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Golvatinib (E7050)

Catalog No.
B1439
C-Met/VEGFR-2 inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$132.00
In stock
10mg
$124.00
In stock
20mg
$214.00
In stock
50mg
$380.00
In stock
100mg
$637.00
In stock
200mg
$903.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

Golvatinib is an inhibitor of c-Met and VEGFR-2 tyrosine kinase with IC50 values of 14nM and 16nM, respectively [1].

The small molecule compound, golvatinib, is a dual inhibitor of both c-Met and VEGFR-2. It is developed as a therapeutic reagent with more potent antitumor activity. Golvatinib inhibits the autophosphorylation of c-Met in MKN45 cells and inhibits the phosphorylation of VEGFR-2 in HUVECs with IC50 values of 14nM and 16nM, respectively. Golvatinib also inhibits the growth of various tumor cells including MKN45, EBC-1, Hs746T and SNU-5. Besides that, golvatinib effectively suppresses the growth induced by HGF or VEGF with IC50 values of 17nM and 84nM [1].

In mice models bearing xenograft tumor cell lines including MKN45, Hs746T, SNU-5 and EBC-1, treatment of golvatinib significantly inhibits the tumor growth. In mice xenograft model with VEGF-overexpressed human pancreatic cancer cell line KP-1 /VEGF, a single administration of E7050 reduces the VEGFR-2 phosphorylation and subsequently inhibits tumor growth through inhibiting VEGF /VEGFR-2 mediated tumor angiogenesis [1].

References:
[1] Nakagawa T, Tohyama O, Yamaguchi A, et al. E7050: A dual c-Met and VEGFR-2 tyrosine kinase inhibitor promotes tumor regression and prolongs survival in mouse xenograft models. Cancer science, 2010, 101(1): 210-215.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt633.69
Cas No.928037-13-2
FormulaC33H37F2N7O4
Solubility≥15.85mg/mL in DMSO with gentle warming
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
SDFDownload SDF
Canonical SMILESCN1CCN(CC1)C2CCN(CC2)C(=O)NC3=NC=CC(=C3)OC4=CC(=C(C=C4)NC(=O)C5(CC5)C(=O)NC6=CC=C(C=C6)F)F
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Biological Activity

Description Golvatinib (E7050) is a dual inhibitor of c-Met and VEGFR-2 with IC50 values of 14 nM and 16 nM, respectively.
Targets c-Met VEGFR2        
IC50 14 nM 16 nM        

Quality Control

Quality Control & MSDS

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Chemical structure

Golvatinib (E7050)