicity tested in two cancer cell lines (Q. Liu et al. 2015)
References
Certificates
Categories
Extra info
C.M. Pavlik et al. Santacruzamate A, a potent and selective histone deacetylase inhibitor from the Panamanian marine cyanobacterium cf. Symploca sp. J Nat Prod. 2013 Nov 22;76(11):2026-33.
Q. Liu et al. Synthesis and biological evaluation of santacruzamate A and analogs as potential anticancer agents. RSC Adv. 2015,5, 1109-1112.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
DNA-damage Response
EC 3.5.1.98
HDAC
Picomolar level HDAC2 inhibitor with little inhibition of HDAC4 and HDAC6
Chemical name
ethyl 4-oxo-4-(phenethylamino)butylcarbamate
Parent CAS No.
[1477949-42-0]
Order
Size
Unit Price
Stock
10 mg
€85.00
In Stock | | axonmedchem |
| LW 479 | Axon 2430
CAS [1688677-89-5]
MF C21H23BrN2O4SMW 479.39
Purity:
98%
Soluble in DMSO
Description
HDAC inhibitor that shows marked cytotoxicity and induces apoptosis as well as cell cycle arrest in a panel of breast cancer cell lines. LW479 silences EGFR expression in breast cancer cells through disrupting Sp1 and HDAC1 binding to EGFR promoter, and blocks EGF/EGFR signalling pathway and EGF-stimulated motility. Moreover, LW-479 attenuates breast cancer metastasis to the lung.
References
Certificates
Categories
Extra info
J. Li et al. Inhibition of breast cancer progression by a novel histone deacetylase inhibitor, LW479, by down-regulating EGFR expression. Br J Pharmacol. 2015 Aug;172(15):3817-30.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
DNA-damage Response
EC 3.5.1.98
HDAC
HDAC inhibitor with cytotoxicity in a panel of breast cancer cell lines.
Chemical name
6-(2-(2-(3-bromophenyl)-4-oxothiazolidin-3-yl)phenoxy)-N-hydroxyhexanamide
Parent CAS No.
[1688677-89-5]
Order
Size
Unit Price
Stock
10 mg
€135.00
In Stock | | axonmedchem |
| JNJ 26481585 dihydrochloride - Quisinostat dihydrochloride | Axon 2529
CAS [875320-31-3]
MF C21H26N6O2.2HClMW 467.39
Purity:
99%
Soluble in DMSO
Description
Potent, orally available second-generation pan-HDAC inhibitor (highest IC50 value 0.11 nM for HDAC1, and sub-nanomolar for HDAC2, HDAC4, HDAC10, and HDAC11 in vitro) with activity in human leukemia. JNJ-26481585 induces continuous acetylation of histone H3, activation of the caspase cascade, and upregulation of p21, resulting in apoptosis and cell cycle arrest in the myeloma cells at low nanomolar concentrations. JNJ26481585 also potently induced tubulin acetylation.
KEYWORDS: JNJ 26481585 HCl | supplier | HDAC inhibitor | Quisinostat dihydrochloride | JNJ26481585 | CAS [875320-31-3] | [875320-29-9] | Histone | HDAC | Inhibitor | HDAC1 | HDAC2 | HDAC4 | HDAC10 | HDAC11 | tubulin | epigenetic | apoptosis | leukemia | acetylation | | axonmedchem |
| BRD 73954 | Axon 2471
CAS [1440209-96-0]
MF C16H16N2O3MW 284.31
Purity:
99%
Soluble in DMSO
Description
First dual HDAC 6/8 inhibitor (IC50 values 9000 nM, >33000 nM, 36 nM, and 120 nM for HDAC2, 4, 6, and 8. respectively) with excellent selectivity over the other class I and II HDACs tested (75- and 130-fold less potent for the next closest isoforms). Simultaneous inhibition of HDAC6 and HDAC8 has many potential therapeutic applications, providing a larger therapeutic window than inhibition of HDAC1–3.
References
Certificates
Categories
Extra info
D.E. Olson et al. Discovery of the first histone deacetylase 6/8 dual inhibitors. J Med Chem. 2013 Jun 13;56(11):4816-20.
