中文同义词:
帕博西尼-D8;[2H8]-PALBOCICLIB;[2H8]-帕博西尼;帕博西尼杂质115
英文同义词:
Palbociclib-d8;PD 0332991-d8;[2H8]-Palbociclib;6-acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl-2,2,3,3,5,5,6,6-d8)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one
生物活性
Palbociclib D8 (PD 0332991 D8) 是 Palbociclib 的氘代物。Palbociclib 是一种选择性的口服活性的 CDK4 和 CDK6 抑制剂,IC50 分别为 11 nM 和 16 nM。Palbociclib 有潜力用于 ER 阳性和 HER2 阴性乳腺癌的研究。
靶点
Cdk4/cyclin D3
9 nM (IC 50 )
Cdk4/cyclin D1
11 nM (IC 50 )
Cdk6/cyclin D2
16 nM (IC 50 )
DYRK1A
2000 nM (IC 50 )
MAPK
8000 nM (IC 50 )
Cdk4/cyclin D3
9 nM (IC 50 )
Cdk4/cyclin D1
11 nM (IC 50 )