产品名称

帕布昔利布(Palbociclib)

一般描述

Palbociclib(帕布昔利布) is an orally available highly selective inhibitor of CDK4/6 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;  PD0332991;帕博西尼;PD-0332991;  Ibrance; PD 0332991

纯 度

≥98%(HPLC)

CAS NO.

571190-30-2

分子式

C²⁴H²⁹N⁷O²

分子量

447.543

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

黄色固体

溶解性(25℃)

DMSO

≥10mg/mL

乙醇

N/A

水

N/A

l  生物学信息

生物活性/药理作用

Treatment of breast cancer cell lines with the combination of palbociclib and antiestrogens leads to decreased retinoblastoma protein (Rb) phosphorylation resulting in reduced E2F and signaling and increased growth arrest compared to treatment  with each drug alone. In vitro treatment of ER-positive breast cancer cell lines with the combination of palbociclib and antiestrogens leads to  increased cell senescence, which was sustained for up to 6 days following drug removal. In vivo studies using a patient-derived ER-positive breast cancer xenograft model demonstrated that the combination of palbociclib and letrozole increased the inhibition of Rb phosphorylation, downstream signaling and tumor growth compared to each drug alone.

Palbociclib is an orally available cyclin-dependent kinase (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.

l  包装与存储

包 装

10mg; 50mg

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