产品简介：
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。
分子式：C22H23N5O 分子量：373.45
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
| 描述 | 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。 |
|---|---|
| IC50& Target |
VEGFR1
(Cell-free assay) 2 nM VEGFR2
(Cell-free assay) 3 nM VEGFR3
(Cell-free assay) 6 nM c-Kit
(Cell-free assay) 8 nM c-Kit
(Cell-free assay) 8 nM |
| 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. |
| 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 |
| 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 |
| 50 mM | 0.0536 mL | 0.2678 mL | 0.5355 mL |
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。
- 【注意】
- ●我司产品为非无菌包装，若用于细胞培养，请提前做预处理，除去热原细菌，否则会导致染菌。
●部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，以上数据仅供参考交流研究之用。
