| Identification | Back Directory | [Name]
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 p-toluenesulfonate | [CAS]
1394820-77-9 | [Synonyms]
CT-053
112176
CT-053 tosylate
Ningetinib (Tosylate)
Ningetinib-Tosylate(tosylate)
Ningetinib Tosylate (CT-053 Tosylate)
N-(3-Fluoro-4-((7-(2-hydroxy-2-methylpropoxy)quinolin-4-yl)oxy)phenyl)-1,5-dimethyl-3-oxo-2-ph
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 p-toluenesulfonate
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 4-methylbenzenesulfonate
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) | [Molecular Formula]
C38H37FN4O8S | [MDL Number]
MFCD28142839 | [MOL File]
1394820-77-9.mol | [Molecular Weight]
728.786 |
| Chemical Properties | Back Directory | [storage temp. ]
Inert atmosphere,2-8°C | [solubility ]
DMSO: 33.33 mg/mL (45.73 mM); Water: < 0.1 mg/mL (insoluble) | [form ]
Solid | [color ]
White to off-white | [InChIKey]
NAUYISNCVNUUDK-UHFFFAOYSA-N | [SMILES]
N1(C)C(C)=C(C(NC2=CC=C(OC3=C4C(=NC=C3)C=C(OCC(O)(C)C)C=C4)C(F)=C2)=O)C(=O)N1C1=CC=CC=C1.C1(S(O)(=O)=O)=CC=C(C)C=C1 |
| Hazard Information | Back Directory | [Uses]
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 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]. | [IC 50]
Axl; VEGFR2: 1.9 nM (IC50) | [storage]
Store at -20°C | [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. |
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