Ningetinib Tosylate structure
|
Common Name | Ningetinib Tosylate | ||
|---|---|---|---|---|
| CAS Number | 1394820-77-9 | Molecular Weight | 728.79 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C38H37FN4O8S | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of Ningetinib TosylateNingetinib 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. |
| Name | Ningetinib Tosylate |
|---|---|
| Synonym | More Synonyms |
| 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 | |
| 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 |
| Molecular Formula | C38H37FN4O8S |
|---|---|
| Molecular Weight | 728.79 |
| Exact Mass | 728.231628 |
| InChIKey | NAUYISNCVNUUDK-UHFFFAOYSA-N |
| SMILES | Cc1c(C(=O)Nc2ccc(Oc3ccnc4cc(OCC(C)(C)O)ccc34)c(F)c2)c(=O)n(-c2ccccc2)n1C.Cc1ccc(S(=O)(=O)O)cc1 |
| Storage condition | 2-8℃ |
| 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) |