Lenvatinib

SKU: orb1310532

特色

描述

Lenvatinib (E7080) is an orally active multi-target tyrosine kinase inhibitor with potent activity against VEGFR2/3, FGFR1-4, RET, KIT, and PDGFR. It demonstrates robust anti-tumor effects in both in vitro assays and in vivo models, supporting its research use in oncology, particularly for studying angiogenesis and tumor proliferation pathways.

研究领域

Cardiovascular Research

图片与验证

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关键属性

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CAS 号	417716-92-8
MW	426.85
纯度	>98%
分子式	C₂₁H₁₉ClN₄O₄
SMILES	O(C=1C2=C(C=C(OC)C(C(N)=O)=C2)N=CC1)C3=CC(Cl)=C(NC(NC4CC4)=O)C=C3
靶点	Kinase
溶解性	Soluble in DMSO (up to 20 mg/ml)

生物活性

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靶点 IC50	VEGFR3/FLT4:5.2 nM\|c-Kit:100 nM\|VEGFR2/KDR:4.0 nM\|FGFR1:46 nM\|VEGFR1/FLT1:22 nM\|PDGFRβ:39 nM\|PDGFRα:51 nM
体内	METHODS: To assay antitumor activity in vivo, Lenvatinib (30-100 mg/kg in 0.5% methylcellulose) was orally administered twice daily for twenty-one days to BALB/c nude mice harboring human small cell lung cancer tumor H146. RESULTS: Oral administration of Lenvatinib inhibited the growth of H146 tumors in a dose-dependent manner and caused tumor regression at 100 mg/kg. METHODS: To test the antitumor activity in vivo, Lenvatinib (100 mg/kg) was orally administered once daily for eight weeks to nude mice harboring human mammary carcinoma tumor MDA-MB-231. RESULTS: Lenvatinib inhibited metastasis to regional lymph nodes and distant lungs in the MDA-MB-231 xenograft model.Lenvatinib decreased angiogenesis and lymphangiogenesis in established metastatic nodes of MDA-MB-231 tumors in lymph nodes.
体外	METHODS: Six human tumor cells, A375, DU145, DX3, KM12C, SK23, and U2OS, were treated with Lenvatinib (1-100 μM) for 72 h. Cell viability was measured by MTT. RESULTS: In most cell lines, Lenvatinib inhibited proliferation only at high concentrations (IC50 23.6-44.17 μM), while the IC50 in the KM12C cell line was 9.54 μM. METHODS: Human umbilical vein endothelial cells HUVECs were treated with Lenvatinib (0.16-20 nM) for 1 h, followed by stimulation with SCF or VEGF (20 ng/mL) for 5 min, and the expression levels of target proteins were detected by Western Blot. RESULTS: Ligand-induced phosphorylation of both KIT and KDR was inhibited by Lenvatinib.
细胞研究	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)

储存与操作

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储存	-20°C
有效期	12 months from date of receipt.
免责声明	For research use only

别名

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E7080

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质量保证

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化合物标识

PubChem CID

9823820 ↗

关键属性

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暂无计算属性。

实验方案信息

查看更多实验方案

CAS 号：	867365-40-0
MW:	652.27
分子式：	C₂₄H₁₇BrCl₂FN₃NaO₅S

CAS 号：	861877-12-5
MW:	470.50
分子式：	C₂₅H₁₈N₄O₄S

CAS 号：	417717-04-5
MW:	412.83
分子式：	C₂₀H₁₇ClN₄O₄

MW:	449.29
分子式：	C₂₀H₁₈Cl₂N₄O₄

Lenvatinib

描述

研究领域

图片与验证

关键属性

生物活性

储存与操作

别名

相似产品

Lenvatinib impurity 1 [orb3181301]

Elsulfavirine sodium [orb3210816]

VEGFR2-IN-84 [orb3211308]

O-Demethyl Lenvatinib hydrochloride [orb1983271]

O-Demethyl Lenvatinib [orb1983272]

质量保证

化合物标识

关键属性

实验方案信息

可选规格