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Golvatinib (E7050)

C-Met/VEGFR-2 inhibitor CAS# 928037-13-2

Golvatinib (E7050)

Catalog No. BCC4423----Order now to get a substantial discount!

Product Name & Size Price Stock
Golvatinib (E7050): 5mg $69 In Stock
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Quality Control of Golvatinib (E7050)

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Chemical structure

Golvatinib (E7050)

3D structure

Chemical Properties of Golvatinib (E7050)

Cas No. 928037-13-2 SDF Download SDF
PubChem ID 16118392 Appearance Powder
Formula C33H37F2N7O4 M.Wt 633.69
Type of Compound N/A Storage Desiccate at -20°C
Synonyms Golvatinib
Solubility Soluble in DMSO > 10 mM
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
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
Standard InChIKey UQRCJCNVNUFYDX-UHFFFAOYSA-N
Standard InChI InChI=1S/C33H37F2N7O4/c1-40-16-18-41(19-17-40)24-9-14-42(15-10-24)32(45)39-29-21-26(8-13-36-29)46-25-6-7-28(27(35)20-25)38-31(44)33(11-12-33)30(43)37-23-4-2-22(34)3-5-23/h2-8,13,20-21,24H,9-12,14-19H2,1H3,(H,37,43)(H,38,44)(H,36,39,45)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Golvatinib (E7050)

DescriptionGolvatinib (E7050) is a dual inhibitor of c-Met and VEGFR-2 with IC50 values of 14 nM and 16 nM, respectively.
Targetsc-MetVEGFR2    
IC5014 nM16 nM    

Protocol

Cell Assay [1]
Cells (1000-3000 cells/100 μL/well) are seeded on 96-well culture plates with various concentrations of E7050 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 Administration [1]
Mice: Nude mice bearing MKN45, Hs746T, SNU-5, or EBC-1 tumors are administered E7050 (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. [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.

Golvatinib (E7050) Dilution Calculator

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Golvatinib (E7050) Molarity Calculator

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Preparing Stock Solutions of Golvatinib (E7050)

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.5781 mL 7.8903 mL 15.7806 mL 31.5612 mL 39.4515 mL
5 mM 0.3156 mL 1.5781 mL 3.1561 mL 6.3122 mL 7.8903 mL
10 mM 0.1578 mL 0.789 mL 1.5781 mL 3.1561 mL 3.9451 mL
50 mM 0.0316 mL 0.1578 mL 0.3156 mL 0.6312 mL 0.789 mL
100 mM 0.0158 mL 0.0789 mL 0.1578 mL 0.3156 mL 0.3945 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Golvatinib (E7050)

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.

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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.

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