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VS-4718 is an inhibitor of focal adhesion kinase (FAK). It blocks FAK Tyr-397 phophorylation in vivo and exhibits antitumor activity in orthotopic breast carcinoma models in mice. VS-4718 also significantly reverses ATP-binding cassette transporter ABCB1 and ABCG2-mediated multi-drug resistance. It shows potential in combination with other therapies to overcome multidrug resistance in ABCB1 or ABCG2-overexpressing cancer cells.
| Cas No. | 1061353-68-1 |
|---|---|
| Purity | ≥99% |
| Formula | C25H26F3N5O3 |
| Formula Wt. | 501.51 |
| Chemical Name | VS-4718 |
| IUPAC Name | 2-{[2-{[2-Methoxy-4-(4-morpholinyl)phenyl]amino}-5-(trifluoromethyl)-4-pyridinyl]amino}-N-methylbenzamide |
| Synonym | VS-4718, VS 4718, VS4718, SR-2516, SR 2516, SR2516, PND-1186, PND 1186, PND1186 |
| Solubility | Insoluble in water. Solubility in DMSO - 24 mg/mL |
| Store Temp | -20°C |
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| Ship Temp | Ambient |
| MSDS | |
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| Info Sheet |
Walsh C., Tanjoni I., et al. Oral delivery of PND-1186 FAK inhibitor decreases tumor growth and spontaneous breast to lung metastasis in pre-clinical models. Cancer Biol Ther. 9(10):778-90 (2010). PMID: 20234193.
Ji N., Yang Y., et al. VS-4718 Antagonizes Multidrug Resistance in ABCB1- and ABCG2-Overexpressing Cancer Cells by Inhibiting the Efflux Function of ABC Transporters. Front PHarmacol. 9:1236 (2018). PMID: 30425643.