Golvatinib (Synonyms: E-7050)

Name: Golvatinib
Brand: MedChemExpress
SKU: HY-13068
Rating: 5.0 (4 reviews)

製品番号: HY-13068 純度: 99.86%: Data Sheet SDS COA 取扱説明書
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Golvatinib (E-7050) is a potent dual inhibitor of both c-Met and VEGFR2 kinases with IC₅₀s of 14 and 16 nM, respectively.

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CAS 番号 : 928037-13-2

容量	価格（税別）	在庫状況	数量

>無料サンプル (0.1 - 0.2 mg)		今すぐ申し込む
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 107	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 107	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$77	在庫あり	Estimated Time of Arrival: December 31
10 mg	$121	在庫あり	Estimated Time of Arrival: December 31
25 mg	$185	在庫あり	Estimated Time of Arrival: December 31
50 mg	$275	在庫あり	Estimated Time of Arrival: December 31
100 mg	$495	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

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This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 4 publication(s) in Google Scholar

Other Forms of Golvatinib:

Golvatinib (Standard) お問い合わせ

顧客検証

: 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.

VEGFR アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

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製品説明

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)

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	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]
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]
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	>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	>1 μM 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]
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]
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]
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	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]
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	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	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]

体外実験

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.

体内実験

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.

臨床実験

分子量

633.69

分子式

C₃₃H₃₇F₂N₇O₄

CAS 番号

928037-13-2

Appearance

Solid

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

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)

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

View the Complete Stock Solution Preparation Table

* 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
Dilution Calculator

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

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

純度とドキュメンテーション

純度: 99.86%

Select Batch:

データシート (274 KB) SDS (393 KB)

COA (244 KB) LCMS (96 KB)

取扱説明書 (2659 KB)

参考文献

[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]

細胞実験 ^[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) はこれらの方法の精度を確認していません。こちらは参照専用です。
動物実験 ^[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) はこれらの方法の精度を確認していません。こちらは参照専用です。
参考文献	[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]

Complete Stock Solution Preparation Table

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

Golvatinib Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

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.

Keywords:

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

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Golvatinib (Synonyms: E-7050)

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参考文献

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Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Golvatinib Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

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Golvatinib (Synonyms: E-7050)

カスタマーレビュー

Other Forms of Golvatinib:

Golvatinib 関連抗体

顧客検証

おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

VEGFR アイソフォーム固有の製品をすべて表示:

生物活性

プロトコル

純度とドキュメンテーション

参考文献

カスタマーレビュー

Golvatinib 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Golvatinib Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

最近チェックした製品:

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