2. Protein Tyrosine Kinase/RTK
  3. c-Met/HGFR VEGFR
  4. Golvatinib

Golvatinib  (Synonyms: E-7050)

Cat. No.: HY-13068 Purity: 99.76%
COA Handling Instructions

Golvatinib (E-7050) is a potent dual inhibitor of both c-Met and VEGFR2 kinases with IC50s of 14 and 16 nM, respectively.

For research use only. We do not sell to patients.

Golvatinib Chemical Structure

Golvatinib Chemical Structure

CAS No. : 928037-13-2

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 108 In-stock
Solution
10 mM * 1 mL in DMSO USD 108 In-stock
Solid
5 mg USD 77 In-stock
10 mg USD 121 In-stock
50 mg USD 275 In-stock
100 mg USD 495 In-stock
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500 mg   Get quote  

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Customer Review

Based on 5 publication(s) in Google Scholar

Golvatinib Related Antibodies

Top Publications Citing Use of Products

    Golvatinib purchased from MedChemExpress. Usage Cited in: Science. 2017 Dec 1;358(6367):eaan4368.  [Abstract]

    Immunoblot analysis in MV-4-11 cells and MOLM-13, FLT3-WT and FLT3-ITD transfected HEK293 cells, and Ba/F3 FLT3-ITD cells revealed FLT3 target engagement for Golvatinib and Cabozantinib.

    View All VEGFR Isoform Specific Products:

    View All Isoforms
    VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Golvatinib (E-7050) is a potent dual inhibitor of both c-Met and VEGFR2 kinases with IC50s of 14 and 16 nM, respectively.

    IC50 & Target[1]

    VEGFR2

    16 nM (IC50)

    c-Met

    14 nM (IC50)

    In Vitro

    Golvatinib (E-7050) potently inhibits phosphorylation of both c-Met and VEGFR-2. Golvatinib also potently represses the growth of both c-met amplified tumor cells and endothelial cells stimulated with either HGF or VEGF.
    Golvatinib 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. The growth of A549, SNU-1 and 0MKN74 tumor cells is inhibited by Golvatinib with much higher IC50 values[1].
    Golvatinib circumvents 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 in vitro.
    Golvatinib also prevents the emergence of gefitinib-resistant HCC827 cells induced by continuous exposure to HGF[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Golvatinib Related Antibodies
    In Vivo

    Golvatinib (E-7050) shows inhibition of the phosphorylation of c-Met and VEGFR-2 in tumors, and strong inhibition of tumor growth and tumor angiogenesis in xenograft models.
    Treatment of some tumor lines containing c-met amplifications with high doses of Golvatinib (50-200 mg/kg) induced tumor regression and disappearance. In a peritoneal dissemination model, Golvatinib shows an antitumor effect against peritoneal tumors as well as a significant prolongation of lifespan in treated mice[1].
    Golvatinib (E7050) plus Gefitinib results in marked regression of tumor growth associated with inhibition of Akt phosphorylation in cancer cells[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    633.69

    Appearance

    Solid

    Formula

    C33H37F2N7O4
    CAS No.
    SMILES

    O=C(NC1=CC=C(C=C1F)OC2=CC(NC(N3CCC(CC3)N4CCN(CC4)C)=O)=NC=C2)C5(CC5)C(NC6=CC=C(C=C6)F)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (78.90 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.5781 mL 7.8903 mL 15.7806 mL
    5 mM 0.3156 mL 1.5781 mL 3.1561 mL
    10 mM 0.1578 mL 0.7890 mL 1.5781 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (3.28 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (3.28 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.08 mg/mL (3.28 mM); Clear solution

    *All of the co-solvents are available by MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.89%

    COA (244 KB) RP-HPLC (194 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [1]

    Cells (1000-3000 cells/100 μL/well) are seeded on 96-well culture plates with various concentrations of Golvatinib and cultured for 3 days. Then, 10 μL of WST-8 reagent is added to each well, and absorbance is measured at 450 nm compared with a reference measurement at 660 nm using a MTP-500 microplate reader[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Mice: Nude mice bearing MKN45, Hs746T, SNU-5, or EBC-1 tumors are administered Golvatinib (25, 50, 100, 200 mg/kg) or vehicle only as a control, once a day. Tumor volume is measured using calipers on the indicated days (0-15 days)[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References
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    Golvatinib Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Keywords:

    Golvatinib928037-13-2E-7050E7050E 7050c-Met/HGFRVEGFRVascular endothelial growth factor receptorInhibitorinhibitorinhibit

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