SGX-523
编号: 16070912
Cas号: 1022150-57-7
纯度: 98% by HPLC
SGX523 is a novel, ATP-competitive kinase inhibitor remarkable for its exquisite selectivity for MET. SGX523 potently inhibited MET with an IC50 of 4 nmol/L and is >1,000-fold selective versus the >200-fold selectivity of other protein kinases tested in biochemical assays. Crystallographic study revealed that SGX523 stabilizes MET in a unique inactive conformation that is inaccessible to other protein kinases, suggesting an explanation for the selectivity. SGX523 inhibited MET-mediated signaling, cell proliferation, and cell migration at nanomolar concentrations but had no effect on signaling dependent on other protein kinases, including the closely related RON, even at micromolar concentrations. SGX523 inhibition of MET in vivo was associated with the dose-dependent inhibition of growth of tumor xenografts derived from human glioblastoma and lung and gastric cancers, confirming the dependence of these tumors on MET catalytic activity. Our results show that SGX523 is the most selective inhibitor of MET catalytic activity described to date and is thus a useful tool to investigate the role of MET kinase in cancer without the confounding effects of promiscuous protein kinase inhibition.
仅供研究使用。 我们不向患者出售。
化学信息
| 名称 | SGX-523 |
|---|---|
| Iupac 化学名称 | 6-((6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)thio)quinoline |
| 同义词 | SGX523; SGX-523 |
| 英文同义词 | SGX523; SGX-523 |
| 分子式 | C18H13N7S |
| 分子量 | 359.41 |
| Smile | CN1N=CC(=C1)C=1C=CC=2N(N1)C(=NN2)SC=2C=C1C=CC=NC1=CC2 |
| InChiKey | BCZUAADEACICHN-UHFFFAOYSA-N |
| InChi | InChI=1S/C18H13N7S/c1-24-11-13(10-20-24)16-6-7-17-21-22-18(25(17)23-16)26-14-4-5-15-12(9-14)3-2-8-19-15/h2-11H,1H3 |
| Cas号 | 1022150-57-7 |
| 相关CAS号 |
订购信息
| 包装 | 价格 | 库存 | 纯度 | 备货期 |
|---|---|---|---|---|
| 大货 | 询价 | 询价 | 询价 |