G. Tang et al. Identification of a novel aminotetralin class of HDAC6 and HDAC8 selective inhibitors. J Med Chem. 2014 Oct 9;57(19):8026-34.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
DNA-damage Response
EC 3.5.1.98
HDAC
Dual HDAC 6/8 inhibitor with excellent selectivity over the other HDACs
Chemical name
N1-hydroxy-N3-phenethylisophthalamide
Parent CAS No.
[1440209-96-0]
Order
Size
Unit Price
Stock
5 mg
€85.00
In Stock | | axonmedchem |
| Tubastatin A hydrochloride | Axon 2004
CAS [1310693-92-5]
MF C20H21N3O2.HClMW 371.86
Purity:
99%
Soluble in DMSO
Description
Tubastatin A is a potent and selective HDAC6 inhibitor (IC50 value of 0.015 µM), which did not display neuronal toxicity, thus forecasting the potential application of this agent to neurodegenerative conditions.
Keywords: Tubastatin A hydrochloride | supplier | HDAC6 Inhibitor | CAS [1310693-92-5] | [1252003-15-8] | Histone | HDAC | Inhibitor | Enzymes | Neuroprotective | | axonmedchem |
| RGFP 966 | Axon 2195
CAS [1357389-11-7]
MF C21H19FN4OMW 362.40
Purity:
99%
Soluble in DMSO
Description
HDAC3 specific inhibitor (IC50 value 0.08 μM) lacking affinity for any other HDAC at concentrations up to 15 μM. RGFP 966 enhances long term object memory acquisition/consolidation, and facilitates extinction of cocaine-seeking behavior in male C57BL/6J mice.
KEYWORDS: RGFP 966 | supplier | HDAC3 inhibitor | RGFP966 | CAS [1357389-11-7] | [1396841-57-8] | [1396720-94-7] | Histone | HDAC | Inhibitor | deacetylase | epigenetic | Cocaine | addiction | learning | memory | | axonmedchem |
| Sodium butyrate - Butanoic acid, sodium salt | Axon 2209
CAS [156-54-7]
MF C4H7NaO2MW 110.09
Purity:
98%
Soluble in water and DMSO
Description
Noncompetitive inhibitor of histone deacetylase (HDAC; IC50 value 0.80 mM). Butyrate inhibits most HDACs, except class III HDAC and class II HDAC6 and HDAC10. Among the fatty acids, butyrate is the most effective in inhibiting HDAC activity and arresting cell proliferation, and stimulating or repressing the expression of specific genes.
References
Certificates
Categories
Extra info
J.R. Davie. Inhibition of histone deacetylase activity by butyrate. J. Nutr. 2003, 133, S2485-S2493.
G. Bora-Tatar et al. Molecular modifications on carboxylic acid derivatives as potent histone deacetylase inhibitors: Activity and docking studies. Bioorg. Med. Chem. 2009, 17, 5219-5228.
K. Steliou et al. Butyrate histone deacetylase inhibitors. Biores. Open Access. 2012, 1, 192-198.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
DNA-damage Response
EC 3.5.1.98
Stem Cell Differentiator
HDAC
Noncompetitive inhibitor of multiple histone deacetylases (HDACs)
Chemical name
sodium butyrate
Parent CAS No.
[107-92-6]
Order
Size
Unit Price
Stock
100 mg
€50.00
In Stock | | axonmedchem |
| TMP 195 - TFMO 2 | Axon 2180
CAS [1314891-22-9]
MF C23H19F3N4O3MW 456.42
Purity:
99%
Soluble in DMSO
Description
Selective and cell-active class IIa histone deacetylase (HDAC) inhibitor, with IC50 values of 111, 106, 46, 9 nM for HDAC4, HDAC5, HDAC7 and HDAC9 respectively; >100 fold more selective vs other HDACs (IC50: >10 μM).The trifluoromethyloxadiazole (TFMO) moiety in TMP 195 as a new metal binding group circumvents the selectivity and pharmacologic liabilities of hydroxamates groups used in other metalloenzyme inhibitors. TMP 195 has a restraint impact on gene expression, and lacks overt cytotoxicity.
