bms-754807

Description: BMS-754807 (BMS754807) is an orally bioavailable small molecule inhibitor of IGF-1R/InsR (growth factor 1 receptor/insulin receptor family kinases) with potential antineoplastic activity. It inhibits IGF-1R/InsR with IC50s of 1.8 nM/1.7 nM in cell-free assays, and is less potent against other kinases such as Met, PKA, Aurora A/B, Flt3, Lck, MK2, TrkA/B, Ron, PKC etc. It exhibits excellent in vivo antitumor efficacy in nude mice bearing IGF-1R-Sal, GEO, Colo205, JJN3, RD1 or Rh41 tumors.

References: Mol Cancer Ther. 2009 Dec; 8(12):3341-9; J Med Chem. 2009 Dec 10; 52(23):7360-3.

Chemical Name: (S)-1-(4-((5-cyclopropyl-1H-pyrazol-3-yl)amino)pyrrolo[2, 1-f][1, 2, 4]triazin-2-yl)-N-(6-fluoropyridin-3-yl)-2-methylpyrrolidine-2-carboxamide.

InChi Key: LQVXSNNAFNGRAH-QHCPKHFHSA-N

InChi Code: InChI=1S/C23H24FN9O/c1-23(21(34)26-15-7-8-18(24)25-13-15)9-3-10-32(23)22-28-20(17-4-2-11-33(17)31-22)27-19-12-16(29-30-19)14-5-6-14/h2, 4, 7-8, 11-14H, 3, 5-6, 9-10H2, 1H3, (H, 26, 34)(H2, 27, 28, 29, 30, 31)/t23-/m0/s1

SMILES Code: O=C([C]1(C)N(C(N=C2NC3=NNC(C4CC4)=C3)=NN5C2=CC=C5)CCC1)NC6=CC=C(F)N=C6