Nintedanib esylate NEW
| Price | $36 | $52 | $65 |
| Package | 5mg | 10mg | 25mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-04 |
Product Details
| Product Name: Nintedanib esylate | CAS No.: 656247-18-6 |
| Purity: 99.96% | Supply Ability: 10g |
| Release date: 2024/11/04 |
Product Introduction
Bioactivity
| 名稱 | Nintedanib esylate |
| 描述 | Nintedanib esylate (BIBF 1120 esylate) is a potent triple angiokinase inhibitor targeting VEGFR1/2/3, FGFR1/2/3, and PDGFRα/β. |
| 激酶實驗 | 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 Each microtiter plate contains internal controls such as blank, maximum reaction, and historical reference compound.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. |
| 動物實驗 | 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. |
| 體外活性 | 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). |
| 體內活性 | BIBF1120, administered orally at doses ranging from 25-100 mg/kg daily, demonstrates high efficacy across various tumor models, including human tumor xenografts in nude mice and a syngeneic rat tumor model. Its effectiveness is confirmed through magnetic resonance imaging, which shows significant reductions in tumor perfusion, vessel density, and vessel integrity within 3 to 5 days, leading to substantial growth inhibition. Moreover, BIBF1120 is well-tolerated and exhibits promising results in in vivo tumor models, highlighting its potential as an effective oral therapeutic option. |
| 存儲條件 | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 45 mg/mL (69.26 mM), Sonication and heating are recommended. |
| 關鍵字 | 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 |
| 相關產(chǎn)品 | Amlexanox | Sorafenib | Ferulic Acid | Regorafenib | Formononetin | Pazopanib |
| 相關庫 | 經(jīng)典已知活性庫 | EMA 上市藥物庫 | 激酶抑制劑庫 | 抗癌臨床化合物庫 | 藥物功能重定位化合物庫 | 抑制劑庫 | 抗癌上市藥物庫 | FDA 上市激酶抑制劑庫 | 已知活性化合物庫 | 抗癌藥物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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