JNJ-38158471

JNJ-38158471 is an inhibitor of VEGFR2 (IC50 = 42 nM). It is selective for VEGFR2 over the PDGFR family kinases CSF-1 receptor tyrosine kinase (FMS), PDGFRalpha, FMS-related tyrosine kinase 3 (FLT3), and KIT (IC50s = 624, 1,109, 4,810, and 511 nM, respectively) and VEGFR family kinases VEGFR1 and VEGFR3 (IC50s = 4,451 and 1,112 nM, respectively) but does inhibit RET (IC50 = 183 nM). JNJ-38158471 (10, 100, or 500 nM) decreases VEGF-induced phosphorylation of VEGFR2 in serum-starved human umbilical vein endothelial cells (HUVECs). It inhibits VEGF-induced migration in HUVECs when used at a concentration of 1 µM. JNJ-38158471 (100 mg/kg) reduces Vegf-induced corneal neovascularization in mice. It decreases tumor size in an HCT116 colorectal cancer mouse xenograft model when administered at doses ranging from 10 to 200 mg/kg per day. JNJ-38158471 (100 mg/kg per day) reduces polyp number in an Apc+/Min-FCCC mouse model of spontaneous colorectal adenoma.Formal Name: N-[4-[[6-amino-5-[(methoxyimino)methyl]-4-pyrimidinyl]oxy]-2-chlorophenyl]-N'-ethyl-urea. CAS Number: 951151-97-6. Molecular Formula: C15H17ClN6O3. Formula Weight: 364.8. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Slightly soluble: 0.1-1 mg/mL. SMILES: O=C(NCC)NC1=C(Cl)C=C(C=C1)OC2=NC=NC(N)=C2C=NOC. InChi Code: InChI=1S/C15H17ClN6O3/c1-3-18-15(23)22-12-5-4-9(6-11(12)16)25-14-10(7-21-24-2)13(17)19-8-20-14/h4-8H,3H2,1-2H3,(H2,17,19,20)(H2,18,22,23). InChi Key: BJHCYTJNPVGSBZ-UHFFFAOYSA-N.