| Identification | Back 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 Properties | Back 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 Information | Back 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 |
|
| Company Name: |
Twochem Co.Ltd.
|
| Tel: |
021-58111628 15800915896 |
| Website: |
cn.twochem.com |
| Company Name: |
Cckinase, Inc.
|
| Tel: |
+1 (732)236-3202 |
| Website: |
www.cckinase.com |
|