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MBM-55
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-55图片
CAS NO:2083622-09-5
包装与价格：
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
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。
生物活性

MBM-55 is a potentNIMA-related kinase 2 (Nek2)inhibitor with anIC50of 1 nM. MBM-55 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-55 effectively inhibits the proliferation ofcancercells by inducing cell cycle arrest andapoptosis. 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].

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.

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

性状

Solid

Formula

C28H27FN6O2

CAS 号

2083622-09-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : 125 mg/mL(250.73 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.0058 mL10.0291 mL20.0582 mL
5 mM0.4012 mL2.0058 mL4.0116 mL
10 mM0.2006 mL1.0029 mL2.0058 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。