Lenvatinib

SKU: orb1225086

Description

Lenvatinib (E7080) is a multitargeted kinase inhibitor with IC50s of 4/5.2/22/46 nM for VEGFR2/VEGFR3/VEGFR1/FGFR1 in cell free assays; also inhibits PDGFR, Kit with IC50< 100 nM; suppresses the phosphorylation of VEGF receptor-2 and FGF receptor 1 and inhibits proliferation of endothelial cellin vitro; orally active.Kidney Cancer Approved(In Vitro):Lenvatinib (E7080) has IC50s of 4, 5.2, 22 nM for VEGFR2 (KDR), VEGFR3 (Flt-4), and VEGFR1 (Flt-1), respectively. Lenvatinib inhibits PDGFRα, PDGFRβ, FGFR1, and KIT with IC50s of 51, 39, 46, and 100 nM, respectively.(In Vivo):Lenvatinib (E7080) (100 mg/kg, p.o.) significantly inhibits local tumor growth at the m.f.p., and at the end of treatment, Lenvatinib mesylate also significantly inhibits metastasis to both regional lymph nodes and distant lung.Lenvatinib (E7080) inhibits the growth of H146 tumor at 30 and 100 mg/kg (BID, QDx21) in a dose-dependent manner and causes tumor regression at 100 mg/kg in H146 xenograft model. IHC analysis with anti-CD31 antibody shows that lenvatinib at 100 mg/kg decreases microvessel density more than anti-VEGF antibody and STI571 treatment.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 417716-92-8
• MW: 426.853
• Purity: >98% (HPLC)
• Formula: C₂₁H₁₉ClN₄O₄
• SMILES: COC1=CC2=NC=CC(OC3=CC(Cl)=C(NC(=O)NC4CC4)C=C3)=C2C=C1C(N)=O
• Target: VEGFR
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  Lenvatinib (E7080) (100 mg/kg, p.o.) significantly inhibits local tumor growth at the m. f. p. , and at the end of treatment, Lenvatinib mesylate also significantly inhibits metastasis to both regional lymph nodes and distant lung. Lenvatinib (E7080) inhibits the growth of H146 tumor at 30 and 100 mg/kg (BID, QDx21) in a dose-dependent manner and causes tumor regression at 100 mg/kg in H146 xenograft model. IHC analysis with anti-CD31 antibody shows that lenvatinib at 100 mg/kg decreases microvessel density more than anti-VEGF antibody and STI571 treatment.
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• In Vitro:
  Lenvatinib (E7080) has IC50s of 4, 5.2, 22 nM for VEGFR2 (KDR), VEGFR3 (Flt-4), and VEGFR1 (Flt-1), respectively. Lenvatinib inhibits PDGFRα, PDGFRβ, FGFR1, and KIT with IC50s of 51, 39, 46, and 100 nM, respectively.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

E7080 | E-7080 | E 7080

Quick Database Links

Gene Symbol

VEGFR