产品名称

Enasidenib

一般描述

Enasidenib is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzyme with IC50 of 12 nM.

别 称

CC-90007 Free Base, AG-221

纯 度

≥98.5%(HPLC)

CAS NO.

1446502-11-9

分子式

C¹⁹H¹⁷F⁶N⁷O

分子量

473.38

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

固体

溶解性(25°C)

DMSO

≥50mg/ml

乙醇

≥50mg/ml

水

Very slightly soluble

l  生物学信息

生物活性/药理作用

Enasidenib is an orally available inhibitor of specific mutant forms of the mitochondrial enzyme isocitrate dehydrogenase type 2 (IDH2), with potential antineoplastic activity. Upon administration, enasidenib specifically inhibits various mutant forms of IDH2, including the IDH2 variants R140Q, R172S, and R172K, which inhibits the formation of 2-hydroxyglutarate (2HG). This may lead to both an induction of cellular differentiation and an inhibition of cellular proliferation in IDH2-expressing tumor cells. IDH2, an enzyme in the citric acid cycle, is mutated in a variety of cancers; it initiates and drives cancer growth by blocking differentiation and the production of the oncometabolite 2HG.

l  存储

存储温度

-20°C

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