KEYWORDS: TMP 195 | supplier | IIa HDAC inhibitor | TFMO 2 | TMP195 | TFMO2 | TMP-195 | TFMO-2 | CAS [1314891-22-9] | Histone | Deacetylase | HDAC | Inhibitor | Enzymes | | axonmedchem |
| CI 994 - PD 123654 | Tacedinaline | Axon 2014
CAS [112522-64-2]
MF C15H15N3O2MW 269.30
Purity:
98%
Soluble in DMSO
Description
Orally bioavailable histone deacetylase (HDAC) inhibitor that causes histone hyperacetylation in living cells. CI-994 inhibited HDAC1 and HDAC2 in a concentration-dependent fashion; mediates G1 cell cycle arrest, inhibits proliferation and induces apoptosis in vitro and in vivo
References
Certificates
Categories
Extra info
AG Kraker et al. Modulation of histone acetylation by [4-(acetylamino)-N-(2-amino-phenyl) benzamide] in HCT-8 colon carcinoma. Mol. Cancer Ther. 2003, (4), 401-408.
M Loprevite et al. In Vitro Study of CI-994, a Histone Deacetylase Inhibitor, in Non-Small Cell Lung Cancer Cell Lines. Oncol. Res. Feat. Preclin. Clin. Cancer Ther. 2005, 15(1), 39-48.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
DNA-damage Response
EC 3.5.1.98
HDAC
Pfizer Licensed Products
HDAC inhibitor that causes histone hyperacetylation in living cells
Chemical name
4-acetamido-N-(2-aminophenyl)benzamide
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[112522-64-2]
Order
Size
Unit Price
Stock
10 mg
€70.00
In Stock | | axonmedchem |
| PCI 34051 | Axon 1853
CAS [950762-95-5]
MF C17H16N2O3MW 296.32
Purity:
98%
Soluble in DMSO
Description
Specific and potent histone deacetylase 8 (HDAC8) inhibitor, with >200-fold selectivity over the other HDAC isoforms. PCI-34051 induces caspase-dependent apoptosis in cell lines derived from T-cell lymphomas or leukemias, but not in other hematopoietic or solid tumor lines
References
Certificates
Categories
Extra info
S Balasubramanian et al. A novel histone deacetylase 8 (HDAC8)-specific inhibitor PCI-34051 induces apoptosis in T-cell lymphomas. Leukemia 2008, 22, 1026-1034.
SM Horwitz. The emerging role of histone deacetylase inhibitors in treating T-cell lymphomas. Curr. Hematol. Malig. Rep. 2011, 6(1), 67-72.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
DNA-damage Response
EC 3.5.1.98
HDAC
HDAC8 Inhibitor
Chemical name
N-hydroxy-1-(4-methoxybenzyl)-1H-indole-6-carboxamide
Parent CAS No.
[950762-95-5]
Order
Size
Unit Price
Stock
10 mg
€90.00
In Stock | | axonmedchem |
| Nexturastat A | Axon 2359
CAS [1403783-31-2]
MF C19H23N3O3MW 341.40
Purity:
99%
Soluble in DMSO
Description
Potent HDAC6 inhibitor with >600 fold and >190 fold selectivity over HDAC1 and HDAC8, respectively (IC50 values 5 nM, 3 µM, 1 µM for HDAC6, HDAC1, and HDAC8, respectively). Nexturastat A was found to be capable of increasing acetylated α-tubulin levels and it inhibited the growth of B16 melanoma cells, albeit with lower potency than LBH 589 (Axon 1548).
References
Certificates
Categories
Extra info
J.A. Bergman et al. Selective histone deacetylase 6 inhibitors bearing substituted urea linkers inhibit melanoma cell growth. J. Med. Chem. 2012, 55, 9891-9899.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
DNA-damage Response
EC 3.5.1.98
HDAC
HDAC6 inhibitor with good selectivity over HDAC1 and HDAC8
Chemical name
4-((1-butyl-3-phenylureido)methyl)-N-hydroxybenzamide
Parent CAS No.
