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编 号：F640590
分子式：C28H28N6O2
分子量：480.56
分子式：C28H28N6O2
分子量：480.56
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CAS No: 2083621-90-1
产品详情
生物活性：
MBM-17 is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 3 nM. It effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55 shows antitumor activities, and no obvious toxicity to mice.
体内研究：
MBM-17 (20 mg/kg; i.p.; twice a day for 21 days) exhibits good antitumor activity and a well-tolerated dose schedule.MBM-17 (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.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:Tmor growth was significantly suppressed.
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 of 42.4 mL/min/kg, 4.06 L/kg, 2.42 hours, 386 ng/h/mL, and 405 ng/h/mL, respectively.
体外研究：
MBM-17 (compound 42c) inhibits MGC-803, HCT-116, Bel-7402 cells proliferation with IC50s of 0.48, 1.06, 4.53 μM, respectively.MBM-17 (0.25-1.0 μM; 24 hours) induced G2/M phase arrest and accumulation of cells with >4N content.MBM-17 (0.5-1.0 μM; 24 hours) triggers apoptosis of cancer cells.
MBM-17 is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 3 nM. It effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55 shows antitumor activities, and no obvious toxicity to mice.
体内研究：
MBM-17 (20 mg/kg; i.p.; twice a day for 21 days) exhibits good antitumor activity and a well-tolerated dose schedule.MBM-17 (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.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:Tmor growth was significantly suppressed.
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 of 42.4 mL/min/kg, 4.06 L/kg, 2.42 hours, 386 ng/h/mL, and 405 ng/h/mL, respectively.
体外研究：
MBM-17 (compound 42c) inhibits MGC-803, HCT-116, Bel-7402 cells proliferation with IC50s of 0.48, 1.06, 4.53 μM, respectively.MBM-17 (0.25-1.0 μM; 24 hours) induced G2/M phase arrest and accumulation of cells with >4N content.MBM-17 (0.5-1.0 μM; 24 hours) triggers apoptosis of cancer cells.
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