Lenvatinib mesylate (E7080 mesylate) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits vascular endothelial growth factor receptor 1-3, vascular endothelial growth factor receptor 1-4, epidermal growth factor receptor, KIT, and RET, showing potent antitumour activity[1][2].The IC50 of Lenvatinib mesylate against VEGFR2, VEGFR3, and VEGFR1 was 4, 5.2, and 22 nM, respectively.The IC50 of Lenvatinib mesylate for inhibition of PDGFRα, PDGFRβ, FGFR1, and KIT was 51, 39, 46, and 100 nM, respectively[3].
Lenvatinib mesylate/仑伐替尼甲酸盐 细胞实验
Cell Line
Concentration
Treated Time
Description
References
TPC-1
15 nM
To investigate the mechanism of resistance to Lenvatinib in TPC-1 cells, it was found that phosphorylation of EGFR, ERK, and Akt was enhanced.
Cancer Sci. 2022 Sep;113(9):3193-3210.
FRO
30 nM
To investigate the mechanism of resistance to Lenvatinib in FRO cells, it was found that phosphorylation of EGFR was enhanced, but downstream signal transduction molecules were not enhanced.
Cancer Sci. 2022 Sep;113(9):3193-3210.
SMMC-7721
10 μM
24 h
To evaluate the effect of lenvatinib on mitochondrial membrane potential in HCC cells, results showed a significant decrease in mitochondrial membrane potential
J Hematol Oncol. 2021 Jan 14;14(1):16.
HCCLM3
10 μM
24 h
To evaluate the effect of lenvatinib on mitochondrial membrane potential in HCC cells, results showed a significant decrease in mitochondrial membrane potential
J Hematol Oncol. 2021 Jan 14;14(1):16.
8505 C cells
2 µM
Evaluate the inhibitory effect of Lenvatinib combined with BRAF inhibitor PLX4720 on the proliferation of thyroid cancer cells
Cell Mol Life Sci. 2024 May 25;81(1):238.
BCPAP cells
2 µM
Evaluate the inhibitory effect of Lenvatinib combined with BRAF inhibitor PLX4720 on the proliferation of thyroid cancer cells
Cell Mol Life Sci. 2024 May 25;81(1):238.
HepG2 cells
80 µM
14 days
To evaluate the effect of Lenvatinib on HepG2 cells, results showed that DUSP4 knockout enhanced Lenvatinib resistance.
Int J Biol Sci. 2022 Jul 4;18(11):4357-4371.
Huh7 cells
20 µM
24 h
To evaluate the effect of Lenvatinib on Huh7 cells, results showed that DUSP4 knockout enhanced Lenvatinib resistance.
Int J Biol Sci. 2022 Jul 4;18(11):4357-4371.
Caki-1
10 μM
24 h
To analyze the global gene expression profile of the B7 family, B7-H4 gene was upregulated in Caki-1 and 786-O cells.
Cells. 2022 Apr 25;11(9):1448.
786-O
10 μM
24 h
To analyze the global gene expression profile of the B7 family, B7-H4 gene was upregulated in Caki-1 and 786-O cells.
Cells. 2022 Apr 25;11(9):1448.
A-498
10 μM
24 h
To analyze the global gene expression profile of the B7 family, B7-H4 gene was not consistently increased in A-498 cells.
Cells. 2022 Apr 25;11(9):1448.
Hep3B/CSQT-2 MUC15
2.5 μM
7 days
To evaluate the response of MUC15 overexpression to lenvatinib treatment, results showed that MUC15 overexpression enhanced sensitivity to lenvatinib.
Cell Death Dis. 2022 Mar 2;13(3):200.
Hep3B MUC15
10 μM
48 h
To evaluate the effect of MUC15 overexpression on lenvatinib-induced apoptosis, results showed that MUC15 overexpression enhanced sensitivity to lenvatinib.
Cell Death Dis. 2022 Mar 2;13(3):200.
HepG2
20 or 40 μM
48 h
To evaluate the effect of Lenvatinib on apoptosis and ROS levels in HepG2 cells, results showed that 20 μM Lenvatinib had limited effect on inducing apoptosis, but 40 μM significantly increased ROS levels.
J Adv Res. 2023 Feb;44:173-183.
