产品描述
MBM-17S effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-17S shows antitumor activities, and no obvious toxicity to mice.MBM-17S is a potent NIMA-related kinase 2 (Nek2) inhibitor, with an IC50 of 3 nM.
体外活性
MBM-17S (0.25-1.0 μM; 24 hours) induced G2/M phase arrest and accumulation of cells with >4N content. MBM-17S (0.5-1.0 μM; 24 hours) triggers apoptosis of cancer cells.MBM-17S inhibits MGC-803, HCT-116, and Bel-7402 cells proliferation with IC50s of 0.48, 1.06, and 4.53 μM, respectively.
体内活性
MBM-17S (1.0 mg/kg; i.v.) treatment shows CL, Vss, T1/2, AUC0-t, and AUC0-∞ values of 42.4 mL/min/kg, 4.06 L/kg, 2.42 hours, 386 ng/h/mL, and 405 ng/h/mL, respectively.MBM-17S (20 mg/kg; i.p.; twice a day for 21 days) exhibits good antitumor activity and a well-tolerated dose schedule.
Cas No.
2083621-91-2
分子式
C36H40N6O10
分子量
716.74
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years