莫替沙尼 T2288
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
1 mg | 453562-69-1 | ¥198.00 | 询底价 |
500 mg | 453562-69-1 | ¥4,260.00 | 询底价 |
10 mg | 453562-69-1 | ¥538.00 | 询底价 |
25 mg | 453562-69-1 | ¥863.00 | 询底价 |
1 mL | 453562-69-1 | ¥496.00 | 询底价 |
50 mg | 453562-69-1 | ¥1,230.00 | 询底价 |
5 mg | 453562-69-1 | ¥446.00 | 询底价 |
100 mg | 453562-69-1 | ¥1,730.00 | 询底价 |
Product Introduction
Bioactivity
英文名: Motesanib
描述: 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。
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.
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.
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].
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 50 mg/mL (133.88 mM)
关键字: c-Kit | VEGFR | Motesanib | inhibit | AMG-706 | SCFR | Vascular endothelial growth factor receptor | CD117 | AMG706 | Inhibitor
相关产品: JNJ-38158471 | WAY-600 | Regorafenib | NVP-ACC789 | (Z)-Semaxinib | Penduletin | AMPK-IN-3 | AG 1406 | Vomifoliol | VEGFR-2-IN-6
相关库: Drug Repurposing Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Anti-Lung Cancer Compound Library | Inhibitor Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Active Compound Library | Reprogramming Compound Library
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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途