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Lenvatinib mesylate

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Chemical Structure| 857890-39-2 同义名 : 乐伐替尼甲磺酸盐 ;E7080 mesylate;Lenvatinib (mesylate);E-7080
CAS号 : 857890-39-2
货号 : A283982
分子式 : C22H23ClN4O7S
纯度 : 99%
分子量 : 522.959
MDL号 : MFCD18633219
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(57.37 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • FGFR1

    FGFR1, IC50:46 nM
描述 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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.91mL

0.38mL

0.19mL

9.56mL

1.91mL

0.96mL

19.12mL

3.82mL

1.91mL
参考文献

[1]Kudo M, et al. Lenvatinib versus sorafenib in first-line treatment of patients with unresectable hepatocellularcarcinoma: a randomised phase 3 non-inferiority trial. Lancet. 2018 Mar 24;391(10126):1163-1173.

[2]Suyama K, et al. Lenvatinib: A Promising Molecular Targeted Agent for Multiple Cancers. Cancer Control. 2018 Jan-Dec;25(1):1073274818789361.

[3]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, 14(17),545.

[4]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, 122(3), 664-671.