Cat No.
CEI-0296
Description
PD 0332991 can potently inhibit CDK4 and CDK6 with IC50 of 11 nM and 16 nM.
CAS No.
827022-32-2
Targets
CDK4, CDK6
Chemical Name
6-acetyl-8-cyclopentyl-5-methyl-2-(5-(piperazin-1-yl)pyridin-2-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one hydrochloride
M.Wt
483.99
Purity
>99%
Solubility
DMSO 3 mg/mL Water 30 mg/mL Ethanol
Storage
2 years at -20centigrade Powder
In vitro
As a highly selective CDK inhibitor, PD 0332991 can potently inhibit CDK4 and CDK6 with IC50 of 11 nM and 16 nM, but shows no activity against other kinases. PD0332991 was able to prevent upregulation of cyclin D1 and CDK6 as well as CDK4 and phosphorylated pRb and this correlated with a more profound reversal of hyperplasia and dysplasia.
In vivo
Inhibition of Cdk4/6 by PD 0332991 in 5T33MM cells could suppress tumor progression and prolong survival, mice were inoculated with 5* 105 5T33MM cells and treated for 2 weeks with 150 mg/kg PD 0332991 daily by gavage after the onset of disease ( day 7). PD 0332991 treatment led to a significant increase in survival, to a mean of 35 days in the PD 0332991-treated mice compared with 25 days in vehicle-treated mice.
