Powder: -20°C for 3 years
In solvent: -80°C for 2 years
MBM-55S 是一种有效的 Nek2 抑制剂,IC50 为 1 nM。 MBM-55S 抑制细胞周期停滞和凋亡,从而抑制癌细胞的增殖。 MBM-55S 表现出抗肿瘤作用。
产品描述 | MBM-55S is an effective inhibitor of Nek2 with an IC50 of 1 nM. MBM-55S indecus cell cycle arrest and apoptosis thereby inhibiting the proliferation of cancer cells. MBM-55S shows antitumor activities. |
靶点活性 | CDK2:370 nM , GSK-3β:91 nM , Nek2:1 nM , RSK1:5.4 nM , Akt1:608 nM , DYRK1A:6.5 nM , Aurora A:5300 nM , Chk1:57 nM , Abl:20 nM , CDK4:441nM |
体外活性 | 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[1]. |
体内活性 | 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[1]. |
分子量 | 734.73 |
分子式 | C36H39FN6O10 |
CAS No. | 2083624-07-9 |
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
( < 1 mg/ml refers to the product slightly soluble or insoluble )
对于不同动物的给药剂量换算,您也可以参考 更多
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您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
MBM-55S 2083624-07-9 MAPK PI3K/Akt/mTOR signaling S6 Kinase MBM 55S MBM55S Inhibitor inhibitor inhibit