JNJ-38158471

• CAT Number: I015026
• CAS Number: 951151-97-6
• Molecular Formula: C15H17ClN6O3
• Molecular Weight: 364.79
• Purity: ≥95%
• Synonyms: 1-[4-[6-amino-5-[(E)-methoxyiminomethyl]pyrimidin-4-yl]oxy-2-chlorophenyl]-3-ethylurea
• InChI: 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)/b21-7+
• InChIKey: BJHCYTJNPVGSBZ-QPSGOUHRSA-N
• SMILES: CCNC(=O)NC1=C(C=C(C=C1)OC2=NC=NC(=C2C=NOC)N)Cl

JNJ-38158471 is a well tolerated, orally available, highly selective VEGFR-2 inhibitor, with an IC50 of 40 nM. JNJ-38158471 also inhibits Ret and Kit with IC50s of 180 and 500 nM, respectively[1].
JNJ-38158471 (1-500 nM; 1 hour) inhibits VEGF-stimulated VEGFR-2 autophosphorylation in HUVECs[1].
JNJ-38158471 (50-1000 nM; 12-16 hours) significantly inhibits VEGF-dependent HUVEC migration. Cellular toxicity is not observed following JNJ-38158471 treatment of HUVECs[1].
JNJ-38158471 (10 or 100 mg/kg; p.o.; once-daily) inhibits VEGF-induced corneal neovascularization[1].
JNJ-38158471 (10-200 mg/kg; p.o.) inhibits the growth of human tumor xenografts in a dose-dependent manner in both A431 and HCT116 models. JNJ-38158471 treatment is well tolerated, following continuous administration for 24 days, body weights were comparable with control animals[1].
JNJ-38158471 (100 mg/kg; p.o.; once-daily) treatment shows statistically significant activity compare with vehicle treat animals. The body weights of both JNJ-38158471-treated and vehicle-treated groups were comparable at study end[1].

Reference

[1]. Kenneth RL, et, al. A Highly Selective, Orally Bioavailable, Vascular Endothelial Growth Factor receptor-2 Tyrosine Kinase Inhibitor Has Potent Activity in Vitro and in Vivo. Angiogenesis. 2009; 12(3): 287-96.
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