Golvatinib
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.
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- Pureté: 99.86%
- CAS No.: 928037-13-2
- Formule: C33H37F2N7O4
- Masse moléculaire:633.69
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Golvatinib
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Customer Validation & Images
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Activité biologique
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VEGFR2 16 nM (IC50) |
c-Met 14 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
6.89 μM
Compound: 3
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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
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[PMID: 32173195] |
| A549 | IC50 |
7.7 μM
Compound: 1
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Cytotoxicity against human A549 cells after 72 hrs by MTT assay
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
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[PMID: 33316412] |
| EBC-1 | IC50 |
6.2 nM
Compound: E7050; Golvatinib
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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
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[PMID: 26717201] |
| EBC-1 | IC50 |
24 nM
Compound: 82
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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
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[PMID: 37262349] |
| HeLa | IC50 |
4.14 μM
Compound: 3
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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
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[PMID: 32173195] |
| HeLa | IC50 |
4.23 μM
Compound: 1
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Cytotoxicity against human HeLa cells after 72 hrs by MTT assay
Cytotoxicity against human HeLa cells after 72 hrs by MTT assay
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[PMID: 33316412] |
| HepG2 | IC50 |
65.5 μM
Compound: Golvatinib
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Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay
Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay
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[PMID: 25082515] |
| Hs746T | IC50 |
23 nM
Compound: E7050; Golvatinib
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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
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[PMID: 26717201] |
| Hs746T | IC50 |
23 nM
Compound: 82
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Antiproliferative activity against human Hs746T cells assessed as inhibition of cell growth
Antiproliferative activity against human Hs746T cells assessed as inhibition of cell growth
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[PMID: 37262349] |
| HUVEC | IC50 |
16 nM
Compound: E7050; Golvatinib
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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
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[PMID: 26717201] |
| HUVEC | IC50 |
17 nM
Compound: E7050; Golvatinib
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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
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[PMID: 26717201] |
| HUVEC | IC50 |
84 nM
Compound: E7050; Golvatinib
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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
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[PMID: 26717201] |
| HUVEC | IC50 |
>1000 nM
Compound: E7050; Golvatinib
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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
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[PMID: 26717201] |
| HUVEC | IC50 |
16 nM
Compound: 15; E7050
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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
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[PMID: 27299736] |
| MCF7 | IC50 |
49.6 μM
Compound: Golvatinib
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Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay
Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay
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[PMID: 25082515] |
| MCF7 | IC50 |
20.61 μM
Compound: 3
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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
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[PMID: 32173195] |
| MCF7 | IC50 |
15.44 μM
Compound: 1
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Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay
Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay
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[PMID: 33316412] |
| MKN-45 | IC50 |
14 nM
Compound: E7050; Golvatinib
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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
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[PMID: 26717201] |
| MKN-45 | IC50 |
37 nM
Compound: E7050; Golvatinib
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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
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[PMID: 26717201] |
| MKN-45 | IC50 |
14 nM
Compound: 15; E7050
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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
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[PMID: 27299736] |
| MKN-45 | IC50 |
37 nM
Compound: 82
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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
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[PMID: 37262349] |
| SNU-5 | IC50 |
24 nM
Compound: E7050; Golvatinib
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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
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[PMID: 26717201] |
| SNU-5 | IC50 |
6.2 nM
Compound: 82
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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
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[PMID: 37262349] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 928037-13-2
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Appearance Solid
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Masse moléculaire 633.69
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Formule C33H37F2N7O4
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Color White to off-white
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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
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Synonyms
E-7050
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
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
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Most Recent
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Science
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.
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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 -
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocole
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.
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.
Pureté et documentation
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Fiche technique (274 KB)
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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)
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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]
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.
| 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
HY-13068 Related Classifications
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