Lenvatinib
作者：齊岳
發(fā)布時間：2023-08-29
13:38:52
點擊數(shù)：
產(chǎn)品名稱：Lenvatinib
產(chǎn)品描述：
| 產(chǎn)品描述 | Lenvatinib is a Kinase Inhibitor. The mechanism of action of lenvatinib is as a Receptor Tyrosine Kinase Inhibitor. | ||||||||||||||||
| 靶點活性 | PDGFRβ:39 nM, VEGFR1/FLT1:22 nM, FGFR1:46 nM, VEGFR2/KDR:4.0 nM, VEGFR3/FLT4:5.2 nM | ||||||||||||||||
| 體外活性 | 與血管內(nèi)皮生長因子抗體和伊馬替尼處理相比,100 mg/kg E7080處理降低微脈管密度效果更好.用30和100 mg/kg E7080口服給藥處理H146 移植瘤模型,可以劑量依賴性抑制H146腫瘤生長,100 mg/kg時導(dǎo)致腫瘤退化
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| 體內(nèi)活性 | 體外受體酪氨酸和絲/蘇氨酸激酶實驗中,E7080抑制Flt-1,KDR和Flt-4,IC50分別為22,4.0和5.2 nM。最新研究顯示,1 μM和10 μM E7080通過抑制FGFR和PDGFR信號通路明顯抑制細(xì)胞遷移和入侵。E7080有效抑制血管生成,也明顯抑制VEGF/KDR和SCF/KIT信號通路。E7080也抑制FGFR1和PDGFR酪氨酸激酶,作用于FGFR1,PDGFRα和PDGFRβ時,IC50分別為46,51和100 nM。E7080分別作用于由血管內(nèi)皮生長因子和血管內(nèi)皮生長因子-C刺激的HUVECs,有效抑制VEGFR2和VEGFR3磷酸化,IC50分別為0.83 nM和0.36 nM。
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| 激酶實驗 | 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. | ||||||||||||||||
| 細(xì)胞實驗 | 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) |
| 別名 | 侖伐替尼, E7080 |
| 化合物與蛋白結(jié)合的復(fù)合物 |
FGFR-1 in complex with ligand lenvatinib |
| 分子量 | 426.86 |
| 分子式 | C21H19ClN4O4 |
| CAS No. | 417716-92-8 |
存儲
| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 38 mg/mL (89 mM)
Ethanol: <1 mg/mL
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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