乙磺酸尼达尼布 T5001
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 |
---|---|---|---|
25 mg | 656247-18-6 | ¥659.00 | 询底价 |
100 mg | 656247-18-6 | ¥1,430.00 | 询底价 |
50 mg | 656247-18-6 | ¥969.00 | 询底价 |
200 mg | 656247-18-6 | ¥2,130.00 | 询底价 |
1 mL | 656247-18-6 | ¥398.00 | 询底价 |
5 mg | 656247-18-6 | ¥279.00 | 询底价 |
10 mg | 656247-18-6 | ¥393.00 | 询底价 |
500 mg | 656247-18-6 | ¥3,580.00 | 询底价 |
Product Introduction
Bioactivity
英文名: Nintedanib esylate
描述: 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)。
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 Each microtiter plate contains internal controls such as blank, maximum reaction, and historical reference compound.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.
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.
存储条件: keep away from direct sunlightPowder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 45 mg/mL (69.26 mM)
关键字: inhibit | Platelet-derived growth factor receptor | Nintedanib | VEGFR | BIBF1120 | Fibroblast growth factor receptor | PDGFR | FGFR | BIBF-1120 | esylate | Vascular endothelial growth factor receptor | Inhibitor | Nintedanib esylate
相关产品: SCR-1481B1 | Toceranib Phosphate | hCA/VEGFR-2-IN-2 | Gandotinib | Regorafenib Hydrochloride | Myricanol | Tyrphostin A9 | SU14813 maleate | TAK-593 | Xanthatin
相关库: Drug Repurposing Compound Library | FDA-Approved Kinase Inhibitor Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | Anti-Cancer Active Compound Library | Tyrosine Kinase Inhibitor Library | EMA Approved Drug Library
乙磺酸尼达尼布 T5001信息由TargetMol中国为您提供,如您想了解更多关于乙磺酸尼达尼布 T5001报价、型号、参数等信息,欢迎来电或留言咨询。
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