CS2164

CS2164 is a multi-kinase inhibitor. It inhibits VEGFR1, -2, and -3 (IC50s = 8, 7, and 9 nM, respectively), PDGFRalpha and PDGFRbeta (IC50s = 1 and 93 nM), c-Kit (IC50 = 4 nM), Aurora B kinase (IC50 = 9 nM), and CSF-1 receptor tyrosine kinase (FMS, IC50 = 7 nM). CS2164 is selective for these kinases over a panel of 72 additional kinases, 76 GPCRs, two phosphatases, and nine ion channels (IC50s = >100 nM for all). It inhibits VEGF-induced proliferation of human umbilical vein endothelial cells (HUVECs, GI50 = 20.7 nM) and PDGF-induced proliferation of NIH3T3 cells (GI50 = 44.16 nM). In vivo, CS2164 (20 mg/kg) reduces tumor vascularization and tumor growth in a COLO 320 colon cancer mouse xenograft model. It also reduces tumor volume in A549, HCT-8, SMMC-7721, and MGC803 mouse xenograft models when administered at doses ranging from 2.5 to 40 mg/kg.Formal Name: N-(2-aminophenyl)-6-[(7-methoxy-4-quinolinyl)oxy]-1-naphthalenecarboxamide. CAS Number: 1256349-48-0. Synonyms: Chiauranib, Ibcasertib. Molecular Formula: C27H21N3O3. Formula Weight: 435.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: Methanol: Soluble. SMILES: O=C(C1=CC=CC2=CC(OC3=C4C=CC(OC)=CC4=NC=C3)=CC=C21)NC5=C(N)C=CC=C5. InChi Code: InChI=1S/C27H21N3O3/c1-32-18-9-12-22-25(16-18)29-14-13-26(22)33-19-10-11-20-17(15-19)5-4-6-21(20)27(31)30-24-8-3-2-7-23(24)28/h2-16H,28H2,1H3,(H,30,31). InChi Key: BRKWREZNORONDU-UHFFFAOYSA-N.