MBM-55S

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

MBM-55S 通过诱导细胞周期停滞和细胞凋亡来有效抑制癌细胞的增殖。 MBM-55S具有抗肿瘤活性，且对小鼠无明显毒性。

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. 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).(In Vitro):MBM-55S shows a 20-fold or greater selectivity in most kinases with the exception of RSK1 and DYRK1a with IC50s of 5.4 and 6.5 nM. MBM-55S inhibits MGC-803, HCT-116, and Bel-7402 the proliferation of cell with IC50s of 0.53, 0.84, and 7.13 μM, respectively. MBM-55S (0.5-1 μM) induces G2/M phase arrest and accumulation of cells with >4N content and causes cell apoptosis in a concentration-dependent manner in HCT-116 cells.(In Vivo):In female BALB/c nu/nu mice, MBM-55S (20 mg/kg; i.p) exhibits good antitumor activity. In male Sprague Dawley rats, MBM-55S (1.0 mg/kg; i.v.) shows good pharmacokinetic profile with the CL, T1/2, Vss, AUC0-t, and AUC0-∞ values of 33.3 mL/min/kg, 1.72 hours, 2.53 L/kg, 495 ng/h/mL and 507 ng/h/mL, respectively.

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.Cell Cycle Analysis Cell Line:HCT-116 cells Concentration:0.5, 1 μM Incubation Time:24 hours Result:Induced G2/M phase arrest and accumulation of cells with >4N content.Apoptosis Analysis Cell Line:HCT-116 cells Concentration:0.5, 1 μM Incubation Time:24 hours Result:Caused cell apoptosis in a concentration-dependent manner.

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.

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PI3K/Akt/mTOR signaling

S6 Kinase

Bcr-Abl

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2083624-07-9

734.738

C36H39FN6O10

>98% (HPLC)

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OC(=O)CCC(O)=O.OC(=O)CCC(O)=O.CN(C)CCn1cc(cn1)-c1ccn2c(cnc2c1)-c1ccc(C(N)=O)c(OCc2cccc(F)c2)c1

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(-20℃)

With Ice Pack

≥ 2 years