MBM-55

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

MBM-55 

MBM-55 是有效的 NIMA-related kinase 2 (Nek2) 抑制剂，IC50 值为 1 nM，是其他激酶选择性的 20 倍甚至更高，除了 RSK1 (IC50=5.4 nM) 和 DYRK1a (IC50=6.5 nM)。MBM-55 通过诱导细胞周期停滞和凋亡 (apoptosis) 抑制癌细胞的增殖。具有抗肿瘤活性，且对小鼠没有明显的毒性。

MBM-55

MBM-55 Chemical Structure

CAS No. : 2083622-09-5

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生物活性

MBM-55 is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 1 nM. MBM-55 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-55 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[1].

IC50 & Target

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]
体外研究
(In Vitro)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[1]

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[1]

Cell Line: HCT-116 cells
Concentration: 0.5, 1 μM
Incubation Time: 24 hours
Result: Caused cell apoptosis in a concentration-dependent manner.

体内研究
(In Vivo)

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, 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.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female BALB/c nu/nu mice (5-6 weeks, bearing HCT-116 xenografts)[1]
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[1]
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 ng/h/mL, respectively.

分子量

498.55

Formula

C28H27FN6O2
CAS 号

2083622-09-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Xi JB, et al. Structure-based design and synthesis of imidazo[1,2-a]pyridine derivatives as novel and potent Nek2 inhibitors with in vitro and in vivo antitumor activities. Eur J Med Chem. 2017 Jan 27;126:1083-1106.

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