产品名称

博舒替尼(Bosutinib (SKI-606))

一般描述

Bosutinib(博舒替尼) is a novel, dual Src/Abl inhibitor.

别 称

4-(2,4-dichloro-5-methoxyanilino)-6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinoline-3-carbonitrile; WAY-173606

纯 度

≥99.0%(HPLC)

CAS NO.

380843-75-4

分子式

C²⁶H²⁹Cl²N⁵O³

分子量

530.45

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

类白色或米白色粉末

溶解性(25℃)

DMSO

≥50mg/mL

乙醇

Slightly soluble

水

Insoluble

l  生物学信息

生物活性/药理作用

Bosutinib is a synthetic quinolone derivative and dual kinase inhibitor that targets both Abl and Src kinases with potential antineoplastic activity. Unlike imatinib, bosutinib inhibits the autophosphorylation of both Abl and Src kinases, resulting in inhibition of cell growth and apoptosis. Because of the dual mechanism of action, this agent may have activity in resistant CML disease, other myeloid malignancies and solid tumors. Abl kinase is upregulated in the presence of the abnormal Bcr-abl fusion protein which is commonly associated with chronic myeloid leukemia (CML). Over of specific Src kinases is also associated with the imatinib-resistant CML phenotype.

Bosutinib (SKI-606) is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM in cell-free assays, respectively.

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