krn-633

Description: KRN 633 (KRN-633) is a novel, potent, selective, cell-permeable, reversible, and ATP-competitive inhibitor of VEGFR1/2/3 with potential antitumor activity. It inhibits VEGFR1/2/3 with IC50s of 170 nM/160 nM/125 nM, weakly inhibits PDGFR-alpha/beta and c-Kit, and does not block the phosphorylation of FGFR-1, EGFR or c-Met in cell. KRN633 inhibits tumor growth in several in vivo tumor xenograft models with diverse tissue origins, including lung, colon, and prostate, in athymic mice and rats. KRN633 also causes the regression of some well-established tumors and those that had regrown after the cessation of treatment. KRN633 was well tolerated and had no significant effects on body weight or the general health of the animals. KRN633 might be useful in the treatment of solid tumors and other diseases that depend on pathologic angiogenesis.

References: Mol Cancer Ther. 2004 Dec; 3(12):1639-49; Cancer Lett. 2010 Oct 1; 296(1):17-26; J Pharmacol Sci. 2010; 112(3):290-8.

Synonym: KRN-633; KRN633; KRN 633.

Chemical Name: 1-(2-chloro-4-(6, 7-dimethoxyquinazolin-4-yloxy)phenyl)-3-propylurea

InChi Key: VPBYZLCHOKSGRX-UHFFFAOYSA-N

InChi Code: InChI=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)

SMILES Code: O=C(NCCC)NC1=CC=C(OC2=C3C=C(OC)C(OC)=CC3=NC=N2)C=C1Cl