CAS NO: | 877399-52-5 |
规格: | 98% |
分子量: | 450.34 |
包装 | 价格(元) |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
Background:
Crizotinib is a potent, ATP-competitive, small-molecule and orally available inhibitor of c-Met kinase with a Ki value?of 4 nmol/L[1].
Crizotinib has shown to inhibit?wild-type c-Met phosphorylation with a mean IC50 value of 11 nmol/L in multiple human endothelial and carcinoma cell lines. Crizotinib has been demonstrated to inhibit cell growth and induce apoptosis in?human GTL-16 gastric carcinoma cells. Additionally, crizotinib could inhibit cell migration and invasion induced by HGF in human NCI-H441 lung cancer cells. Moreover, crizotinib has revealed to block cell scattering of MDCK [1].
Crizotinib has been indicated to suppress tumor growth in GTL-16, NCI-H441 NSCLC, Caki-1 RCC, U87MG glioblastoma or PC-3 prostate tumor xenograft mice [1].
参考文献:
[1] Zou HY1,?Li Q,?Lee JH,?Arango ME,?McDonnell SR,?Yamazaki S,?Koudriakova TB,?Alton G,?Cui JJ,?Kung PP,?Nambu MD,?Los G,?Bender SL,Mroczkowski B,?Christensen JG. An orally available small-molecule inhibitor of c-Met, PF-2341066, exhibits cytoreductive antitumor efficacy through antiproliferative and antiangiogenic mechanisms. Cancer Res.?2007 May 1;67(9):4408-17.