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Réactifs et instruments pour l'immunologie, la biologie cellulaire et la biologie moléculaire.

Golvatinib [928037-13-2]

Imprimer

Référence HY-13068-5mg

Conditionnement : 5mg

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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)

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]

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.

Solvant et solubilité

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)

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.

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.

Pureté et documentation

Purity: 99.86%

Fiche technique (274 KB) SDS (393 KB)

COA (244 KB) LCMS (96 KB)

Instruction de manipulation (2659 KB)

Références

[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]

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Marque : MedChemExpress

Contactez votre distributeur local :

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