Afuresertib hydrochloride 是一个口服有效的,ATP 竞争性的选择性泛Akt抑制剂,作用于Akt1、Akt2和Akt3,Ki值分别为 0.08、2和 2.6 nM。
产品描述
Afuresertib hydrochloride is an inhibitor of Akt kinase (Kis of 0.08/2/2.6 nM for Akt1/Akt2/Akt3 respectively)
体外活性
Afuresertib-induced p21 expression promotes G1 phase arrest by inducing FOXO activity.?Furthermore, afuresertib significantly enhanced cisplatin-induced cytotoxicity.Afuresertib modulated the expression E2F1 and MYC, which are associated with fibroblast core serum response.?Suggest that afuresertib is a useful anticancer drug for treating patients with MPM[1].
细胞实验
Cell confluence proliferation assay was performed using Incucyte ZOOM Live‐Cell Imaging System.?Briefly, ACC‐MESO‐4 and MSTO‐211H cells were seeded in 12‐well plates (cell density, 1 × 104 cells/well) and were incubated for 24 h at 37°C.?Then, the cells were incubated with 0, 2, 5, or 10 μmol/L afuresertib.?During treatment, cell growth was monitored by recording phase images using the IncuCyte ZOOM Live‐Cell Imaging System (magnification, ×100)[1].
Cas No.
1047645-82-8
分子式
C18H18Cl3FN4OS
分子量
463.78
储存和溶解度
DMSO:100 mg/mL (215.62 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years