CAS NO: | 939791-41-0 |
包装 | 价格(元) |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
生物活性 | PF-562271 (VS-6062) hydrochloride is a potent, ATP-competitive and reversibleFAKandPyk2kinase inhibitor withIC50s of 1.5 nM and 13 nM, respectively[1]. |
IC50& Target | IC50: 1.5 nM (FAK), 13 nM (Pyk2), 30 nM (CDK2), 47 nM (CDK3), 58 nM (CDK1), 97 nM (CDK7), 97 nM (Flt3)[1] |
体外研究 (In Vitro) | PF-562271 (VS-6062) hydrochloride is shown to be a 30- to 120-nM inhibitor of CDK2/E, CDK5/p35, CDK1/B, and CDK3/E in recombinant enzyme assays, in cell-based assays evaluating the role of CDKs, a 48-hour exposure of 3.3 μM PF-562271 is required to alter cell cycle progression. PF-562271 is potent in an inducible cell-based assay measuring phospho-FAK with a IC50of 5 nM[1]. |
体内研究 (In Vivo) | PF-562271 inhibits FAK phosphorylation in vivo in a dose-dependent fashion (calculated EC50of 93 ng/mL, total) after p.o. administration to tumor-bearing mice[1]. Rats that receive PF-562271 demonstrate a decrease in tumor growth after 2 weeks of treatment with signs of bone healing as evidenced by the deposition of new bone (cortical and cancellous) at sites previously damaged by the tumor[3]. |
分子量 | 543.95 |
Formula | C21H21ClF3N7O3S |
CAS 号 | 939791-41-0 |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |