| 货号 | 11732-5mg |
| 描述 | O6-Methylguanine-DNA methyltransferase (MGMT) (Item No. 11176) is a DNA repair protein which removes an alkyl group from the O6 position on guanine in an autoinactivating reaction.1 Although important in normal DNA repair, this reaction confers resistance to treatments that use O6-alkylating agents to produce cytotoxicity, e.g., in cancer.2,3 Lomeguatrib is a modified quanine base which acts as a pseudosubstrate inactivator of MGMT (IC50 = ~3 nM).2,1 A non-toxic compound, lomeguatrib completely inactivates MGMT in human prostate and colorectal tumors when given as a single 120 mg oral dose and in primary central nervous system cancers at 160 mg.4,5 |
| 别名 | PaTrin 2; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.McMurry, T.B.H. MGMT inhibitors-the Trinity College-Paterson Institute experience, a chemist’s perception. DNA Repair 6(8), 1161-1169 (2007). 2.Clemons, M.,Kelly, J.,Watson, A.J., et al. O6-(4-bromothenyl)guanine reverses temozolomide resistance in human breast tumour MCF-7 cells and xenografts. British Journal of Cancer 93, 1152-1156 (2005). 3.Marchesi, F.,Turriziani, M.,Tortorelli, G., et al. Triazene compounds: Mechanism of action and related DNA repair systems. Pharmacol. Res. 56(4), 275-287 (2007). 4.Ranson, M.,Middleton, M.R.,Bridgewater, J., et al. Lomeguatrib, a potent inhibitor of O6-alkylguanine-DNA-alkyltransferase: Phase I safety, pharmacodynamic, and pharmacokinetic trial and evaluation in combination with temozolomide in patients with advanced solid tumors. Clinical Cancer Research 12, 1577-1584 (2006). 5.Watson, A.J.,Sabharwal, A.,Thorncroft, M., et al. Tumor O6-methylguanine-DNA methyltransferase inactivation by oral lomeguatrib. Clinical Cancer Research 16(2), 743-749 (2010). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 326.2 |
| 分子式 | C10H8BrN5OS |
| CAS号 | 192441-08-0 |
| 稳定性 | ≥ 2 years |
| 本官网所有报价均为常温或者蓝冰运输价格，如有产品需要干冰运输，需另外加收干冰运输费。 |