产品名称

Linsitinib (OSI-906)

一般描述

Linsitinib is an orally bioavailable small molecule inhibitor of the insulin-like growth factor 1 receptor (IGF-1R) with potential antineoplastic activity.

别 称

3-[8-amino-1-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl]-1-methylcyclobutan-1-ol

纯 度

≥98.0%(HPLC)

CAS NO.

867160-71-2

分子式

C²⁶H²³N⁵O

分子量

421.49

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

≥50mg/mL

乙醇

Insoluble

水

Insoluble

l  生物学信息

生物活性/药理作用

Linsitinib is an orally bioavailable small molecule inhibitor of the insulin-like growth factor 1 receptor (IGF-1R) with potential antineoplastic activity. Linsitinib selectively inhibits IGF-1R, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. Overexpressed in a variety of human cancers, IGF-1R stimulates cell proliferation, enables oncogenic transformation, and suppresses apoptosis.

Linsitinib (OSI-906) is a selective inhibitor of IGF-1R with IC50 of 35 nM in cell-free assays; modestly potent to InsR with IC50 of 75 nM, and no activity towards Abl, ALK, BTK, EGFR, FGFR1/2, PKA 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