Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Motesanib (AMG 706) 是有效的、ATP 竞争性的 VEGFR1/2/3 的抑制剂,其IC50值为 2 nM/3 nM/6 nM,与对 Kit 的选择性相似,是 PDGFR 和 Ret 的 10 倍多。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 198 | 现货 | ||
5 mg | ¥ 446 | 现货 | ||
10 mg | ¥ 538 | 现货 | ||
25 mg | ¥ 863 | 现货 | ||
50 mg | ¥ 1,230 | 现货 | ||
100 mg | ¥ 1,730 | 现货 | ||
500 mg | ¥ 4,260 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 496 | 现货 |
产品描述 | Motesanib (AMG 706) is an orally bioavailable receptor tyrosine kinase inhibitor with potential antineoplastic activity. AMG 706 selectively targets and inhibits vascular endothelial growth factor (VEGFR), platelet-derived growth factor (PDGFR), Kit, and Ret receptors, thereby inhibiting angiogenesis and cellular proliferation. |
靶点活性 | c-Kit:8 nM, VEGFR1:2 nM, VEGFR3:6 nM, VEGFR2:3 nM |
体外活性 | Motesanib has broad activity against the human VEGFR family that displays > 1000 selectivity against EGFR, Src, and p38 kinase. Motesanib 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 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 treatment significantly sensitizes the cells to fractionated radiation[2]. |
体内活性 | Motesanib (100 mg/kg) markedly 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 ED50 of 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[1]. Motesanib in combination with radiation displays significant anti-tumor activity in head and neck squamous cell carcinoma (HNSCC) xenograft models[2]. 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[3]. |
激酶实验 | Optimal enzyme, ATP, and substrate (gastrin peptide) concentrations are established for each enzyme using homogeneous time-resolved fluorescence (HTRF) assays. Motesanib is tested in a 10-point dose-response curve for each enzyme using an ATP concentration of two-thirds Km?for each. Most assays consist of enzyme mixed with kinase reaction buffer [20 mM Tris-HCl (pH 7.5), 10 mM MgCl2, 5 mM MnCl2, 100 mM NaCl, 1.5 mM EGTA]. A final concentration of 1 mM DTT, 0.2 mM NaVO4, and 20 μg/mL BSA is added before each assay. For all assays, 5.75 mg/mL streptavidin-allophycocyanin and 0.1125 nM Eu-PT66 are added immediately before the HTRF reaction. Plates are incubated for 30 minutes at room temperature and read on a Discovery instrument. IC50 values are calculated using the Levenberg-Marquardt algorithm into a four-parameter logistic equation. |
细胞实验 | Cells are preincubated for 2 hours with different concentrations of Motesanib, and exposed with 50 ng/mL VEGF or 20 ng/mL bFGF for an additional 72 hours. Cells are washed twice with DPBS, and plates are frozen at -70°C for 24 hours. Proliferation is assessed by the addition of CyQuant dye, and plates are read on a Victor 1420 workstation. IC50 data are calculated using the Levenberg-Marquardt algorithm into a four-parameter logistic equatio. |
别名 | AMG 706, 莫特塞尼, 莫替沙尼 |
分子量 | 373.45 |
分子式 | C22H23N5O |
CAS No. | 453562-69-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mM
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.6777 mL | 13.3887 mL | 26.7773 mL | 66.9434 mL |
5 mM | 0.5355 mL | 2.6777 mL | 5.3555 mL | 13.3887 mL | |
10 mM | 0.2678 mL | 1.3389 mL | 2.6777 mL | 6.6943 mL | |
20 mM | 0.1339 mL | 0.6694 mL | 1.3389 mL | 3.3472 mL | |
50 mM | 0.0536 mL | 0.2678 mL | 0.5355 mL | 1.3389 mL | |
100 mM | 0.0268 mL | 0.1339 mL | 0.2678 mL | 0.6694 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Motesanib 453562-69-1 Angiogenesis Tyrosine Kinase/Adaptors VEGFR c-Kit inhibit AMG-706 SCFR AMG 706 莫特塞尼 Vascular endothelial growth factor receptor CD117 莫替沙尼 AMG706 Inhibitor inhibitor