产品名称

Entospletinib (GS-9973)

一般描述

Entospletinib (GS-9973) is an orally bioavailable, selective Syk inhibitor.

别 称

6-(1H-indazol-6-yl)-N-(4-morpholin-4-ylphenyl)imidazo[1,2-a]pyrazin-8-amine

纯 度

≥98.0%(HPLC)

CAS NO.

1229208-44-9

分子式

C²³H²¹N⁷O

分子量

411.46

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℃)

DMSO

≥25mg/mL(warmed)

乙醇

Insoluble

水

Insoluble

l  生物学信息

生物活性/药理作用

Entospletinib is an orally available inhibitor of spleen tyrosine kinase (Syk), with potential antineoplastic activity. Upon oral administration of entospletinib, this agent may inhibit the activity of Syk, which inhibits B-cell receptor (BCR) signaling and leads to an inhibition of tumor cell activation, migration, adhesion and proliferation. Syk, a non-receptor cytoplasmic, BCR-associated tyrosine kinase, is expressed in hematopoietic tissues and is often overexpressed in hematopoeitic malignancies.

Entospletinib (GS-9973) is an orally bioavailable, selective Syk inhibitor with IC50 of 7.7 nM in a cell-free assay and showed 13- to >1000-fold cellular selectivity for Syk over other kinases(including Jak2, ckit, Flt3, Ret, KDR) as assessed by target protein phosphorylation or functional response.

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