二磷酸莫替沙尼 T2288L

Product Introduction
Bioactivity


英文名: Motesanib Diphosphate

描述: Motesanib Diphosphate (AMG 706) 是一种有效的VEGFR1/2/3的 ATP 竞争性抑制剂，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 Diphosphate, 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(Only for Reference)

激酶实验: In vitro kinase assays: Optimal enzyme, ATP, and substrate (gastrin peptide) concentrations are established for each enzyme using homogeneous time-resolved fluorescence (HTRF) assays. Motesanib Diphosphate 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: 在大鼠角膜模型中,每天口服两次（ED50=2.1 mg/kg ）或一次（ED50=4.9 mg/kg ）Motesanib Diphosphate能够抑制血管内皮生长因子诱导的血管生成.在头部和颈部鳞状细胞癌移植瘤模型中,Motesanib Diphosphate和辐射治疗联用,显示出显著地抗癌活性.

体内活性: 在VEGF诱导的HUVECs细胞中（IC50 =10 nM）,Motesanib Diphosphate 明显抑制细胞增殖。对于血小板衍生因子诱导的增殖（IC50=207 nM）和SCF诱导的c-kit磷酸化（IC50=37 nM）,Motesanib Diphosphate能够显著抑制。人脐静脉内皮细胞,Motesanib Diphosphate增强细胞对于放射性的敏感程度。对人VEGFR家族,Motesanib Diphosphate具有广谱活性。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : 16 mg/mL (28.1 mM)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 93 mg/mL (163.3 mM)


关键字: c-Kit | AMG-706 | inhibit | AMG 706 Diphosphate | Vascular endothelial growth factor receptor | AMG706 | SCFR | Inhibitor | VEGFR | CD117 | Motesanib Diphosphate

相关产品: VEGFR-2/c-Met-IN-1 | FGFR1/VEGFR2-IN-1 | Pamufetinib | SU5208 | (Rac)-SAR131675 | BMS-605541 | Regorafénib N-oxyde (M2) | SAR131675 | Golvatinib | Takeda-6d

相关库: Drug Repurposing Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Anti-Ovarian Cancer Compound Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Active Compound Library | Tyrosine Kinase Inhibitor Library | Anti-Pancreatic Cancer 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