二磷酸莫替沙尼 T2288L
面议
- TargetMol
- 生产商
- 进口
- 美国
- 现货
- 全国
- 8
- 1
Product IntroductionBioactivity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
AI问答
配套的仪器设备？
可以搭配的相关耗材试剂？
耗材描述
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
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
猜你喜欢
感兴趣产品