NPS-1034

Description: NPS-1034 (NPS1034; NPS 1034) is a novel, potent dual inhibitor of the tyrosine kinases Met and Axl with potential antineoplastic activity. It inhibits Met and Axl with IC50s of 48 nM and 10.3 nM, respectively. NPS-1034 shows potent anti-proliferative activity in vitro against cells expressing MET and and high in vivo antitumor efficacy by promoting the regression of tumors in a mouse xenograft via anti-angiogenic & pro-apoptotic actions.

References: Cancer Res. 2014 Jan 1; 74(1):253-62; Invest New Drugs. 2014 Jun; 32(3):389-99.

Chemical Name: N-(3-fluoro-4-((3-phenyl-1H-pyrrolo[2, 3-b]pyridin-4-yl)oxy)phenyl)-2-(4-fluorophenyl)-1, 5-dimethyl-3-oxo-2, 3-dihydro-1H-pyrazole-4-carboxamide.

InChi Key: RGAZVGZUBCFHRJ-UHFFFAOYSA-N

InChi Code: InChI=1S/C31H23F2N5O3/c1-18-27(31(40)38(37(18)2)22-11-8-20(32)9-12-22)30(39)36-21-10-13-25(24(33)16-21)41-26-14-15-34-29-28(26)23(17-35-29)19-6-4-3-5-7-19/h3-17H, 1-2H3, (H, 34, 35)(H, 36, 39)

SMILES Code: O=C(C1=C(C)N(C)N(C2=CC=C(F)C=C2)C1=O)NC3=CC=C(OC4=C5C(NC=C5C6=CC=CC=C6)=NC=C4)C(F)=C3