1394820-69-9

1394820-69-9 structure

Name: Ningetinib
Chemical Name: Ningetinib
CAS Number: 1394820-69-9
Molecular Formula: C₃₁H₂₉FN₄O₅
Molecular Weight: 556.58
Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK c-Met/HGFR
Create Date: 2018-04-06 23:23:07
Modify Date: 2024-01-08 10:00:07
Ningetinib is a potent, orally bioavailable small molecule tyrosine kinase inhibitor (TKI) with IC50s of 6.7, 1.9 and <1.0 nM for c-Met, VEGFR2 and Axl, respectively.

Name	Ningetinib

Description	Ningetinib is a potent, orally bioavailable small molecule tyrosine kinase inhibitor (TKI) with IC50s of 6.7, 1.9 and <1.0 nM for c-Met, VEGFR2 and Axl, respectively.
Related Catalog	Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Met/HGFR Signaling Pathways >> Protein Tyrosine Kinase/RTK >> TAM Receptor Research Areas >> Cancer
Target	VEGFR2:1.9 nM (IC50)
In Vitro	Ningetinib is a potent, orally bioavailable small molecule tyrosine kinase inhibitor (TKI) with IC50s of 6.7, 1.9 and <1.0 nM for c-Met, VEGFR2 and Axl, respectively. In cell-based functional assays, Ningetinib (CT053PTSA) inhibits HGF and VEGF-stimulated HUVEC proliferation and microvascular angiogenesis in rat aortic rings with IC50 values of 8.6 and 6.3 nM, respectively[1].
In Vivo	When single dosed orally (3 mg/kg) to U87MG tumor-bearing nude mice, Ningetinib (CT053PTSA) potently inhibits the phosphorylation of c-Met and its downstream signaling kinases AKT and ERK1/2 for up to 6 hours in tumor tissues. In orthotopic U87MG human glioblastoma xenograft model, Ningetinib prolongs the median survival time (MST) and yields significant increase in life-span value (ILS=32%, p=0.003) at an oral dose of 20 mg/kg/day (dosed 21 days) versus the vehicle-treated group[1].
References	[1]. Ning Xi, et al. Abstract 1755: CT053PTSA, a novel c-MET and VEGFR2 inhibitor, potently suppresses angiogenesis and tumor growth. Cancer Res 2014;74(19 Suppl):Abstract nr 1755.