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Motesanib Diphosphate

Cat. No. M1920
Motesanib Diphosphate Structure
Synonym:

AMG 706

Size Price Availability Quantity
10mg USD 200 In stock
50mg USD 600 In stock
100mg USD 980 In stock
200mg USD 1180 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 569.44
Formula C22H23N5O.2H3PO4
CAS Number 857876-30-3
Purity >99%
Solubility DMSO 100 mg/mL
Water 100 mg/mL
Storage at -20°C
References

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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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Motesanib Diphosphate, AMG 706 supplier, VEGFR/PDGFR, inhibitors

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