CYY292

CYY292 is an inhibitor of PDGFRalpha, PDGFRbeta, FGFR1, -2, and -3, (IC50s = 5.35, 4.6, 28, 28, and 78 nM, respectively). It is selective for these kinases over FGFR4 (IC50 = >1,000 nM) but also inhibits c-Kit, VEGFR2, VEGFR1, and insulin-like growth factor 1 receptor (IGF-1R, IC50s = 67, 33, 36, and 75 nM, respectively), as well as EGFR, Bruton's tyrosine kinase (BTK), cyclin-dependent kinase 4 (Cdk4)/cyclin D3, and MET (IC50s = 128, 198, 214, and 396 nM, respectively). CYY292 inhibits the proliferation of MG-63, U2OS, MNNG/HOS, and Saos-2 osteosarcoma cells (IC50s = 0.84, 0.76, 1.36, and 0.72 µM, respectively). It inhibits the migration and invasion of U87MG and LN-229 glioblastoma cells when used at concentrations of 0.3 and 0.5 µM. CYY292 (30 mg/kg) decreases tumor volume and increases survival in a U87MG orthotopic mouse xenograft model.Formal Name: N4-1H-indazol-6-yl-N2-[3-methoxy-4-(4-methyl-1-piperazinyl)phenyl]-5-methyl-2,4-pyrimidinediamine. CAS Number: 2644673-04-9. Molecular Formula: C24H28N8O. Formula Weight: 444.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: Ethanol: Slightly soluble, Methanol: Slightly soluble. SMILES: CN1CCN(C2=CC=C(NC(N=C3NC4=CC(NN=C5)=C5C=C4)=NC=C3C)C=C2OC)CC1. InChi Code: InChI=1S/C24H28N8O/c1-16-14-25-24(29-23(16)27-18-5-4-17-15-26-30-20(17)12-18)28-19-6-7-21(22(13-19)33-3)32-10-8-31(2)9-11-32/h4-7,12-15H,8-11H2,1-3H3,(H,26,30)(H2,25,27,28,29). InChi Key: PCQOIBJOKXSDEB-UHFFFAOYSA-N.