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(AMG 706; AMG-706)
Motesanib Chemical Structure
|Product name: Motesanib|
|Cat. No.: HY-10228|
Motesanib (AMG-706) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 2 nM/3 nM/6 nM, respectively; similar activity against Kit, ~10-fold more selective for VEGFR than PDGFR and Ret.
IC50 value: 2 nM/3 nM/6 nM/8 nM(VEGFR1/2/3/c-Kit) 
Target: pan-VEGFR; Kit
in vitro: Motesanib Diphosphate has broad activity against the human VEGFR family, and displays >1000 selectivity against EGFR, Src, and p38 kinase. 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 also potently inhibits PDGF-induced proliferation and SCF-induced c-kit phosphorylation with IC50 of 207 nM and 37 nM, respectively, but not effective against the EGF-induced EGFR phosphorylation and cell viability of A431 cells . Althouth displaying little antiproliferative activity on cell growth of HUVECs alone, Motesanib Diphosphate treatment significantly sensitizes the cells to fractionated radiation .
in vivo: Administration of Motesanib Diphosphate at 100 mg/kg significantly inhibits VEGF-induced vascular permeability in a time-dependent manner. Oral administration of Motesanib Diphosphate twice daily or once daily potently inhibits, in a dose-dependent manner, VEGF-induced angiogenesis using the rat corneal model with ED50 of 2.1 mg/kg and 4.9 mg/kg, respectively. Motesanib Diphosphate induces a dose-dependent tumor regression of established A431 xenografts by selectively targeting neovascularization in tumor cells . Administration of Motesanib Diphosphate in combination with radiation displays significant anti-tumor activity in head and neck squamous cell carcinoma (HNSCC) xenograft models . Motesanib Diphosphate treatment also induces significant dose-dependent reductions in tumor growth and blood vessel density of MCF-7, MDA-MB-231, or Cal-51 xenografts, which can be markedly enhanced when combined with docetaxel or tamoxifen .
|M.Wt||373.45||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
10 mM in DMSO
|1 mg||5 mg||10 mg|
|1 mM||2.6777 mL||13.3887 mL||26.7773 mL|
|5 mM||0.5355 mL||2.6777 mL||5.3555 mL|
|10 mM||0.2678 mL||1.3389 mL||2.6777 mL|
|Product Name||Sponsor Only||Condition||Start Date||End Date||Phase||Last Change Date|
|Motesanib||Amgen Inc||Metastatic non small cell lung cancer||31-JUL-07||28-FEB-13||Phase 3||29-MAR-13|
|Amgen Inc||Metastatic ovary cancer||31-JUL-07||31-DEC-13||Phase 2||12-NOV-13|
|Amgen Inc||Solid tumor||31-DEC-05||31-JUL-12||Phase 2||12-OCT-12|
|Amgen Inc||Fallopian tube cancer||31-JUL-07||31-DEC-13||Phase 2||12-NOV-13|
|Amgen Inc||Peritoneal tumor||31-JUL-07||31-DEC-13||Phase 2||12-NOV-13|
|Amgen Inc||Non-small-cell lung cancer||31-JUL-07||31-AUG-11||Phase 2||16-AUG-12|
. Polverino A, et al. AMG 706, an oral, multikinase inhibitor that selectively targets vascular endothelial growth factor, platelet-derived growth factor, and kit receptors, potently inhibits angiogenesis and induces regression in tumor xenografts. Cancer Res, 2006, 66(17), 8715-8721.
. Coxon A, et al. Broad antitumor activity in breast cancer xenografts by motesanib, a highly selective, oral inhibitor of vascular endothelial growth factor, platelet-derived growth factor, and Kit receptors. Clin Cancer Res, 2009, 15(1), 110-118.
CAS No.: 857876-30-3 In-stock
2,4-Pyrimidinediamine with linker is a patent compound in WO2013055780A1, Page 71; multikinase inhibitor and has a -NH2 terminal linker for further synthesis.
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