Lenvatinib mesylate

SKU: orb1220195

Description

Lenvatinib mesylate (E7080 mesylate), an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 857890-39-2
• MW: 522.96
• Purity: >98% (HPLC)
• Formula: C??H??ClN?O?S
• SMILES: O=C(C1=C(OC)C=C2N=CC=C(OC3=CC=C(NC(NC4CC4)=O)C(Cl)=C3)C2=C1)N.OS(=O)(C)=O
• Target: VEGFR
• Solubility: DMSO : 7.35 mg/mL (14.05 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  Lenvatinib mesylate (E7080 mesylate) (100 mg/kg, p.o.) is administeredand bevacizumab 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 mesylate (E7080 mesylate) 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 imatinib treatment.
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• In Vitro:
  Lenvatinib mesylate (E7080 mesylate) 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, 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 mesylate

Quick Database Links

Gene Symbol

VEGFR