2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
生物活性
Description
In Vivo
In Vitro
化合物的使用
Kinase Assay
Cell Assay
Animal Administration
参考文献
Defactinib is a potent, selective, and orally active FAK inhibitor with demonstrated tolerability and preliminary clinical activity working as a single agent as well as in combination with paclitaxel.Defactinib inhibited FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner. The combination of VS-6063 and paclitaxel markedly decreased proliferation and increased apoptosis, which resulted in 92.7% to 97.9% reductions in tumor weight. RPPA data showed that VS-6063 reduced levels of AKT and YB-1 in taxane-resistant cell lines. FAK inhibition enhanced chemosensitivity in taxane-resistant cells by decreasing YB-1 phosphorylation and subsequently CD44 in an AKT-dependent manner.For the detailed information about the solubility of Defactinib (VS-6063, PF-04554878) in water, the solubility of Defactinib (VS-6063, PF-04554878) in DMSO, the solubility of Defactinib (VS-6063, PF-04554878) in PBS buffer, the animal experiment of Defactinib (VS-6063, PF-04554878) ,the in vivo and in vitro test of Defactinib (VS-6063, PF-04554878) ,the cell experiment of Defactinib (VS-6063, PF-04554878) ,the IC50 and EC50 of Defactinib (VS-6063, PF-04554878) please contact DC Chemicals.
