cp-673451

Description: CP-673451 (CP673451) is a novel, potent, selective and ATP-competitive inhibitor of PDGFR(alpha/beta) with potential antitumor activity. It inhibits PDGFR(alpha/beta) with IC50s of 10 nM/1 nM in cell-free assays and displays > 450-fold selectivity for PDGFR(alpha/beta) over other angiogenic receptors. CP-673451 has antiangiogenic and antitumor activity. and is being investigated to treat cancer. CP-673451 exhibits excellent anti-proliferative activity in vitro and high in vivo antitumor efficacy (at 20 mg/kg) with a medium suppression of tumor growth, while high-dose CP-673451 (40 mg/kg) strongly inhibits tumor growth in mice without significant weitht loss.

References: Cancer Res. 2005 Feb 1; 65(3):957-66; Cancer Res. 2013 Apr 1; 73(7):2139-49.

Chemical Name: 1-(2-(5-(2-Methoxyethoxy)benzimidazol-1-yl)quinolin-8-yl)piperidin-4-ylamine

InChi Key: DEEOXSOLTLIWMG-UHFFFAOYSA-N

InChi Code: InChI=1S/C24H27N5O2/c1-30-13-14-31-19-6-7-21-20(15-19)26-16-29(21)23-8-5-17-3-2-4-22(24(17)27-23)28-11-9-18(25)10-12-28/h2-8, 15-16, 18H, 9-14, 25H2, 1H3

SMILES Code: NC1CCN(C2=C3N=C(N4C5=CC=C(OCCOC)C=C5N=C4)C=CC3=CC=C2)CC1