Cat. No.: HY-13068

Golvatinib

(Synonyms: E-7050)

4 Cited Publications

Customer Review

Based on 4 publication(s) in Google Scholar

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.

Purity: 99.86%
CAS No.: 928037-13-2
Formula: C₃₃H₃₇F₂N₇O₄
Molecular Weight:633.69

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Golvatinib Chemical Structure

CAS No.: 928037-13-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (4)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

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)

All VEGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	6.89 μM Compound: 3	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 32173195]
A549	IC₅₀	7.7 μM Compound: 1	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 33316412]
EBC-1	IC₅₀	6.2 nM Compound: E7050; Golvatinib	Cytotoxicity against human EBC1 cells assessed as inhibition of tumour growth after 3 days by WST-8 assay Cytotoxicity against human EBC1 cells assessed as inhibition of tumour growth after 3 days by WST-8 assay	[PMID: 26717201]
EBC-1	IC₅₀	24 nM Compound: 82	Antiproliferative activity against human EBC-1 cells assessed as inhibition of cell growth Antiproliferative activity against human EBC-1 cells assessed as inhibition of cell growth	[PMID: 37262349]
HeLa	IC₅₀	4.14 μM Compound: 3	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 32173195]
HeLa	IC₅₀	4.23 μM Compound: 1	Cytotoxicity against human HeLa cells after 72 hrs by MTT assay Cytotoxicity against human HeLa cells after 72 hrs by MTT assay	[PMID: 33316412]
HepG2	IC₅₀	65.5 μM Compound: Golvatinib	Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay	[PMID: 25082515]
Hs746T	IC₅₀	23 nM Compound: E7050; Golvatinib	Cytotoxicity against human Hs 746T cells assessed as inhibition of tumour growth after 3 days by WST-8 assay Cytotoxicity against human Hs 746T cells assessed as inhibition of tumour growth after 3 days by WST-8 assay	[PMID: 26717201]
Hs746T	IC₅₀	23 nM Compound: 82	Antiproliferative activity against human Hs746T cells assessed as inhibition of cell growth Antiproliferative activity against human Hs746T cells assessed as inhibition of cell growth	[PMID: 37262349]
HUVEC	IC₅₀	16 nM Compound: E7050; Golvatinib	Inhibition of VEGFR-2 autophosphorylation in HUVEC after 1 hr by Western blot analysis Inhibition of VEGFR-2 autophosphorylation in HUVEC after 1 hr by Western blot analysis	[PMID: 26717201]
HUVEC	IC₅₀	17 nM Compound: E7050; Golvatinib	Antiangiogenic activity in HUVEC assessed as inhibition of HGF induced cell proliferation after 3 days by WST-1 assay Antiangiogenic activity in HUVEC assessed as inhibition of HGF induced cell proliferation after 3 days by WST-1 assay	[PMID: 26717201]
HUVEC	IC₅₀	84 nM Compound: E7050; Golvatinib	Antiangiogenic activity in HUVEC assessed as inhibition of VEGF induced cell proliferation after 3 days by WST-1 assay Antiangiogenic activity in HUVEC assessed as inhibition of VEGF induced cell proliferation after 3 days by WST-1 assay	[PMID: 26717201]
HUVEC	IC₅₀	>1000 nM Compound: E7050; Golvatinib	Antiangiogenic activity in HUVEC assessed as inhibition of bFGF induced cell proliferation after 3 days by WST-1 assay Antiangiogenic activity in HUVEC assessed as inhibition of bFGF induced cell proliferation after 3 days by WST-1 assay	[PMID: 26717201]
HUVEC	IC₅₀	16 nM Compound: 15; E7050	Inhibition of VEGF induced VEGFR2 phosphorylation in HUVEC preincubated for 1 hr followed by VEGF-stimulation for 5 mins by Western blot analysis Inhibition of VEGF induced VEGFR2 phosphorylation in HUVEC preincubated for 1 hr followed by VEGF-stimulation for 5 mins by Western blot analysis	[PMID: 27299736]
MCF7	IC₅₀	49.6 μM Compound: Golvatinib	Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 25082515]
MCF7	IC₅₀	20.61 μM Compound: 3	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 32173195]
MCF7	IC₅₀	15.44 μM Compound: 1	Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 33316412]
MKN-45	IC₅₀	14 nM Compound: E7050; Golvatinib	Inhibition of c-Met autophosphorylation in human MKN45 cells after 2 hrs by Western blot analysis Inhibition of c-Met autophosphorylation in human MKN45 cells after 2 hrs by Western blot analysis	[PMID: 26717201]
MKN-45	IC₅₀	37 nM Compound: E7050; Golvatinib	Cytotoxicity against human MKN45 cells assessed as inhibition of tumour growth after 3 days by WST-8 assay Cytotoxicity against human MKN45 cells assessed as inhibition of tumour growth after 3 days by WST-8 assay	[PMID: 26717201]
MKN-45	IC₅₀	14 nM Compound: 15; E7050	Inhibition of MET autophosphorylation in human MKN45 cells after 2 hrs by Western blot analysis Inhibition of MET autophosphorylation in human MKN45 cells after 2 hrs by Western blot analysis	[PMID: 27299736]
MKN-45	IC₅₀	37 nM Compound: 82	Antiproliferative activity against human MKN-45 cells assessed as inhibition of cell growth Antiproliferative activity against human MKN-45 cells assessed as inhibition of cell growth	[PMID: 37262349]
SNU-5	IC₅₀	24 nM Compound: E7050; Golvatinib	Cytotoxicity against human SNU5 cells assessed as inhibition of tumour growth after 3 days by WST-8 assay Cytotoxicity against human SNU5 cells assessed as inhibition of tumour growth after 3 days by WST-8 assay	[PMID: 26717201]
SNU-5	IC₅₀	6.2 nM Compound: 82	Antiproliferative activity against human SNU-5 cells assessed as inhibition of cell growth Antiproliferative activity against human SNU-5 cells assessed as inhibition of cell growth	[PMID: 37262349]