[1403783-31-2]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| MS 275 - Entinostat | SNDX 275 | Axon 1803
CAS [209783-80-2]
MF C21H20N4O3MW 376.41
Purity:
99%
Soluble in DMSO
Description
Potent and long-lasting histone deacetylase (HDAC) inhibitor undergoing clinical trials for treatment of various cancers; Entinostat inhibits class I HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM, respectively
References
Certificates
Categories
Extra info
A Saito et al. A synthetic inhibitor of histone deacetylase, MS-275, with marked in vivo antitumor activity against human tumors. Proc. Natl. Acad. Sci. USA 1999, 96, 4592-4597.
M. V. Simonini et al. The benzamide MS-275 is a potent, long-lasting brain region-selective inhibitor of histone deacetylases. Proc. Natl. Acad. Sci. USA 2006, 103(5), 1587-1592.
IY Eyüpoglu et al. Experimental therapy of malignant gliomas using the inhibitor of histone deacetylase MS-275. Mol. Cancer Ther. 2006, 5, 1248-1255.
HS Lin et al. Anti-rheumatic activities of histone deacetylase (HDAC) inhibitors in vivo in collagen-induced arthritis in rodents. Br. J. Pharmacol. 2007, 150, 862-872.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
DNA-damage Response
EC 3.5.1.98
HDAC
Inhibitor of HDAC (1 and 3 Selective)
Chemical name
pyridin-3-ylmethyl 4-(2-aminophenylcarbamoyl)benzylcarbamate
Parent CAS No.
[209783-80-2]
Order
Size
Unit Price
Stock
10 mg
€80.00
In Stock | | axonmedchem |
| Pyroxamide | Axon 1801
CAS [382180-17-8]
MF C13H19N3O3MW 265.31
Purity:
98%
Soluble in DMSO
Description
Histone deacetylase (HDAC) inhibitor; a potent inhibitor of affinity-purified HDAC1 (IC50: 100 nM); an inducer of differentiation and/or apoptosis in transformed cells
References
Certificates
Categories
Extra info
LM Butler et al. Inhibition of transformed cell growth and induction of cellular differentiation by pyroxamide, an inhibitor of histone deacetylase. Clin. Cancer Res. 2001, 7(4), 962-970.
JE Bradner et al. Chemical Phylogenetics of Histone Deacetylases. Nat. Chem. Biol. 2010, 6(3), 238.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
DNA-damage Response
EC 3.5.1.98
Stem Cell Differentiator
HDAC
HDAC1 Inhibitor
Chemical name
N1-hydroxy-N8-(pyridin-3-yl)octanediamide
Parent CAS No.
[382180-17-8]
Order
Size
Unit Price
Stock
10 mg
€90.00
In Stock | | axonmedchem |
| SB 939 - Pracinostat | Axon 1777
CAS [929016-96-6]
MF C20H30N4O2MW 358.48
Purity:
99%
Soluble in DMSO
Description
Potent and oral inhibitor of histone deacetylase (HDAC), selective for class I, II and IV HDACs. SB939 shows significant antiproliferative activity against a wide variety of tumor cell lines, with high tumor exposure and efficacy in mouse models of colorectal cancer
References
Certificates
Categories
Extra info
V Novotny-Diermary et al. SB939, a novel potent and orally active histone deacetylase inhibitor with high tumor exposure and efficacy in mouse models of colorectal cancer. Mol. Cancer Ther. 2010, 9(3), 642-652.
V Novotny-Diermary et al. Pharmacodynamic evaluation of the target efficacy of SB939, an oral HDAC inhibitor with selectivity for tumor tissue. Mol. Cancer Ther. 2011, 10(7), 1207-1217.
AR Razak et al. Phase I clinical, pharmacokinetic and pharmacodynamic study of SB939, an oral histone deacetylase (HDAC) inhibitor, in patients with advanced solid tumours. Br. J. Cancer. 2011, 104(5), 756-762.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
DNA-damage Response
EC 3.5.1.98
HDAC
HDAC inhibitor (1, 2, 4 Selective)
Chemical name
(E)-3-(2-butyl-1-(2-(diethylamino)ethyl)-1H-benzo[d]imidazol-5-yl)-N-hydroxyacrylamide
Parent CAS No.
[929016-96-6]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| HDAC6 inhibitor ISOX | Axon 1645
CAS [1045792-66-2]
MF C22H30N4O6MW 446.50
Purity:
99%
Soluble in DMSO
Description
Potent and selective histone deacetylase 6 (HDAC6) inhibitor, with IC50 to be 2.4 nM (HDAC6) and 71 nM (HDAC1). (*2010 revised affinities).
