MBM-55 是一种有效的中心体相关激酶 2 (NEK2) 抑制剂,IC50 为 1 nM。 MBM-55 通过诱导细胞周期停滞和凋亡有效抑制癌细胞的增殖。
产品描述
MBM-55 is an effective inhibitor of NIMA related kinase 2 (NEK2) with an IC50 of 1 nM. MBM-55 effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis.
体外活性
MBM-55 (0.5-1 μM; 24 hours) induces G2/M phase arrest and accumulation of cells with >4N content in HCT-116 cells. MBM-55 (0.5-1 μM; 24 hours) causes cell apoptosis in a concentration-dependent manner in HCT-116 cells.MBM-55 inhibits MGC-803, HCT-116, Bel-7402 cells proliferation with IC50s of 0.53, 0.84, 7.13 μM, respectively[1].
体内活性
In female BALB/c nu/nu mice bearing HCT-116 xenografts, MBM-55 (20 mg/kg; i.p.) exhibits good antitumor activity and a well-tolerated dose schedule. MBM-55 (1.0 mg/kg; i.v.) shows the CL, Vss, T1/2, AUC0-t, and AUC0-∞ values of 33.3 mL/min/kg, 2.53 L/kg, 1.72 hours, 495 ng/h/mL and 507 ng/h/mL, respectively[1].
Cas No.
2083622-09-5
分子式
C28H27FN6O2
分子量
498.55
储存和溶解度
DMSO:120 mg/mL (240.70 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years