产品名称

司美替尼(Selumetinib (AZD6244))

一般描述

Selumetinib is a potent, highly selective MEK inhibitor with potential antineoplastic activity.

别 称

6-(4-bromo-2-chloroanilino)-7-fluoro-N-(2-hydroxyethoxy)-3-methylbenzimidazole-5-carboxamide; ARRY-142886

纯 度

≥98.0%(HPLC)

CAS NO.

606143-52-6

分子式

C¹⁷H¹⁵BrClFN⁴O³

分子量

457.68

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

白色至类白色固体

溶解性(25℃)

DMSO

≥50mg/mL(warmed)

乙醇

Insoluble

水

Insoluble

l  生物学信息

生物活性/药理作用

Selumetinib is an orally active, small molecule with potential antineoplastic activity. Selumetinib is an ATP-independent inhibitor of mitogen-activated protein kinase kinase (MEK or MAPK/ERK kinase) 1 and 2. MEK 1 and 2 are dual specificity kinases that are essential mediators in the activation of the RAS/RAF/MEK/ERK pathway, are often upregulated in various cancer cells, and are drivers of diverse cellular responses, including proliferation. Inhibition of both MEK1 and 2 by selumetinib prevents the activation of MEK1/2 dependent effector proteins and tranion factors, thereby leading to an inhibition of cellular proliferation in various cancers.

Selumetinib (AZD6244) is a potent, highly selective MEK inhibitor with IC50 of 14 nM for MEK1 and Kd value of 530 nM for MEK2. It also inhibits ERK1/2 phosphorylation with IC50 of 10 nM, no inhibition to p38α, MKK6, EGFR, ErbB2, ERK2, B-Raf, etc.

l  存储

存储温度

-20℃

l  注意事项及免责声明

本产品仅用于实验研究，不得作为药物使用，不得用于家用或其它用途。

l  参考文献

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov