| Identification | Back Directory | [Name]
1,6-Naphthyridin-4(1H)-one, 5-[[3-fluoro-4-[[7-(2-hydroxy-2-methylpropoxy)-4-quinolinyl]oxy]phenyl]amino]-1-methyl-3-phenyl- | [CAS]
2426675-70-7 | [Synonyms]
c-Met-IN-12
1,6-Naphthyridin-4(1H)-one, 5-[[3-fluoro-4-[[7-(2-hydroxy-2-methylpropoxy)-4-quinolinyl]oxy]phenyl]amino]-1-methyl-3-phenyl- | [Molecular Formula]
C34H29FN4O4 | [MOL File]
2426675-70-7.mol | [Molecular Weight]
576.62 |
| Hazard Information | Back Directory | [Uses]
c-Met-IN-12 (compound 4r) is an orally active, potent and selective type II c-Met kinase inhibitor, with an IC50 of 10.6 nM. c-Met-IN-12 displays high inhibitory effects (inhibition rate > 80% in 1 μM) against AXL, Mer and TYRO3 kinases. c-Met-IN-12 can be used a scaffold for further kinase selectivity enhancement. c-Met-IN-12 shows antitumor efficacy[1]. | [in vivo]
c-Met-IN-12 (compound 4r) (Tumor-bearing nude mice, 45 mg/kg, Orally, Q.D. for 21 days) exhibits significant tumor growth inhibition (93%) in a U-87MG human gliobastoma xenograft model[1]. | [References]
[1] Xu H, et al. Discovery of N-substituted-3-phenyl-1,6-naphthyridinone derivatives bearing quinoline moiety as selective type II c-Met kinase inhibitors against VEGFR-2. Bioorg Med Chem. 2020 Jun 15;28(12):115555. DOI:10.1016/j.bmc.2020.115555 |
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