KEYWORDS: HDAC6 inhibitor ISOX | supplier | HDAC6 inhibitor | ISOX | CAS [1045792-66-2] | Histone | HDAC | Inhibitor | Enzymes | | axonmedchem |
| MC 1568 | Axon 1707
CAS [852475-26-4]
MF C17H15FN2O3MW 314.31
Purity:
98%
Soluble in DMSO
Description
Potent and selective class II (IIa) histone deacetylase (HDAC) inhibitor
References
Certificates
Categories
Extra info
V Duong et al. Specific activity of class II histone deacetylases in human breast cancer cells. Mol. Cancer Res. 2008, 6(12), 1908–1919.
A Nebbioso et al. Selective class II HDAC inhibitors impair myogenesis by modulating the stability and activity of HDAC–MEF2 complexes. EMBO Rep. 2009, 10(7), 776-782.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
DNA-damage Response
EC 3.5.1.98
HDAC
HDAC inhibitor (class IIA selective)
Chemical name
3-(4-(3-(3-fluorophenyl)-3-oxoprop-1-enyl)-1-methyl-1H-pyrrol-2-yl)-N-hydroxyacrylamide
Parent CAS No.
[852475-26-4 (double bonds unspecified)]
Order
Size
Unit Price
Stock
5 mg
€85.00
In Stock | | axonmedchem |
| SU 11274 | Axon 1581
CAS [658084-23-2]
MF C28H30ClN5O4SMW 568.09
Purity:
99%
Soluble in DMSO
Description
ATP-competitive and selective MET inhibitor; inhibition of the Met kinase activity by SU11274 led to time- and dose-dependent reduced cell growth and induced G1 cell cycle arrest and apoptosis
References
Certificates
Categories
Extra info
S Berthou et al. The Met kinase inhibitor SU11274 exhibits a selective inhibition pattern toward different receptor mutated variants. Oncogene 2004, 23, 5387-5393.
PC Ma et al. Functional expression and mutations of c-Met and its therapeutic inhibition with SU11274 and small interfering RNA in non-small cell lung cancer. Cancer Res. 2005, 65, 1479-1488.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
c-MET
RTK class X; EC 2.7.10.1
ATP-competitive inhibitor of c-MET
Chemical name
(Z)-N-(3-chlorophenyl)-3-((3,5-dimethyl-4-(4-methylpiperazine-1-carbonyl)-1H-pyrrol-2-yl)methylene)-N-methyl-2-oxoindoline-5-sulfonamide
Parent CAS No.
[658084-23-2]
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5 mg
€95.00
In Stock | | axonmedchem |
| Dorsomorphin | Axon 1708
CAS [866405-64-3]
MF C24H25N5OMW 399.49
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Selective inhibitor of BMP signaling; functions through inhibition of BMP type I receptors ALK2, ALK3 and ALK6 and thus blocks BMP-mediated SMAD1/5/8 phosphorylation; Also a AMPK inhibitor (Ki value 109 nM)
* Note: The water-soluble form, Dorsomorphin dihydrochloride (Axon 2150) is also available.
References
Certificates
Categories
Extra info
PB Yu et al. Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolism. Nat. Chem. Biol. 2007, 4(1), 33-41.
J Hao et al. Dorsomorphin, a selective small molecule inhibitor of BMP signaling, promotes cardiomyogenesis in embryonic stem cells. PLoS ONE 2008, 3(8), e2904.
JH Boergermann et al. Dorsomorphin and LDN-193189 inhibit BMP-mediated Smad, p38 and Akt signalling in C2C12 cells. Intl. J. Biochem. Cell Biol. 2010, 42(11), 1802-1807.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Stem Cell
TGF-β
RSTK class I; EC 2.7.11.30
Stem Cell Differentiator
BMP-ALK
Inhibitor of BMP signaling. Inhibits ALK2, 3 and 6
Chemical name
6-(4-(2-(piperidin-1-yl)ethoxy)phenyl)-3-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidine
Parent CAS No.
[866405-64-3]
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2 mg
€65.00
In Stock | | axonmedchem |