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Ningetinib is a potent, orally bioavailable tyrosine kinase inhibitor for Axl, VEGFR2 and c-Met with IC50 values of <1.0, 1.9 and 6.7 nM, respectively. Ningetinib (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.
In vivo, Ningetinib (3 mg/kg; orally) treatment on U87MG tumor-bearing nude mice 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 | 556.58 |
| Formula | C31H29FN4O5 |
| CAS Number | 1394820-69-9 |
| Solubility (25°C) | DMSO 16 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related VEGFR/PDGFR Products |
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| ABT-869
ABT-869 (Linifanib) is an ATP-competitive, multi-targeted RTK inhibitor that is completely effective against all members of VEGFR and PDGFR. |
| Tivozanib (AV-951)
Tivozanib (AV-951) is a potent VEGFR-1, 2 and 3, c-Kit and PDGFR inhibitor with IC50 of 0.21, 0.16, 0.24, 1.63 and 1.72 nM respectively. |
| Axitinib
Axitinib (AG013736) inhibits multiple targets including VEGFR, PDGFR and cKit. |
| Regorafenib
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