1. Protein Tyrosine Kinase/RTK
  2. VEGFR
    FGFR
    PDGFR
    RET
    c-Kit
  3. Lenvatinib mesylate

Lenvatinib mesylate (Synonyms: E7080 mesylate)

Cat. No.: HY-10981A
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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.

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Lenvatinib mesylate Chemical Structure

Lenvatinib mesylate Chemical Structure

CAS No. : 857890-39-2

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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[1][2].

IC50 & Target[1][2][3]

VEGFR1

22 nM (IC50)

VEGFR2

4 nM (IC50)

VEGFR3

5.2 nM (IC50)

FGFR1

46 nM (IC50)

FGFR2

 

FGFR3

 

FGFR4

 

PDGFRα

51 nM (IC50)

PDGFRβ

39 nM (IC50)

c-Kit

100 nM (IC50)

RET

 

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[3].

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[3].
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[4].

Molecular Weight

522.96

Formula

C₂₂H₂₃ClN₄O₇S

CAS No.

857890-39-2

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

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Lenvatinib mesylate
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