Lenvatinib

SKU: orb1310532

Description

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.

Research Area

Cardiovascular Research

Key Properties

• CAS Number: 417716-92-8
• MW: 426.85
• Purity: >98%
• Formula: 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
• Target: Kinase
• Solubility: Soluble in DMSO (up to 20 mg/ml)

Bioactivity

• Target 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
• In Vivo:
  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.
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• In Vitro:
  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.
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• Cell Research:
  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)
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

E7080

Compound Identifiers

PubChem CID

9823820