| 产品名称 | Lomeguatrib - PaTrin 2 |
| 产品货号 | Axon 2223 CAS [192441-08-0] MF C10H8BrN5OSMW 326.17 Purity: 99% Soluble in DMSO Description Potent, orally active inhibitor of O6-methylguanine-DNA-methyltransferase (MGMT; IC50 value 5 nM). Lomeguatrib effectively inactivated MGMT in MCF-7 cells and in xenografts there was complete inactivation of MGMT within 2 h of dosing (20 mg/kg i.p.) and only slight recovery by 24 h.Oral administration of Lomeguatrib substantially increases the haematological toxicity of Dacarbazine, the only approved chemotherapeutic agent for the treatment of metastatic melanoma. In combination with Temozolomide, Lomeguatrib produced a substantial tumour growth delay in MCF-7 xenografts. References Certificates Categories Extra info H.A. Tawbi et al. Inhibition of DNA repair with MGMT pseudosubstrates: phase I study of lomeguatrib in combination with dacarbazine in patients with advanced melanoma and other solid tumours. Br. J. Cancer. 2011, 105, 773-777. M. Clemons et al. O6-(4-bromothenyl)guanine reverses temozolomide resistance in human breast tumour MCF-7 cells and xenografts. Br. J. Cancer. 2005, 93, 1152-1156. M. Turriziani et al. O6-(4-bromothenyl)guanine (PaTrin-2), a novel inhibitor of O6-alkylguanine DNA alkyl-transferase, increases the inhibitory activity of temozolomide against human acute leukaemia cells in vitro. Pharmacol. Res. 2006, 53, 317-323. Certificate of Analysis Material Safety Data Sheet Cell Signaling & Oncology Epigenetics Stem Cell EC 2.1.1.63 DNA methyltransferase Potent, orally active inhibitor of MGMT Chemical name 6-((4-bromothiophen-2-yl)methoxy)-7H-purin-2-amine Parent CAS No. [192441-08-0] Order Size Unit Price Stock 10 mg €135.00 In Stock |
| 产品价格 | 现货询价，电话：010-67529703 |
| 产品规格 | |
| 产品品牌 | axonmedchem |
| 产品概述 | |
| 产品详情 |
Lomeguatrib - PaTrin 2Axon 2223 CAS [192441-08-0] MF C10H8BrN5OS
Description
Potent, orally active inhibitor of O6-methylguanine-DNA-methyltransferase (MGMT; IC50 value 5 nM). Lomeguatrib effectively inactivated MGMT in MCF-7 cells and in xenografts there was complete inactivation of MGMT within 2 h of dosing (20 mg/kg i.p.) and only slight recovery by 24 h.Oral administration of Lomeguatrib substantially increases the haematological toxicity of Dacarbazine, the only approved chemotherapeutic agent for the treatment of metastatic melanoma. In combination with Temozolomide, Lomeguatrib produced a substantial tumour growth delay in MCF-7 xenografts.
Potent, orally active inhibitor of MGMT
Chemical name6-((4-bromothiophen-2-yl)methoxy)-7H-purin-2-amine Parent CAS No.[192441-08-0] |
| 产品资料 |
