Ningetinib
Ningetinib Basic information
- Product Name:
- Ningetinib
- Synonyms:
-
- CS-2653
- Ningetinib-Tosylate(free base)
- Ningetinib
- Ningetinib(free base)
- CT053PTSA
- 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-
- N-(3-fluoro-4-((7-(2-hydroxy-2-methylpropoxy)quinolin-4-yl)oxy)phenyl)-1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide
- Vascular endothelial growth factor receptor,inhibit,c-Met/HGFR,TAM Receptor,Mer,Tyro3,VEGFR,Ningetinib,Axl,Inhibitor
- CAS:
- 1394820-69-9
- MF:
- C31H29FN4O5
- MW:
- 556.58
- Mol File:
- 1394820-69-9.mol
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Ningetinib Chemical Properties
- 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
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Ningetinib Usage And Synthesis
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
NingetinibSupplier
ChemShuttle, Inc.
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- 0510-83588313-811 18800520310
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Shanghai Topbiochem Technology Co., Ltd
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- 021-58170097
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ShangHai Caerulum Pharma Discovery Co., Ltd.
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- 18149758185
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Shanghai Lollane Biological Technology Co.,Ltd.
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- 021-52996696，15000506266 15000506266
Shanghai YuanYe Biotechnology Co., Ltd.
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- 021-61312847; 18021002903
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