产品名称

羟乙基磺酸帕博西丽(Palbociclib Isethionate)

一般描述

Palbociclib Isethionate is the isethionate salt form of palbociclib, an orally available CDK inhibitor with potential antineoplastic activity.

别 称

6-acetyl-8-cyclopentyl-5-methyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrido[2,3-d]pyrimidin-7-one;2-hydroxyethanesulfonic acid; PD0332991 Isethionate

纯 度

≥98.0%(HPLC)

CAS NO.

827022-33-3

分子式

C²⁴H²⁹N⁷O²·C²H⁶O⁴S

分子量

573.66

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

Insoluble

乙醇

Insoluble

水

≥5mg/mL(warmed)

l  生物学信息

生物活性/药理作用

Palbociclib Isethionate is the isethionate salt form of palbociclib, an orally available CDK inhibitor with potential antineoplastic activity. Palbociclib selectively inhibits cyclin-dependent kinase 4 (CDK4) and 6 (CDK6), thereby inhibiting retinoblastoma (Rb) protein phosphorylation early in the G1 phase leading to cell cycle arrest. This suppresses DNA replication and decreases tumor cell proliferation. CDK4 and 6 are serine/threonine kinases that are upregulated in many tumor cell types and play a key role in the regulation of cell cycle progression. Palbociclib Isethionate is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, 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