产品名称

Volasertib (BI 6727)

一般描述

Volasertib is a dihydropteridinone Polo-like kinase 1 (Plk1) inhibitor with potential antineoplastic activity.

别 称

N-[4-[4-(cyclopropylmethyl)piperazin-1-yl]cyclohexyl]-4-[[(7R)-7-ethyl-5-methyl-6-oxo-8-propan-2-yl-7H-pteridin-2-yl]amino]-3-methoxybenzamide

纯 度

≥98.0%(HPLC)

CAS NO.

755038-65-4

分子式

C³⁴H⁵⁰N⁸O³

分子量

618.81

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

≥15mg/mL(warmed)

乙醇

Insoluble

水

Insoluble

l  生物学信息

生物活性/药理作用

Volasertib is a dihydropteridinone Polo-like kinase 1 (Plk1) inhibitor with potential antineoplastic activity.  Volasertib selectively inhibits Plk1, inducing selective G2/M arrest followed by apoptosis in a variety of tumor cells while causing reversible cell arrest at the G1 and G2 stage without apoptosis in normal cells. Plk1, named after the polo gene of Drosophila melanogaster, is a serine/threonine protein kinase involved in regulating mitotic spindle function in a non-ATP competitive manner. Volasertib is a highly potent Plk1 inhibitor with IC50 of 0.87 nM in a cell-free assay. It shows 6- and 65-fold greater selectivity against Plk2 and Plk3.

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