Cat. No. Name Size Price Add Cart
KI2658E-705010 mg$592
E-705020 mg$946
E-705050 mg$1712
E-7050100 mg$2738
E-7050200 mg$3952

Chemical Characteristic

Product NameE-7050
CAS No.928037-13-2
Molecular Weight 633.69
FormulaC33H37F2N7O4
Chemical Name1-N'-[2-fluoro-4-[2-[[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]amino]pyridin-4-yl]oxyphenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
SmilesC1(CC1)(C(=O)Nc1c(cc(cc1)Oc1cc(ncc1)NC(=O)N1CCC(CC1)N1CCN(CC1)C)F)C(=O)Nc1ccc(cc1)F
Chemical Structure

Biological activities

E-7050 is novel small molecule inhibitor of the c-Met and VEGFR-2 tyrosine kinases. E-7050 inhibits phosphorylation of both c-Met and VEGFR-2 with IC50s of 14 and 16 nM, respectively.[1] In vitro, E-7050 overcomes HGF-induced EGFR-TKI resistance in EGFR mutant lung cancer cell lines through the inhibition of the Met/Gab1/P13K/Akt pathway.[2] In vivo, E-7050 shows strong inhibition of tumor growth and tumor angiogenesis in xenograft models. Furthermore, in a peritoneal dissemination model, E-7050 shows antitumor effects against peritoneal tumors as well as a significant prolongation of lifespan in treated mice.[1]

Protocols

In vitro, E-7050 is dissolved in DMSO.[1]

References

[1] Nakagawa T, et al. E7050: a dual c-Met and VEGFR-2 tyrosine kinase inhibitor promotes tumor regression and prolongs survival in mouse xenograft models. Cancer Sci. 2010, 101 (1): 210-215.
[2] Tartarone A, et al. Mechanisms of resistance to EGFR tyrosine kinase inhibitors gefitinib/erlotinib and to ALK inhibitor crizotinib. Lung Cancer. 2013, 81(3): 328-336.

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