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  • 仑伐替尼|T0520

仑伐替尼|T0520

Lenvatinib
417716-92-8
313 1mg 起订
433 2mg 起订
535 5mg 起订
上海 更新日期:2024-12-02

TargetMol中国(陶术生物)

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邮箱:marketing@targetmol.com

产品详情:

中文名称:
仑伐替尼
英文名称:
Lenvatinib
CAS号:
417716-92-8
品牌:
TargetMol
产地:
美国
保存条件:
store at low temperature | Powder: -20°C for 3 years | Shipping with blue ice.
纯度规格:
99.8000%
产品类别:
抑制剂
货号:
T0520

Product Introduction

Bioactivity

名称Lenvatinib
描述Lenvatinib (E7080) is a multi-target receptor tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, KIT, PDGFR, and RET, and has oral activity. Lenvatinib has the strongest inhibitory activity on VEGFR2 and VEGFR3 (IC50=4/5.2 nM). Lenvatinib has strong anti-tumor activity.
细胞实验HUVECs (1,000 cells in each well in serum-free medium containing 2% fetal bovine serum) and L6 rat skeletal muscle myoblasts (5,000 cells in each well in serum-free DMEM) are dispensed in a 96-well plate and incubated overnight. E7080 and either VEGF (20 ng/mL) or FGF-2 (20 ng/mL) containing 2% fetal bovine serum and PDGFβ (40 ng/mL) are added to each well. Cells are incubated for 3 days and then the ratios of surviving cells are measured by WST-1 reagent. For proliferation assay, samples are duplicated and three separate experiments are done. (Only for Reference)
激酶实验In vitro kinase assay [1]: Tyrosine kinase assays are performed by HTRF (KDR, VEGFR1, FGFR1, c-Met, EGFR) and ELISA (PDGFRβ), using the recombinant kinase domains of receptors. In both assays, 4 μL of serial dilutions of E7080 are mixed in a 96-well round plate with 10 μL of enzyme, 16 μL of poly (GT) solution (250 ng) and 10 μL of ATP solution (1 μM ATP) (final concentration of DMSO is 0.1%). In wells for blanks, no enzyme is added. In control wells no test article is added. The kinase reaction is initiated by adding ATP solution to each well. After 30-minute incubation at 30°C, the reaction is stopped by adding 0.5 M EDTA (10 μL/well) to the reaction mixture in each well. Dilution buffer adequate to each kinase assay is added to the reaction mixture. In the HTRF assay, 50 μL of the reaction mixture is transferred to a 96-well 1/2 area black EIA/RIA plate, HTRF solution (50 μL/well) is added to the reaction mixture, and then kinase activity is determined by measurement of fluorescence with a time-resolved fluorescence detector at an excitation wavelength of 337 nm and an emission wavelengths of 620 and 665 nm. In the ELISA, 50 μL of the reaction mixture is incubated in avidin coated 96-well polystyrene plates at room temperature for 30 minutes. After washing with wash buffer, PY20-HRP solution (70 μL/well) is added and the reaction mixture is incubated at room temperature for 30 minutes. After washing with wash buffer, TMB reagent (100 μL/well) is added to each well. After several minutes (10–30 minutes), 1 M H3PO4 (100 μL/well) is added to each well. Kinase activity is determined by measurement of absorbance at 450 nm with a microplate reader.
体外活性方法:六种人肿瘤细胞 A375、DU145、DX3、KM12C、SK23 和 U2OS 用 Lenvatinib (1-100 μM) 处理 72 h,使用 MTT 检测细胞活力。 结果:大多数细胞系中,Lenvatinib 仅在高浓度下抑制增殖 (IC50 为 23.6-44.17 μM),而 KM12C 细胞系中的 IC50 为 9.54 μM。[1] 方法:人脐静脉内皮细胞 HUVECs 用 Lenvatinib (0.16-20 nM) 处理 1 h,随后用 SCF 或 VEGF (20 ng/mL) 刺激 5 min,使用 Western Blot 方法检测靶点蛋白表达水平。 结果:配体诱导的 KIT 和 KDR 的磷酸化均被 Lenvatinib 抑制。[2]
体内活性方法:为检测体内抗肿瘤活性,将 Lenvatinib (30-100 mg/kg in 0.5% methylcellulose) 口服给药给携带人小细胞肺癌肿瘤 H146 的 BALB/c nude 小鼠,每天两次,持续二十一天。 结果:口服 Lenvatinib 以剂量依赖性方式抑制 H146 肿瘤的生长,并在 100 mg/kg 时引起肿瘤消退。[2] 方法:为检测体内抗肿瘤活性,将 Lenvatinib (100 mg/kg) 口服给药给携带人乳腺癌肿瘤 MDA-MB-231 的 nude 小鼠,每天一次,持续八周。 结果:Lenvatinib 在 MDA-MB-231 异种移植物模型中抑制向区域淋巴结和远处肺的转移。Lenvatinib 降低了淋巴结中 MDA-MB-231 肿瘤的已建立转移结节的血管生成和淋巴管生成。[3]
存储条件store at low temperature | Powder: -20°C for 3 years | Shipping with blue ice.
溶解度DMSO : 15 mg/mL (35.14 mM), Sonication is recommended.(The compound is unstable in solution, please use soon.)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1.9 mg/mL (4.45 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
关键字SCFR | PDGFR | CD117 | Platelet-derived growth factor receptor | Fibroblast growth factor receptor | 伦伐替尼 | RET | Lenvatinib | inhibit | c-Kit | E-7080 | VEGFR | E 7080 | FGFR | Inhibitor | Vascular endothelial growth factor receptor | 伦伐替尼 | 伦伐替尼
相关产品Imatinib | Amlexanox | Gilteritinib | Ribociclib | Formononetin | Axitinib | Ferulic Acid | Regorafenib | Pazopanib | Nintedanib | Sorafenib | Regorafenib monohydrate
相关库经典已知活性库 | 抗癌活性化合物库 | 抗癌上市药物库 | 已知活性化合物库 | EMA 上市药物库 | 激酶抑制剂库 | FDA 上市药物库 | 膜蛋白靶向化合物库 | FDA 上市激酶抑制剂库 | 药物功能重定位化合物库 | 酪氨酸激酶分子库 | 抗癌临床化合物库
仑伐替尼|||E7080|TargetMol

公司简介

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起,为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部,化学事业部,生物事业部和新材料部。 从虚拟筛选到实体化合物分子供应;从商业化产品销售到个性化定制合成;从对明确靶点的分子筛选到对明确分子的多靶点筛选,从高通量筛选到化学结构优化,我们都可以满足您的科研用品及技术服务的需求。 经过在中国市场五年的精心耕耘,我们已成为筛选化合物领域优秀的供应商,为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期 (12年)
注册资本 566.2651万人民币
员工人数 100-500人
年营业额 ¥ 1亿以上
经营模式 贸易,试剂,定制,服务
主营行业 化学试剂,生物活性小分子

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