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Ningetinib Tosylate is an orally bioavailable tyrosine kinase inhibitor with IC50s of <1.0, 1.9 and 6.7 nM for Axl, VEGFR2, and c-Met, respectively.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | 38 € | In Stock | |
10 mg | 55 € | In Stock | |
25 mg | 107 € | In Stock | |
50 mg | 197 € | In Stock | |
100 mg | 362 € | In Stock | |
1 mL x 10 mM (in DMSO) | 61 € | In Stock |
Description | Ningetinib Tosylate is an orally bioavailable tyrosine kinase inhibitor with IC50s of <1.0, 1.9 and 6.7 nM for Axl, VEGFR2, and c-Met, respectively. |
Targets&IC50 | VEGFR2:1.9 nM (cell free), Axl:<1 nM (cell free), c-Met:6.7 nM (cell free) |
In vitro | In cell-based functional assays, Ningetinib inhibits VEGF and HGF-stimulated HUVEC proliferation and microvascular angiogenesis in rat aortic rings with IC50 values of 6.3 and 8.6 nM, respectively. |
In vivo | In the orthotopic U87MG human glioblastoma xenograft model, Ningetinib prolongs the median survival time and yields a significant increase in life-span value (ILS=32%) at an oral dose of 20 mg/kg/day (dosed 21 days) versus the vehicle-treated group. When single dosed orally (3 mg/kg) to U87MG tumor-bearing nude mice, Ningetinib potently inhibits the phosphorylation of c-Met and its downstream signaling kinases AKT and ERK1/2 for up to 6 hours in tumor tissues. |
Molecular Weight | 728.79 |
Formula | C38H37FN4O8S |
Cas No. | 1394820-77-9 |
Smiles | Cc1ccc(cc1)S(O)(=O)=O.Cc1c(C(=O)Nc2ccc(Oc3ccnc4cc(OCC(C)(C)O)ccc34)c(F)c2)c(=O)n(-c2ccccc2)n1C |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
Solubility Information | DMSO: 8 mg/mL (10.98 mM), Sonication and heating are recommended. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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