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MBM-55S
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
MBM-55S图片
CAS NO:2083624-07-9
包装与价格：
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
MBM-55S 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-55S 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。
生物活性

MBM-55S is a potentNIMA-related kinase 2 (Nek2)inhibitor with anIC50of 1 nM. MBM-55S 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-55S effectively inhibits the proliferation ofcancercells by inducing cell cycle arrest andapoptosis. MBM-55S shows antitumor activities, and no obvious toxicity to mice[1].

IC50& Target

RSK1

5.4 nM (IC50)

DYRK1A

6.5 nM (IC50)

体外研究
(In Vitro)

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

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-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[1]. 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[1].

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 ml/min/kg, respectively.
分子量

734.73

Formula

C36H39FN6O10

CAS 号

2083624-07-9

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.