PF-06873600

PF-06873600 is an inhibitor of cyclin-dependent kinase 2 (Cdk2), Cdk4, and Cdk6 (Kis = 0.13, 1.25, and 0.11 nM, respectively). It is selective for these CDKs over Cdk1 and Cdk9 (Kis = 4.5 and 19.6 nM, respectively). PF-06873600 inhibits the phosphorylation of RB transcriptional corepressor 1 (RB1) in, and the proliferation of, OVCAR-3 ovarian cancer cells (EC50s = 19 and 45 nM, respectively). In vivo, PF-06873600 (30 mg/kg) reduces tumor volume in CTG-0464 and CTG-01912 non-small cell lung cancer (NSCLC) patient-derived xenograft (PDX) mouse models.Formal Name: 6-(difluoromethyl)-8-[(1R,2R)-2-hydroxy-2-methylcyclopentyl]-2-[[1-(methylsulfonyl)-4-piperidinyl]amino]-pyrido[2,3-d]pyrimidin-7(8H)-one. CAS Number: 2185857-97-8. Synonyms: PF-3600. Molecular Formula: C20H27F2N5O4S. Formula Weight: 471.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 10 mg/ml, DMSO: 15 mg/ml. lambdamax: 228, 350 nm. SMILES: O=C1N([C@@]2([H])[C@](O)(CCC2)C)C3=NC(NC4CCN(CC4)S(C)(=O)=O)=NC=C3C=C1C(F)F. InChi Code: InChI=1S/C20H27F2N5O4S/c1-20(29)7-3-4-15(20)27-17-12(10-14(16(21)22)18(27)28)11-23-19(25-17)24-13-5-8-26(9-6-13)32(2,30)31/h10-11,13,15-16,29H,3-9H2,1-2H3,(H,23,24,25)/t15-,20-/m1/s1. InChi Key: QIEKHLDZKRQLLN-FOIQADDNSA-N.