keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Nintedanib esylate (BIBF 1120 esylate) 是一种有效的三重血管激酶抑制剂,能够抑制 VEGFR1 (IC50:34 nM)、VEGFR2 (IC50:13 nM)、VEGFR3 (IC50:13 nM),FGFR1 (IC50:69 nM)、FGFR2 (IC50:37 nM)、FGFR3 (IC50:108 nM),PDGFRα (IC50:59 nM)、PDGFRβ (IC50:65 nM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 279 | 现货 | ||
10 mg | ¥ 393 | 现货 | ||
25 mg | ¥ 659 | 现货 | ||
50 mg | ¥ 969 | 现货 | ||
100 mg | ¥ 1,430 | 现货 | ||
200 mg | ¥ 2,130 | 现货 | ||
500 mg | ¥ 3,580 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 398 | 现货 |
产品描述 | Nintedanib esylate (BIBF 1120 esylate) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β |
靶点活性 | PDGFRβ:65 nM, PDGFRα:59 nM, FGFR3:108 nM, FGFR1:69 nM, FGFR2:37 nM, VEGFR1:34 nM, VEGFR3:13 nM, VEGFR2:13 nM |
体外活性 | BIBF 1120 binds to the ATP-binding site in the cleft between the amino and carboxy terminal lobes of the kinase domain. BIBF 1120 inhibits proliferation of PDGF-BB stimulated BRPs with EC50 of 79 nM in cell assays. BIBF1120 (100 nM) blocks activation of MAPK after stimulation with 5% serum plus PDGF-BB. BIBF1120 prevents PDGF-BB stimulated proliferation with an EC50 of 69 nM in cultures of human vascular smooth muscle cells (HUASMC). |
体内活性 | BIBF1120 (25-100 mg/kg daily p.o.) is highly active in all tumor models, including human tumor xenografts growing in nude mice and a syngeneic rat tumor model. This is evident in the magnetic resonance imaging of tumor perfusion after 3 days, reducing vessel density and vessel integrity after 5 days, and profound growth inhibition. BIBF1120 is orally available and displays encouraging efficacy in in vivo tumor models while being well tolerated. |
激酶实验 | Enzyme activity is assayed in the presence or absence of serial dilutions of BIBF1120 performed in 25% DMSO. Each microtiter plate contains internal controls such as blank, maximum reaction, and historical reference compound. All incubations are conducted at room temperature on a rotation shaker. 10 μL of each BIBF1120 dilution is added to 10 μL of diluted kinase (0.8 μg/mL VEGFR2, 10 mM Tris pH 7.5, 2 mM EDTA, and 2 mg/mL BSA) and preincubated for 1 hour. The reaction is started by addition of 30 μL of substrate mix containing 62.4 mM Tris pH 7.5, 2.7 mM DTT, 5.3 mM MnCl2, 13.3 mM Mg-acetate, 0.42 mM ATP, 0.83 mg/mL Poly-Glu-Tyr(4:1), and 1.7 μg/mL Poly-Glu-Tyr(4:1)-biotin and incubated for 1 hour. The reaction is stopped by addition of 50 μL of 250 mM EDTA, 20 mM HEPES, pH 7.4. 90 μL of the reaction mix is transferred to a streptavidin plate and incubated for 1-2 hours. After three washes with PBS the EU-labeled antibody, PY20 is added (recommended dilution 1:2000 of 0.5 mg/mL labeled antibody in DELFIA assay buffer). Excessive detection antibody is removed by three ishes of DELFIA washing buffer. Then 10 minutes before measurement on the multilabel reader, each well is incubated with 100 μL of DELFIA enhancement solution. |
动物实验 | Five-week-old to 6-wk-old athymic NMRI-nu/nu female mice (21-31 g) are used for the assay. After acclimatization, mice are inoculated with 1 to 5×106 (in 100 μL) FaDu, Caki-1, SKOV-3, H460, HT-29, or PAC-120 cells s.c. into the right flank of the animal. After acclimatization, F344 Fischer rats are injected with 5×106 (in 100 μL) GS-9L cells s.c. into the right flank of the animal. For pharmacokinetic analysis, blood is isolated at indicated time points from the retroorbital plexus of mice and plasma is analyzed using high performance liquid chromatography-mass spectrometry methodology. |
别名 | Intedanib, 乙磺酸尼达尼布, BIBF 1120 (esylate), 尼达尼布乙磺酸盐, Nintedanib Ethanesulfonate Salt, BIBF 1120 |
分子量 | 649.76 |
分子式 | C31H33N5O4.C2H6O3S |
CAS No. | 656247-18-6 |
keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 92.85 mg/mL (142.90 mM), Sonification and heating are recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.539 mL | 7.6951 mL | 15.3903 mL | 38.4757 mL |
5 mM | 0.3078 mL | 1.539 mL | 3.0781 mL | 7.6951 mL | |
10 mM | 0.1539 mL | 0.7695 mL | 1.539 mL | 3.8476 mL | |
20 mM | 0.077 mL | 0.3848 mL | 0.7695 mL | 1.9238 mL | |
50 mM | 0.0308 mL | 0.1539 mL | 0.3078 mL | 0.7695 mL | |
100 mM | 0.0154 mL | 0.077 mL | 0.1539 mL | 0.3848 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。
Nintedanib esylate 656247-18-6 Angiogenesis Tyrosine Kinase/Adaptors VEGFR FGFR PDGFR inhibit Platelet-derived growth factor receptor Nintedanib Intedanib BIBF1120 Fibroblast growth factor receptor 乙磺酸尼达尼布 BIBF-1120 BIBF 1120 (esylate) esylate 尼达尼布乙磺酸盐 Vascular endothelial growth factor receptor Inhibitor Nintedanib Ethanesulfonate Salt BIBF 1120 inhibitor