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Golvatinib

Cat. No. M1901
Golvatinib Structure
Synonym:

E7050

Size Price Availability Quantity
10mg USD 140 In stock
50mg USD 440 In stock
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Quality Control
Biological Activity

Golvatinib (also known as E7050) is a highly potent, small molecule ATP-competitive inhibitor of the c-Met receptor tyrosine kinase and multiple members of the Eph receptor family. c-Met and VEGFR-2 play important roles in tumor cell growth, migration and angiogenesis. Golvatinib (E7050) inhibits the activities of both c-Met and VEGFR-2, which may inhibit tumor cell growth and survival of tumor cells that overexpress these receptor tyrosine kinases. In vitro, Golvatinib (E7050) circumvented resistance to all of the reversible, irreversible, and mutant-selective EGFR-TKIs induced by exogenous and/or endogenous HGF in EGFR mutant lung cancer cell lines, by blocking the Met/Gab1/PI3K/Akt pathway. Golvatinib (E7050) plus gefitinib resulted in marked regression of tumor growth associated with inhibition of Akt phosphorylation in cancer cells in the in vivo model. Golvatinib is currently under evaluation in a phase I clinical trial, it may overcome HGF-induced resistance to gefitinib and next-generation EGFR-TKIs.

Protocol
Cell Experiment
Cell lines MKN45, SNU-5, Hs746, TEBC-1, MKN74, SNU-1 and A549 cells line
Preparation method Cell proliferation assay.
Cells (1-3*103 cells/100 uL/well) were seeded on 96-well culture plates with various concentrations of E7050 and cultured for 3 days. Then, 10 uL of CCK-8 reagent was added to each well, and absorbance was measured at 450 nm compared with a reference measurement at 660 nm using a MTP-500 microplate reader (Corona Electric, Ibaraki, Japan). Proliferation assays using HUVEC were performed as described previously. Briefly, HUVEC (2*103 cells/well) were cultured for 3 days in medium containing HGF (30 ng/mL), VEGF (20 ng/mL) (R&D Systems), or basic fibroblast growth factor (bFGF) (20 ng/mL) (Wako Pure Chemicals, Osaka, Japan) together with serially diluted E7050.
Concentrations 0~10 μM
Incubation time 3 days
Animal Experiment
Animal models Nude mice bearing MKN45 (a), Hs746T (b), SNU-5 (c), or EBC-1 (d) tumors model
Formulation saline
Dosages 25, 50, 100 or 200mg/kg daily for15 days
Administration oral
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 633.69
Formula C33H37F2N7O4
CAS Number 928037-13-2
Purity >99%
Solubility DMSO
Storage at -20°C
References

Met kinase inhibitor E7050 reverses three different mechanisms of hepatocyte growth factor-induced tyrosine kinase inhibitor resistance in EGFR mutant lung cancer.
Wang W, et al. Clin Cancer Res. 2012 Mar 15;18(6):1663-71. PMID: 22317763.

E7050: a dual c-Met and VEGFR-2 tyrosine kinase inhibitor promotes tumor regression and prolongs survival in mouse xenograft models.
Nakagawa T, et al. Cancer Sci. 2010 Jan;101(1):210-5. PMID: 19832844.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Golvatinib, E7050 supplier, c-Met, inhibitors

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