C-Met inhibitor, potent and selective
CAS：1025720-94-8
分子式：C25H19ClF2N4O4
分子量：512.89
纯度：98%
存储：Store at -20°C

Background:

BMS 777607 is a novel, selective and orally available ATP-competitive MET kinase inhibitor that primarily targets several MET family members, including RON, MET, Tyro-3 and AxI, with half maximal inhibitory concentration IC50 of 1.8 nmol/L, 3.9 nmol/L, 4.3 nmol/L and 1.1 nmol/L respectively. Moreover, at higher concentrations, BMS 777607 has been found to inhibit other protein tyrosine kinases, including Mer, Flt-3, Aurora B, Lck and VEGFR2 with IC50 of 14 nmol/L, 16 nmol/L, 78 nmol/L, 120 nmol/L and 180 nmol/L respectively. In previous studies, BMS 777607 potently inhibited the auto-phosphorylation of c-MET (IC50: 20 nmol/L) leading to impaired xenograft growth.

参考文献:
[1]Dai Y, Siemann DW. BMS-777607, a small-molecule met kinase inhibitor, suppresses hepatocyte growth factor-stimulated prostate cancer metastatic phenotype in vitro. Mol Cancer Ther. 2010 Jun;9(6):1554-61. doi: 10.1158/1535-7163.MCT-10-0359. Epub 2010 Jun 1.
[2]Sharma S, Zeng JY, Zhuang CM, Zhou YQ, Yao HP, Hu X, Zhang R, Wang MH.

Small-molecule inhibitor BMS-777607 induces breast cancer cell polyploidy with increased resistance to cytotoxic chemotherapy agents. Mol Cancer Ther. 2013 May;12(5):725-36. doi: 10.1158/1535-7163.MCT-12-1079. Epub 2013 Mar 6.