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Cat. No. Name Size Price Add Cart
KI3395E7080 (Lenvatinib)QuoteQuote

Chemical Characteristic

Product NameE7080 (Lenvatinib)
SynonymsLenvatinib
CAS No.417716-92-8
Molecular Weight 426.85
FormulaC21H19ClN4O4
Chemical Name4-[3-chloro-4-(cyclopropylcarbamoylamino)phenoxy]-7-methoxyquinoline-6-carboxamide
Smilesn1ccc(c2cc(c(cc12)OC)C(=O)N)Oc1cc(c(cc1)NC(=O)NC1CC1)Cl
Chemical Structure

Biological activities

E7080 is an orally active inhibitor of multiple receptor tyrosine kinases, mostly for VEGFR2 (KDR)/VEGFR3 (Flt-4). E7080 inhibits VEGFR-2 and VEGFR-3 with IC50s of 4 and 5.2 nM, respectively.[1] E7080 inhibits KIT with an IC50 of 0.27 µM.[2] E7080 also has activity against VEGFR-1, FGFR-1, and PDGFRa/b tyrosine kinases, fibroblast growth factor receptor (FGFR) and platelet derived growth factor receptor (PDGFR). E7080 inhibits human cell lines DU145, DX3, KM12C and U2OS proliferation with IC50s of 23.62, 33.95, 9.54, 34.82 µM, respectively.[1] E7080 also has anti-tumor efficacy via inhibiting KIT signaling in small lung cancer cells. E7080 inhibits stem cell factor (SCF)-stimulated cell proliferation with an IC50 of 10 nM in KIT-expressing SCLC cell line (NCI-H526).[2] Besides, E7080 inhibits SCF-driven tube formation of human umbilical vein endothelial cell (HUVEC), which expresses KIT at the IC50 value of 5.2 nM.[3] E7080 shows anti-tumor activity in human cancer cell xenografts by inhibiting both tumor cell migration and invasion.[1] In vivo in nude mice, oral administration of E7080 inhibits tumor growth of H146 cells at doses of 30 and 100 mg/kg in a dose-dependent manner and causes tumor regression at 100 mg/kg.[3]

Protocols

In vitro, E7080 is prepared as a 10 mM stock in DMSO and diluted in culture media.[1]

References

[1] Glen H, et al. E7080, a multi-targeted tyrosine kinase inhibitor suppresses tumor cell migration and invasion. BMC Cancer. 2011, 11: 309.
[2] Yamamoto Y, et al. E7080, an oral multitargeted tyrosine kinase inhibitor, has direct anti-tumor efficacy via inhibition of KIT signaling in small cell lung cancer.
[3]MatsuiJ,etal.E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibition.Int J Cancer.2008,122(3): 664-671.

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