MBM-55 is a potentNIMA-related kinase 2 (Nek2)inhibitor with anIC₅₀of 1 nM. MBM-55 shows a 20-fold or greater selectivity in most kinases with the exception ofRSK1(IC₅₀=5.4 nM) and DYRK1a (IC₅₀=6.5 nM). MBM-55 effectively inhibits the proliferation ofcancercells by inducing cell cycle arrest andapoptosis. MBM-55 shows antitumor activities, and no obvious toxicity to mice^[1].

IC50: 1 nM (Nek2), 5.4 nM (RSK1), 6.5 nM (DYRK1a), 57 nM (CHK1), 91 nM (GSK-3β), 20 nM (ABL), 370 nM (CDK2), 441nM (CDK4), 608 nM (AKT1), 5300 nM (Aurora A)^[1]

MBM-55 (compound 42g) inhibits MGC-803, HCT-116, Bel-7402 cells proliferation with IC₅₀s of 0.53, 0.84, 7.13 μM, respectively^[1].
MBM-55 (0.5-1 μM; 24 hours) induces G2/M phase arrest and accumulation of cells with >4N content in HCT-116 cells^[1].
MBM-55 (0.5-1 μM; 24 hours) causes cell apoptosis in a concentration-dependent manner in HCT-116 cells^[1].

MBM-55 (20 mg/kg; i.p.; twice a day for 21 days) exhibits good antitumor activity and a well-tolerated dose schedule in nude mice bearing HCT-116 xenografts^[1].
MBM-55 (1.0 mg/kg; i.v.) treatment shows the CL, V_ss, T_1/2, AUC_0-t, and AUC_0-∞values of 33.3 mL/min/kg, 2.53 L/kg, 1.72 hours, 495 ng/h/mL and 507 ng/h/mL, respectively.

498.55

Solid

C₂₈H₂₇FN₆O₂

2083622-09-5

Room temperature in continental US; may vary elsewhere.

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

DMSO : 125 mg/mL(250.73 mM;Need ultrasonic)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。