Motesanib (AMG-706)
分子式：C22H23N5O分子量：373.45
简介：Motesanib (AMG-706)是一种具有口服生物活性的受体酪氨酸激酶 (receptor tyrosine kinase)抑制剂，对VEGFR1, VEGFR2, VEGFR3, Kit, PDGFR和Ret的IC50值分别为2、3、6、8、84和59 nM。
物理性状及指标：
外观：……………………粉末
溶解性：…………………H2O ：Insoluble；Ethanol：8 mg/mL (21.42 mM)；DMSO: 75 mg/mL (200.83 mM)
含量：……………………>98%
储存温度：-20℃，避光防潮密闭干燥
运输条件：2~8℃运输
生物活性
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描述
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Motesanib (AMG-706)是一种具有口服生物活性的受体酪氨酸激酶 (receptor tyrosine kinase)抑制剂，对VEGFR1, VEGFR2, VEGFR3, Kit, PDGFR和Ret的IC50值分别为2、3、6、8、84和59 nM。 |
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IC50& Target |
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体外 |
Motesanib has broad activity against the human VEGFR family, and displays > 1000 selectivity against EGFR, Src, and p38 kinase. Motesanib significantly inhibits VEGF-induced cellular proliferation of HUVECs with an IC50of 10 nM, while displaying little effect at bFGF-induced proliferation with an IC50of >3,000 nM. Motesanib also potently inhibits PDGF-induced proliferation and SCF-induced c-kit phosphorylation with IC50of 207 nM and 37 nM, respectively, but not effective against the EGF-induced EGFR phosphorylation and cell viability of A431 cellsAlthouth displaying little antiproliferative activity on cell growth of HUVECs alone, Motesanib treatment significantly sensitizes the cells to fractionated radiation. |
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体内 |
Motesanib (100 mg/kg) significantly inhibits VEGF-induced vascular permeability in a time-dependent manner. Oral administration of Motesanib twice daily or once daily potently inhibits, in a dose-dependent manner, VEGF-induced angiogenesis using the rat corneal model with ED50of 2.1 mg/kg and 4.9 mg/kg, respectively. Motesanib induces a dose-dependent tumor regression of established A431 xenografts by selectively targeting neovascularization in tumor cells. Motesanib in combination with radiation displays significant anti-tumor activity in head and neck squamous cell carcinoma (HNSCC) xenograft models.Motesanib 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 |
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储液配置及储存：按表中溶解性配置；如溶解困难，可以通过快速搅拌，超声或温和加热（在45-60°C下水浴）。液体稳定性报道的很少，建议现配现用，如需储存，建议：-20℃1-3月；-80℃ 3-6月。
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1 mg |
5 mg |
10 mg |
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1 mM |
2.6777 mL |
13.3887 mL |
26.7773 mL |
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5 mM |
0.5355 mL |
2.6777 mL |
5.3555 mL |
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10 mM |
0.2678 mL |
1.3389 mL |
2.6777 mL |
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50 mM |
0.0536 mL |
0.2678 mL |
0.5355 mL |
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