KRN-633

• CAT Number: I002976
• CAS Number: 286370-15-8
• Molecular Formula: C₂₀H₂₁ClN₄O₄
• Molecular Weight: 416.86
• Purity: ≥95%
• Synonyms: 1-[2-chloro-4-(6,7-dimethoxyquinazolin-4-yl)oxyphenyl]-3-propylurea
• Target: VEGFR
• Solubility: DMSO ≥8mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL
• Storage: 3 years -20C powder
• IC50: 170 nM/160 nM/125 nM (VEGFR1/2/3) [1]
• InChI: nChI=1S/C20H21ClN4O4/c1-4-7-22-20(26)25-15-6-5-12(8-14(15)21)29-19-13-9-17(27-2)18(28-3)10-16(13)23-11-24-19/h5-6,8-11H,4,7H2,1-3H3,(H2,22,25,26)
• InChIKey: VPBYZLCHOKSGRX-UHFFFAOYSA-N
• SMILES: CCCNC(=O)NC1=C(C=C(C=C1)OC2=NC=NC3=CC(=C(C=C32)OC)OC)Cl

KRN-633 (Cat No.: I002976) is a potent and selective inhibitor of vascular endothelial growth factor receptors (VEGFRs), particularly VEGFR-2, with additional activity against PDGFR and FGFR1. It blocks angiogenesis and tumor growth by targeting key pathways involved in blood vessel formation. KRN-633 has shown antitumor effects in preclinical cancer models, making it valuable in oncology research. Its oral bioavailability and kinase selectivity profile support its use in studying VEGF-mediated signaling and developing anti-angiogenic therapeutic strategies for cancer and related diseases.

Reference

[1]. Nakamura K, et al. KRN633: A selective inhibitor of vascular endothelial growth factor receptor-2 tyrosine kinase that suppresses tumor angiogenesis and growth. Mol Cancer Ther, 2004, 3(12), 1639-1649.
[2]. Ban HS, et al. Suppression of hypoxia-induced HIF-1alpha accumulation by VEGFR inhibitors: Different profiles of AAL993 versus SU5416 and KRN633. Cancer Lett, 2010, 296(1), 17-26.
[3]. Wada Y, et al. Effects of KRN633, an inhibitor of vascular endothelial growth factor receptor-2 tyrosine kinase, on vascular development of placenta and fetus of mid-pregnancy in mice. J Pharmacol Sci, 2010, 112(3), 290-298.