Ningetinib Tosylate

Modify Date: 2024-01-08 11:21:32

Ningetinib Tosylate structure	Common Name	Ningetinib Tosylate
	CAS Number	1394820-77-9	Molecular Weight	728.79
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₃₈H₃₇FN₄O₈S	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of Ningetinib Tosylate

Ningetinib Tosylate 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 Tosylate
Synonym	More Synonyms

Description	Ningetinib Tosylate 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 Tosylate 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 Tosylate (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 Tosylate (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 Tosylate 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.

Molecular Formula	C₃₈H₃₇FN₄O₈S
Molecular Weight	728.79
Exact Mass	728.231628
Storage condition	2-8℃

N-(3-Fluoro-4-{[7-(2-hydroxy-2-methylpropoxy)-4-quinolinyl]oxy}phenyl)-1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide 4-methylbenzenesulfonate (1:1)

1H-Pyrazole-4-carboxamide, N-[3-fluoro-4-[[7-(2-hydroxy-2-methylpropoxy)-4-quinolinyl]oxy]phenyl]-2,3-dihydro-1,5-dimethyl-3-oxo-2-phenyl-, 4-methylbenzenesulfonate (1:1) (salt)

Ningetinib Tosylate

Use of Ningetinib Tosylate

Names

Ningetinib Tosylate Biological Activity

Chemical & Physical Properties

Synonyms