产品名称

MK-1775

一般描述

MK-1775 is a potent and selective Wee1 inhibitor.

别 称

AZD1775

纯 度

≥98%(HPLC)

CAS NO.

955365-80-7

分子式

C²⁷H³²N⁸O²

分子量

500.607

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

浅黄色或浅黄绿固体

溶解性(25℃)

DMSO

≥50mg/mL

乙醇

~10mg/mL

水

Insoluble

l  生物学信息

生物活性/药理作用

Adavosertib is a small molecule inhibitor of the tyrosine kinase WEE1 with potential antineoplastic sensitizing activity. Adavosertib selectively targets and inhibits WEE1, a tyrosine  kinase that phosphorylates cyclin-dependent kinase 1 (CDK1, CDC2) to inactivate the CDC2/cyclin B complex. Inhibition of WEE1 activity prevents  the phosphorylation of CDC2 and impairs the G2 DNA damage checkpoint. This may lead to apoptosis upon treatment with DNA damaging chemotherapeutic agents. Unlike normal cells, most p53 deficient or mutated human cancers lack the G1 checkpoint as p53 is the key regulator of the G1 checkpoint and these cells rely on the G2 checkpoint for DNA repair to damaged cells. Annulment of the G2 checkpoint may therefore make p53 deficient tumor cells more vulnerable to antineoplastic agents and enhance their cytotoxic effect.

l  包装与存储

包 装

10mg; 50mg; 250mg

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