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Lenvatinib

Lenvatinib

产品编号 T0520   CAS 417716-92-8
别名: 仑伐替尼, E7080

Lenvatinib (E7080) 是一种多靶点受体酪氨酸激酶抑制剂,抑制 VEGFR1-3、FGFR1-4、KIT、PDGFR 和 RET 等,具有口服活性。Lenvatinib 对 VEGFR2 和 VEGFR3 的抑制活性最强 (IC50=4/5.2 nM)。Lenvatinib 具有强效抗肿瘤活性。

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Lenvatinib Chemical Structure
Lenvatinib, CAS 417716-92-8
规格 价格/CNY 货期 数量
1 mg ¥ 313 现货
2 mg ¥ 433 现货
5 mg ¥ 535 现货
10 mg ¥ 859 现货
25 mg ¥ 1,550 现货
50 mg ¥ 2,570 现货
100 mg ¥ 3,280 现货
500 mg ¥ 5,430 现货
1 mL * 10 mM (in DMSO) ¥ 657 现货
其他形式的 Lenvatinib:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
Venetoclax限时半价
产品目录号及名称: Lenvatinib (T0520)
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纯度: 99.8000%
纯度: 98.57%
纯度: 98.46%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 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.
靶点活性 PDGFRβ:39 nM, VEGFR1/FLT1:22 nM, FGFR1:46 nM, VEGFR2/KDR:4.0 nM, VEGFR3/FLT4:5.2 nM
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]
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.
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)
别名 仑伐替尼, E7080
化合物与蛋白结合的复合物

T0520_2

FGFR-1 in complex with ligand lenvatinib

分子量 426.85
分子式 C21H19ClN4O4
CAS No. 417716-92-8

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 38 mg/mL (89 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3427 mL 11.7137 mL 23.4274 mL 58.5686 mL
5 mM 0.4685 mL 2.3427 mL 4.6855 mL 11.7137 mL
10 mM 0.2343 mL 1.1714 mL 2.3427 mL 5.8569 mL
20 mM 0.1171 mL 0.5857 mL 1.1714 mL 2.9284 mL
50 mM 0.0469 mL 0.2343 mL 0.4685 mL 1.1714 mL

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TargetMol Library Books参考文献

1. Glen H, et al. E7080, a multi-targeted tyrosine kinase inhibitor suppresses tumor cell migration and invasion. BMC Cancer. 2011 Jul 22;11:309. 2. Matsui J, et al. E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibition. Int J Cancer. 2008 Feb 1;122(3):664-71. 3. Matsui J, et al. Multi-kinase inhibitor E7080 suppresses lymph node and lung metastases of human mammary breast tumor MDA-MB-231 via inhibition of vascular endothelial growth factor-receptor (VEGF-R) 2 and VEGF-R3 kinase. Clin Cancer Res. 2008 Sep 1;14(17):5459-65.

TargetMol Library Books文献引用

1. Kui L, Kong Q, Yang X, et al. High-throughput in vitro gene expression profile to screen of natural herbals for Breast Cancer treatment. Frontiers in Oncology. 2021, 11. 2. Sun L, Wan A H, Yan S, et al.A multidimensional platform of patient-derived tumors identifies drug susceptibilities for clinical lenvatinib resistance.Acta Pharmaceutica Sinica B.2023
Golvatinib TIE-2/VEGFR-2 kinase-IN-5 TG 100572 Hydrochloride (Z)-FeCP-oxindole Ribociclib Sunitinib-d10 JK-P3 Vomifoliol

相关化合物库

该产品包含在如下化合物库中:
FDA 上市激酶抑制剂库 膜蛋白靶向化合物库 激酶抑制剂库 酪氨酸激酶分子库 抗癌活性化合物库 抗癌临床化合物库 抗癌上市药物库 抗癌药物库 抑制剂库 药物功能重定位化合物库

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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。

Keywords

Lenvatinib 417716-92-8 Angiogenesis Apoptosis Tyrosine Kinase/Adaptors c-Kit PDGFR VEGFR FGFR c-RET SCFR CD117 Platelet-derived growth factor receptor Fibroblast growth factor receptor 伦伐替尼 RET 仑伐替尼 inhibit E-7080 E 7080 Inhibitor E7080 Vascular endothelial growth factor receptor inhibitor

 

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