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Ningetinib Tosylate

Names

[ CAS No. ]:
1394820-77-9

[ Name ]:
Ningetinib Tosylate

[Synonym ]:
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)

Biological Activity

[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.


[Related Small Molecules]

Bemcentinib (R428) | Nintedanib (BIBF 1120) | SU5416 | Gilteritinib | Apatinib Mesylate | PD173074 | Capmatinib (INCB28060) | Foretinib (GSK1363089) | PHA-665752 | SU 5402 | Linifanib (ABT-869) | Cediranib | Lucitanib | RAF265 (CHIR-265) | LY2784544

Chemical & Physical Properties

[ Molecular Formula ]:
C38H37FN4O8S

[ Molecular Weight ]:
728.79

[ Exact Mass ]:
728.231628

[ Storage condition ]:
2-8℃

Related Compounds