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Ningetinib (CT-053) (CT053PTSA) 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 |
---|---|---|---|
2 mg | $42 | In Stock | |
5 mg | $68 | In Stock | |
10 mg | $97 | In Stock | |
25 mg | $198 | In Stock | |
50 mg | $343 | In Stock | |
100 mg | $587 | In Stock | |
1 mL x 10 mM (in DMSO) | $75 | In Stock |
Description | Ningetinib (CT-053) (CT053PTSA) 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), c-Met:6.7 nM (cell free), Axl:<1 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. |
Alias | CT053PTSA, CT-053 |
Molecular Weight | 556.58 |
Formula | C31H29FN4O5 |
Cas No. | 1394820-69-9 |
Smiles | Cc1c(C(=O)Nc2ccc(Oc3ccnc4cc(OCC(C)(C)O)ccc34)c(F)c2)c(=O)n(-c2ccccc2)n1C |
Relative Density. | 1.348 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
Solubility Information | DMSO: 15 mg/mL (26.95 mM), Sonication is recommended. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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