Huh7
20 or 40 μM
48 h
To evaluate the effect of Lenvatinib on apoptosis and ROS levels in Huh7 cells, results showed that 20 and 40 μM Lenvatinib significantly induced apoptosis and increased ROS levels.
J Adv Res. 2023 Feb;44:173-183.
PLC/PRF5
20 or 40 μM
48 h
To evaluate the effect of Lenvatinib on apoptosis and ROS levels in PLC/PRF5 cells, results showed that 20 μM Lenvatinib had limited effect on inducing apoptosis, but 40 μM significantly increased ROS levels.
J Adv Res. 2023 Feb;44:173-183.
Hep3B
20 or 40 μM
48 h
To evaluate the effect of Lenvatinib on apoptosis and ROS levels in Hep3B cells, results showed that 20 and 40 μM Lenvatinib significantly induced apoptosis and increased ROS levels.
J Adv Res. 2023 Feb;44:173-183.
Lenvatinib mesylate/仑伐替尼甲酸盐 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
BALB/c-nu nude female mice
TPC-1/LR tumor xenograft model
Oral
6 mg/kg
Once daily for 9 days
To investigate the inhibitory effect of Lenvatinib combined with Lapatinib on TPC-1/LR tumors, it was found that the combination significantly inhibited tumor growth.
Cancer Sci. 2022 Sep;113(9):3193-3210.
Nude mice
HCCLM3 xenograft model
Intraperitoneal injection
5 mg/kg or 10 mg/kg
Once daily until the end of the experiment
To evaluate the inhibitory effect of lenvatinib alone or in combination with hydroxychloroquine on HCC growth and metastasis, results showed the best efficacy in the combination therapy group
J Hematol Oncol. 2021 Jan 14;14(1):16.
Nude mice
8505 C cell-derived xenograft model
Oral
25 mg/kg
Daily for 3 weeks
Evaluate the anti-tumor efficacy of Lenvatinib combined with BRAF inhibitor PLX4720 in thyroid cancer xenograft model
Cell Mol Life Sci. 2024 May 25;81(1):238.
Nude mice
Hepatocellular carcinoma xenograft model
Oral
30 mg/kg/d
Once daily for 4 weeks
To evaluate the effect of Lenvatinib on hepatocellular carcinoma xenograft model, results showed that DUSP4 knockout attenuated the anti-tumor effect of Lenvatinib.
Int J Biol Sci. 2022 Jul 4;18(11):4357-4371.
Mice
Hepa1-6 hepatoma orthotopic model
Oral
10 mg/kg
Once daily for two weeks
To evaluate the effect of Lenvatinib on tumor angiogenesis in a hepatocellular carcinoma model, results showed that Lenvatinib inhibited tumor angiogenesis.
iScience. 2024 Jan 4;27(2):108797
Mice
HCC cell line-derived xenograft models
Oral
4 mg/kg
Every 5 days
Knockdown of TBC1D31 significantly increases the sensitivity of HCCLM3 cells to lenvatinib
Adv Sci (Weinh). 2024 Oct;11(40):e2405459.
BALB/c nude mice
Huh7 xenograft tumor model
Oral
10 or 30 mg/kg
Once daily for two weeks
To evaluate the anti-tumor effect of Lenvatinib on Huh7 xenograft tumors, results showed that 10 and 30 mg/kg/d Lenvatinib significantly inhibited tumor growth.
J Adv Res. 2023 Feb;44:173-183.
Lenvatinib mesylate/仑伐替尼甲酸盐 动物研究
Animal study
Administered orally at a dose of 100 mg/kg, Lenvatinib mesylate in combination with bevacizumab significantly inhibited local tumour growth, and at the end of treatment, Lenvatinib mesylate also significantly inhibited metastasis to regional lymph nodes and distant lungs[3].In an H146 xenograft model, Lenvatinib mesylate inhibited H146 tumour growth in a dose-dependent manner at 30 mg/kg and 100 mg/kg doses (BID, QDx21), and led to tumour regression at 100 mg/kg dose. IHC analysis of the anti-CD31 antibody showed that the 100 mg/kg dose of Lenvatinib mesylate reduced microvessel density more than anti-vascular endothelial growth factor antibody and imatinib treatment[4].
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