ChemicalBook--->CAS DataBase List--->1394820-69-9

1394820-69-9

1394820-69-9 Structure

1394820-69-9 Structure
IdentificationBack Directory
[Name]

Ningetinib
[CAS]

1394820-69-9
[Synonyms]

CS-2653
CT053PTSA
Ningetinib
Ningetinib(free base)
Ningetinib-Tosylate(free base)
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-
[Molecular Formula]

C31H29FN4O5
[MDL Number]

MFCD28502048
[MOL File]

1394820-69-9.mol
[Molecular Weight]

556.58
Chemical PropertiesBack Directory
[density ]

1.348±0.06 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[solubility ]

DMF: 15 mg/ml; DMF:PBS (pH 7.2) (1:5): 0.16 mg/ml; DMSO: 2 mg/ml
[form ]

A crystalline solid
[pka]

11.00±0.70(Predicted)
[color ]

White to off-white
Hazard InformationBack Directory
[Uses]

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 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].

[IC 50]

VEGFR2: 1.9 nM (IC50); Axl
Spectrum DetailBack Directory
[Spectrum Detail]

Ningetinib(1394820-69-9)1HNMR
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