产品
编 号：F621000
分子式：C36H39FN6O10
分子量：734.73
分子式：C36H39FN6O10
分子量：734.73
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CAS No: 2083624-07-9
产品详情
生物活性：
MBM-55S is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 1 nM. MBM-55S shows a 20-fold or greater selectivity in most kinases with the exception of RSK1 (IC50=5.4 nM) and DYRK1a (IC50=6.5 nM). MBM-55S effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55S shows antitumor activities, and no obvious toxicity to mice.
体内研究：
MBM-55S (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.MBM-55S (1.0 mg/kg; i.v.) treatment 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.Animal Model:Female BALB/c nu/nu mice (5-6 weeks, bearing HCT-116 xenografts)
Dosage:20 mg/kg
Administration:Intraperitoneal injection; twice a day for 21 days
Result:Significantly suppressed tumor growth.
Animal Model:Male Sprague Dawley (SD) rats
Dosage:1.0 mg/kg
Administration:IV injection (Pharmacokinetic Analysis)
Result:The CL, Vss, T1/2, AUC0-t, and AUC0-∞ values were 33.3 mL/min/kg, 2.53 L/kg, 1.72 hours, 495 ng/h/mL and 507 ml/min/kg, respectively.
体外研究：
MBM-55S inhibits MGC-803, HCT-116, Bel-7402 cells proliferation with IC50s of 0.53, 0.84, 7.13 μM, respectively.MBM-55S (0.5-1 μM; 24 hours) induces G2/M phase arrest and accumulation of cells with >4N content in HCT-116 cells.MBM-55S (0.5-1 μM; 24 hours) causes cell apoptosis in a concentration-dependent manner in HCT-116 cells.
MBM-55S is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 1 nM. MBM-55S shows a 20-fold or greater selectivity in most kinases with the exception of RSK1 (IC50=5.4 nM) and DYRK1a (IC50=6.5 nM). MBM-55S effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55S shows antitumor activities, and no obvious toxicity to mice.
体内研究：
MBM-55S (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.MBM-55S (1.0 mg/kg; i.v.) treatment 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.Animal Model:Female BALB/c nu/nu mice (5-6 weeks, bearing HCT-116 xenografts)
Dosage:20 mg/kg
Administration:Intraperitoneal injection; twice a day for 21 days
Result:Significantly suppressed tumor growth.
Animal Model:Male Sprague Dawley (SD) rats
Dosage:1.0 mg/kg
Administration:IV injection (Pharmacokinetic Analysis)
Result:The CL, Vss, T1/2, AUC0-t, and AUC0-∞ values were 33.3 mL/min/kg, 2.53 L/kg, 1.72 hours, 495 ng/h/mL and 507 ml/min/kg, respectively.
体外研究：
MBM-55S inhibits MGC-803, HCT-116, Bel-7402 cells proliferation with IC50s of 0.53, 0.84, 7.13 μM, respectively.MBM-55S (0.5-1 μM; 24 hours) induces G2/M phase arrest and accumulation of cells with >4N content in HCT-116 cells.MBM-55S (0.5-1 μM; 24 hours) causes cell apoptosis in a concentration-dependent manner in HCT-116 cells.
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