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MedKoo CAT#: 406461
CAS#: 1221713-92-3
Description: NPS-1034 is a novel MET inhibitor, which inhibits the activated MET receptor and its constitutively active mutants. NPS-1034, inhibits various constitutively active mutant forms of MET as well as HGF-activated wild-type MET. NPS-1034 inhibited the proliferation of cells expressing activated MET and promoted the regression of tumors formed from such cells in a mouse xenograft model through anti-angiogenic and pro-apoptotic actions. NPS-1034 also inhibited HGF-stimulated activation of MET signaling in the presence or absence of serum. Notably, NPS-1034 inhibited three MET variants that are resistant to the MET inhibitors SU11274, NVP-BVU972, and PHA665752.
MedKoo Cat#: 406461
Name: NPS-1034
CAS#: 1221713-92-3
Chemical Formula: C31H23F2N5O3
Exact Mass: 551.1769
Molecular Weight: 551.54283
Elemental Analysis: C, 67.51; H, 4.20; F, 6.89; N, 12.70; O, 8.70
Synonym: NPS1034; NPS-1034; NPS 1034.
IUPAC/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
1: Shin JS, Hong SW, Moon JH, Kim JS, Jung KA, Kim SM, Lee DH, Kim I, Yoon SJ, Lee CG, Choi EK, Lee JY, Kim KP, Hong YS, Lee JL, Kim B, Choi EK, Lee JS, Jin DH, Kim TW. NPS-1034, a novel MET inhibitor, inhibits the activated MET receptor and its constitutively active mutants. Invest New Drugs. 2013 Oct 31. [Epub ahead of print] PubMed PMID: 24173966.