PD 0332991-d8

PD 0332991-d8 is intended for use as an internal standard for the quantification of PD 0332991 (Cay-16273) by GC- or LC-MS. 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 cyclin D1-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-2,2,3,3,5,5,6,6-d8)-2-pyridinyl]amino]-pyrido[2,3-d]pyrimidin-7(8H)-one. CAS Number: 1628752-83-9. Synonyms: Palbociclib-d8. Molecular Formula: C24H21D8N7O2. Formula Weight: 455.6. Purity: >99% deuterated forms (d1-d8). Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble. SMILES: O=C1N(C2CCCC2)C3=NC(NC4=NC=C(N5C([2H])([2H])C([2H])([2H])NC([2H])([2H])C5([2H])[2H])C=C4)=NC=C3C(C)=C1C(C)=O. InChi Code: InChI=1S/C24H29N7O2/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)/i9D2,10D2,11D2,12D2. InChi Key: AHJRHEGDXFFMBM-PMCMNDOISA-N.