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 (Synonyms  AMG 706; AMG-706)
453562-69-1  Technical Data: Price and Availability of  Cas No:453562-69-1

Cas : 453562-69-1 M.Wt: 373.45
Cas : 453562-69-1 Formula: C22H23N5O
Cas : 453562-69-1 Purity: >98 %
Cas : 453562-69-1 Storage: at 20℃ 2 years
Cas : 453562-69-1 Solubility: 10 mM in DMSO
Cas : 453562-69-1 Name: Motesanib
10mg/$50 In-stock
50mg/$160 In-stock
100mg/$280 In-stock
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453562-69-1  Data Sheet:
Introduction of 453562-69-1 :
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) [1] 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 [1]. Althouth displaying little antiproliferative activity on cell growth of HUVECs alone, Motesanib Diphosphate treatment significantly sensitizes the cells to fractionated radiation [2]. 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 [1]. Administration of Motesanib Diphosphate in combination with radiation displays significant anti-tumor activity in head and neck squamous cell carcinoma (HNSCC) xenograft models [2]. 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 [3].
References on 453562-69-1 :

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