DC Chemicals · Product datasheet

LENVATINIB MESYLATE — Datasheet

CAT. NO. DC8488

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ParameterValue
Chemical NameLenvatinib mesylate
CAS No.857890-39-2
Synonyms6-Quinolinecarboxamide,4-[3-chloro-4-[[(cyclopropylamino)carbonyl]amino]phenoxy]-7-methoxy-,monomethanesulfonate;4-[3-chloro-4-(cyclopropylcarbamoylamino)phenoxy]-7-methoxyquinoline-6-carboxamide,methanesulfonic acid;lenvatinib Mesylate;4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide mesylate;4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide methanesulfonate;Lenvatinib mesilate (JAN);Lenvatinib mesylate [USAN];Lenvatinib mesilate;Lenvima;Lenvatinib (mesylate);3J78384F61;Lenvatinib mesylate (USAN);N-(4-((6-Carbamoyl-7-methoxyquinolin-4-yl)oxy)-2-chlorophenyl)-N'-cyclopropylurea monomethanesulfonate;lenvatinibMesylate;Lenvima (TN);E7080Mesylate;Lenvatinib methanesulfonate;E7080 MESYLATE;BCP11858;SB16581
FormulaC22H23ClN4O7S
M.Wt522.9586
SMILESClC1C([H])=C(C([H])=C([H])C=1N([H])C(N([H])C1([H])C([H])([H])C1([H])[H])=O)OC1C([H])=C([H])N=C2C([H])=C(C(C(N([H])[H])=O)=C([H])C=12)OC([H])([H])[H].S(C([H])([H])[H])(=O)(=O)O[H]
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

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].

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].

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

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