Golvatinib (E7050)C-Met/VEGFR-2 inhibitor CAS# 928037-13-2 |
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Quality Control & MSDS
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| 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. |
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| 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. |
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| 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. | ||
| Description | Golvatinib (E7050) is a dual inhibitor of c-Met and VEGFR-2 with IC50 values of 14 nM and 16 nM, respectively. | |||||
| Targets | c-Met | VEGFR2 | ||||
| IC50 | 14 nM | 16 nM | ||||
Golvatinib (E7050) Dilution Calculator
Golvatinib (E7050) Molarity Calculator
| 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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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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