Motesanib diphosphate (AMG 706) is a novel oral inhibitor of VEGF receptors, platelet-derived growth-factor receptor, and KIT. It is used as the phosphate salt motesanib diphosphate. Motesanib Diphosphate significantly inhibits VEGF-induced cellular proliferation of HUVECs with an IC50 of 10 nM, while displaying little effect at bFGF-induced proliferation with an IC50 of >3,000 nM. Motesanib Diphosphate (AMG 706) induces a dose-dependent tumor regression of established A431 xenografts by selectively targeting neovascularization in tumor cells. Motesanib diphosphate (AMG 706) can induce partial responses in patients with advanced or metastatic differentiated thyroid cancer that is progressive.
|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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO 100 mg/mL
Water 100 mg/mL
In vitro metabolism of the novel, highly selective oral angiogenesis inhibitor motesanib diphosphate in preclinical species and in humans.
Li C, et al. Drug Metab Dispos. 2009 Jul;37(7):1378-94. PMID: 19372226.
Motesanib diphosphate in progressive differentiated thyroid cancer.
Sherman SI, et al. N Engl J Med. 2008 Jul 3;359(1):31-42. PMID: 18596272.
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Ranibizumab is a monoclonal antibody that inhibits angiogenesis by inhibiting Vascular endothelial growth factor A.
NVP-ACC789 is an inhibitor of human VEGFR-1, VEGFR-2 (mouse VEGFR-2), VEGFR-3 and PDGFR-β with IC50s of 0.38, 0.02 (0.23), 0.18, 1.4 μM, respectively.
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