SGX-523,1022150-57-7

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YZ剂描述：

产品名称：SGX-523

产品别名：SGX523

英文别名：SGX523

靶点：c-Met

CAS：1022150-57-7

纯度：>98%

外观：见爱必信官网

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

SGX-523是一种选择性的MetYZ剂，IC50为4 nM，对BRAFV599E， c-Raf， Abl和p38α无YZ活性。SGX-523属于c-Met/肝细胞生长因子受体 (HGFR) 酪氨酸激酶YZ剂，使MET处于失活状态而不能接近其他蛋白激酶。SGX523有效YZ纯化的MET催化区，而不是紧密相关的受体酪氨酸激酶RON。SGX523是ATP竞争性YZ剂，作用于低活性和非磷酸化的MET时亲和力更高（MET-KD(0P), K_i = 2.7 nM）。

溶解性：DMSO ：3 mg/mL (8.35 mM)

体外研究：

SGX-523 belongs to the class of c-Met/hepatocyte growth factor receptor (HGFR) tyrosine kinase inhibitors. SGX-523 stabilizes MET in a unique inactive conformation that is inaccessible to other protein kinases, suggesting an explanation for its selectivity. SGX523 potently inhibits the purified MET catalytic domain but not the closely related receptor tyrosine kinase RON. SGX523 indicates ATP-competitive inhibition with higher apparent affinity for the less active, unphosphorylated form of MET versus the more active phospho-enzyme , a phenomenon consistent with preferential binding to an inactive enzyme conformation. SGX523 inhibits 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.

体内研究：SGX523 significantly retards the growth of preestablished GTL16 tumors when administered orally at doses of ≥10 mg/kg twice daily. SGX523 potently inhibits U87MG tumor growth; at 30 mg/kg dosed twice daily, SGX523 leads to clear regression of U87MG tumors. SGX523, dosed twice daily at 30 mg/kg, also retards the growth of H441 tumors with concomitant reduction in tumor MET autophosphorylation levels. SGX523 inhibition of MET in vivo is associated with the dose-dependent inhibition of growth of tumor xenografts derived from human glioblastoma, lung and gastric cancers, confirming the dependence of these tumors on MET catalytic activity.

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