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.

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 928037-13-2
Appearance Solid
Molecular Weight 633.69
Formula C₃₃H₃₇F₂N₇O₄
Color White to off-white
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
Synonyms

E-7050
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

Publications (4)

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Journal Impact Factor

Science

The target landscape of clinical kinase drugs. [Abstract]

2017 Dec 1;358(6367):eaan4368. PMID: 29191878

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.
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
PLoS Biol

Structural basis for neutralization of hepatitis A virus informs a rational design of highly potent inhibitors. [Abstract]

2019 Apr 30;17(4):e3000229. PMID: 31039149
Technical University of Munich

24.01.2018.

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (78.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocol

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].

MedChemExpress (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].

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

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. [Content Brief]

[2]. Wang W et al. Met kinase inhibitor E7050 reverses three different mechanisms of hepatocyte growth factor-induced tyrosine kinase inhibitor resistance in EGFR mutant lung cancer. Clin Cancer Res, 2012, 18(6), 1663-1671. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.5781 mL	7.8903 mL	15.7806 mL	39.4515 mL
	5 mM	0.3156 mL	1.5781 mL	3.1561 mL	7.8903 mL
	10 mM	0.1578 mL	0.7890 mL	1.5781 mL	3.9451 mL
	15 mM	0.1052 mL	0.5260 mL	1.0520 mL	2.6301 mL
	20 mM	0.0789 mL	0.3945 mL	0.7890 mL	1.9726 mL
	25 mM	0.0631 mL	0.3156 mL	0.6312 mL	1.5781 mL
	30 mM	0.0526 mL	0.2630 mL	0.5260 mL	1.3150 mL
	40 mM	0.0395 mL	0.1973 mL	0.3945 mL	0.9863 mL
	50 mM	0.0316 mL	0.1578 mL	0.3156 mL	0.7890 mL
	60 mM	0.0263 mL	0.1315 mL	0.2630 mL	0.6575 mL

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Golvatinib

Kinase Inhibitor Library

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Publications Citing Use of MedChemExpress (MCE) Golvatinib

All VEGFR Isoforms

Biological Activity

Chemical Information

Publications (4)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Golvatinib Related Classifications

Cat. No.: HY-13068