Golvatinib (E7050) (Synonyms: E7050) |
| Catalog No.GC17715 |
Golvatinib (E7050) (E-7050) is a potent dual inhibitor of both c-Met and VEGFR2 kinases with IC50s of 14 and 16 nM, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 928037-13-2
Sample solution is provided at 25 µL, 10mM.
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Golvatinib is an inhibitor of c-Met and VEGFR-2 tyrosine kinase with IC50 values of 14nM and 16nM, respectively [1].
The small molecule compound, golvatinib, is a dual inhibitor of both c-Met and VEGFR-2. It is developed as a therapeutic reagent with more potent antitumor activity. Golvatinib inhibits the autophosphorylation of c-Met in MKN45 cells and inhibits the phosphorylation of VEGFR-2 in HUVECs with IC50 values of 14nM and 16nM, respectively. Golvatinib also inhibits the growth of various tumor cells including MKN45, EBC-1, Hs746T and SNU-5. Besides that, golvatinib effectively suppresses the growth induced by HGF or VEGF with IC50 values of 17nM and 84nM [1].
In mice models bearing xenograft tumor cell lines including MKN45, Hs746T, SNU-5 and EBC-1, treatment of golvatinib significantly inhibits the tumor growth. In mice xenograft model with VEGF-overexpressed human pancreatic cancer cell line KP-1 /VEGF, a single administration of E7050 reduces the VEGFR-2 phosphorylation and subsequently inhibits tumor growth through inhibiting VEGF /VEGFR-2 mediated tumor angiogenesis [1].
References:
[1] Nakagawa T, Tohyama O, Yamaguchi A, et al. E7050: A dual c-Met and VEGFR-2 tyrosine kinase inhibitor promotes tumor regression and prolongs survival in mouse xenograft models. Cancer science, 2010, 101(1): 210-215.
Cell experiment: | 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]. |
Animal experiment: | 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]. |
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. | |
| Cas No. | 928037-13-2 | SDF | |
| Synonyms | E7050 | ||
| Chemical Name | 1-N'-[2-fluoro-4-[2-[[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]amino]pyridin-4-yl]oxyphenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide | ||
| Canonical SMILES | CN1CCN(CC1)C2CCN(CC2)C(=O)NC3=NC=CC(=C3)OC4=CC(=C(C=C4)NC(=O)C5(CC5)C(=O)NC6=CC=C(C=C6)F)F | ||
| Formula | C33H37F2N7O4 | M.Wt | 633.69 |
| Solubility | ≥ 15.85mg/mL in DMSO with gentle warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 | 0.789 mL | 1.5781 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 35 reference(s) in Google Scholar.)
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