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E-7050

Chemical Structure : E-7050

CAS No.: 928037-13-2

E-7050 (Golvatinib;E7050)

Catalog No.: PC-43372Not For Human Use, Lab Use Only.

E-7050 (Golvatinib) is a potent, dual c-Met and VEGFR-2 tyrosine kinase inhibitor with IC50 of 14 and 16 nM (kinase phosphorylation inhibition).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

E-7050 (Golvatinib) is a potent, dual c-Met and VEGFR-2 tyrosine kinase inhibitor with IC50 of 14 and 16 nM (kinase phosphorylation inhibition).
E-7050 (Golvatinib) also strongly inhibits the growth of MKN45, EBC-1, Hs746T, and SNU-5 tumor cells with IC50 values of 37, 6.2, 23, and 24 nM, respectively.
E-7050 (Golvatinib) selectively inhibits the growth of the c-Met amplified tumor cell lines in vitro.
E-7050 (Golvatinib) specifically inhibits HGF and VEGF stimulated HUVEC growth with IC50 values of 17 nM and 84 nM respectively, but bFGF stimulated HUVEC.
E-7050 (Golvatinib) demonstrates inhibition of the phosphorylation of c-Met and VEGFR-2 in tumors, and strong inhibition of tumor growth and tumor angiogenesis in xenograft models.

Physicochemical Properties

M.Wt 633.6882
Formula C33H37F2N7O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1,1-Cyclopropanedicarboxamide, N-[2-fluoro-4-[[2-[[[4-(4-methyl-1-piperazinyl)-1-piperidinyl]carbonyl]amino]-4-pyridinyl]oxy]phenyl]-N'-(4-fluorophenyl)-

References

1. Nakagawa T, et al. Cancer Sci. 2010 Jan;101(1):210-5.

2. Wang W, et al. Clin Cancer Res. 2012 Mar 15;18(6):1663-71.

3. Nakagawa T, et al. Mol Cancer Ther. 2012 Oct;11(10):2149-57.

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