c-Met-IN-12

Names

[ CAS No. ]:
2426675-70-7

[ Name ]:
c-Met-IN-12

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Met/HGFR

[Target]

c-Met:10.6 nM (IC50)


[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C34H29FN4O4

[ Molecular Weight ]:
576.62

Related Compounds