PD 0332991 (hydrochloride)

PD 0332991 is an orally active, selective inhibitor of the cyclin D kinases Cdk4 (IC50 = 11 nM) and Cdk6 (IC50= 16 nM) with no activity against a panel of 36 additional protein kinases. It has been reported to have antiproliferative activity against retinoblastoma-positive tumor cells, blocking retinoblastoma phosphorylation and inducing G1 arrest at nanomolar concentrations. PD 0332991 can inhibit the growth of certain ER-positive or HER2-amplified breast cancer cells (IC50s as low as 4 nM) and demonstrates synergy with tamoxifen (Cay-13258) and trastuzumab, respectively. PD 0332991 inhibition of Cdk4 activity has been used to demonstrate a role for insulin-activated cyclinD1-Cdk4 signaling in the control of glucose metabolism that is independent of cell cycle progression.Formal Name: 6-acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]-pyrido[2,3-d]pyrimidin-7(8H)-one, monohydrochloride. CAS Number: 827022-32-2. Synonyms: Palbociclib. Molecular Formula: C24H29N7O2 . HCl. Formula Weight: 484.0. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: Ethanol: 0.2 mg/ml. lambdamax: 222, 266, 295, 363 nm. SMILES: O=C1N(C2CCCC2)C3=NC(NC4=NC=C(N5CCNCC5)C=C4)=NC=C3C(C)=C1C(C)=O. InChi Code: InChI=1S/C24H29N7O2.ClH/c1-15-19-14-27-24(28-20-8-7-18(13-26-20)30-11-9-25-10-12-30)29-22(19)31(17-5-3-4-6-17)23(33)21(15)16(2)32,/h7-8,13-14,17,25H,3-6,9-12H2,1-2H3,(H,26,27,28,29),1H. InChi Key: STEQOHNDWONVIF-UHFFFAOYSA-N.