| 货号 | 18093-1mg |
| 描述 | The hepatocyte growth factor receptor c-Met commonly shows elevated activity in several forms of cancer.1,2 SGX523 is a potent, selective, ATP-competitive inhibitor that blocks the tyrosine kinase activity of c-Met with an IC50 value of 4 nM.1 It is over 1,000-fold selective for c-Met over a panel of other kinases.1 SGX523 is orally active and dose-dependently inhibits the growth of a variety of tumor xenografts in mice.1,3 The effectiveness of SGX523 is enhanced when combined with other chemotherapeutic compounds, including inhibitors of EGFR.2,4 SGX523 is metabolized, at least in part, by aldehyde oxidase, an enzyme that differs in activity across different species.5 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Buchanan, S.G.,Hendle, J.,Lee, P.S., et al. SGX523 is an exquisitely selective, ATP-competitive inhibitor of the MET receptor tyrosine kinase with antitumor activity in vivo. Molecular Cancer Therapeutics 8(12), 3181-3190 (2009). 2.Padda, S.,Neal, J.W., and Wakelee, H.A. MET inhibitors in combination with other therapies in non-small cell lung cancer. Transl.Lung Cancer Res. 1(4), 238-253 (2012). 3.Guessous, F.,Zhang, Y.,diPierro, C., et al. An orally bioavailable c-Met kinase inhibitor potently inhibits brain tumor malignancy and growth. Anticancer Agents Med.Chem. 10(1), 28-35 (2010). 4.Zhang, Y.W.,Staal, B.,Essenburg, C., et al. Strengthening context-dependent anticancer effects on non-small cell lung carcinoma by inhibition of both MET and EGFR. Molecular Cancer Therapeutics 12(8), 1429-1441 (2013). 5.Diamond, S.,Boer, J.,Maduskuie, T.P., Jr., et al. Species-specific metabolism of SGX523 by aldehyde oxidase and the toxicological implications. Drug Metabolism and Disposition 38(8), 1277-1285 (2010). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 359.4 |
| 分子式 | C18H13N7S |
| CAS号 | 1022150-57-7 |
| 稳定性 | ≥ 2 years |
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