CGP 60474

CGP 60474 is an inhibitor of cyclin-dependent kinases (CDKs, IC50s = 0.017, 0.08, and 0.05 µM for Cdk1/cyclin B, Cdk2/cyclin A, and Cdk2/cyclin E, respectively). It is selective for these CDKs over Cdk4/cyclin D1 (IC50 = 0.7 µM) and a variety of other kinases, including several PKC isoforms (IC50s = 1.9->100 µM), PKA (IC50 = 160 µM), and FLT1 (IC50 = 1 µM), among others, but does inhibit PKCalpha and v-Abl (IC50s = 0.25 and 0.4 µM, respectively). It inhibits proliferation of colon, breast, lung, prostate, and ovarian cancer cells (IC50s = 25-84, 21-280, 40 and 68, 17 and 20, and 18-38 nM, respectively). CGP 60474 also reduces LPS-induced IL-6, TNF-alpha, and RANTES secretion from J774.1 cells in a concentration-dependent manner and inhibits poly(I:C)-induced NF-kappaB nuclear translocation in the same cells when used at concentrations of 8 and 32 nM. It reduces plasma IL-6 levels and increases survival in a mouse model of LPS-induced endotoxemia when administered at a dose of 10 mg/kg.Formal Name: 3-[[4-[2-[(3-chlorophenyl)amino]-4-pyrimidinyl]-2-pyridinyl]amino]-1-propanol. CAS Number: 164658-13-3. Molecular Formula: C18H18ClN5O. Formula Weight: 355.8. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: 10 mM. SMILES: ClC1=CC(NC2=NC(C3=CC=NC(NCCCO)=C3)=CC=N2)=CC=C1. InChi Code: InChI=1S/C18H18ClN5O/c19-14-3-1-4-15(12-14)23-18-22-9-6-16(24-18)13-5-8-21-17(11-13)20-7-2-10-25/h1,3-6,8-9,11-12,25H,2,7,10H2,(H,20,21)(H,22,23,24). InChi Key: IYNDTACKOAXKBJ-UHFFFAOYSA-N.