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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO 18 mg/mL|
|Related VEGFR/PDGFR Products|
TAS-115 (Pamufetinib) mesylate inhibited the kinase activity of both VEGFR2 and MET and their signal-dependent cell growth as strongly as other known VEGFR or MET inhibitors.
Tanshinone IIA suppresses angiogenesis by targeting the protein kinase domains of VEGF/VEGFR2. *The compound is unstable in solutions, freshly prepared is recommended.
AC710 is a potent, selective and orally active platelet-derived growth factor receptor-family (PDGFR) kinase inhibitor with potential anticancer activity.
Sitravatinib (MGCD516) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor.
ODM-203 is an orally available inhibitor of VEGFR and FGFR, with IC50s of 26, 9, 5 nM for VEGFR1, VEGFR2 and VEGFR3, and 11, 16, 6, 35 nM for recombinant FGFR1, FGFR2, FGFR3 and FGFR4, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.