Dofequidar - CAS 129716-58-1
Catalog number:
129716-58-1
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
COA:
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Targets:
P-glycoprotein
Description:
Dofequidar, also known as MS-209, is a quinolone-derived sphingomyelin synthase inhibitor that blocks P-glycoprotein and multidrug resistance-associated protein-1, is under development by Schering for the potential treatment of multidrug resistant tumors. Dofequidar was found to sensitizes cancer stem-like side population cells to chemotherapeutic drugs by inhibiting ABCG2/BCRP-mediated drug export.
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Appearance:
white solid powder
Synonyms:
Dofequidar
MSDS:
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Current Developer:
Mitsui Pharmaceuticals (Originator), Nihon Schering (Originator), Schering AG (Originator).
1.Dofequidar fumarate (MS-209) in combination with cyclophosphamide, doxorubicin, and fluorouracil for patients with advanced or recurrent breast cancer.
Saeki T1, Nomizu T, Toi M, Ito Y, Noguchi S, Kobayashi T, Asaga T, Minami H, Yamamoto N, Aogi K, Ikeda T, Ohashi Y, Sato W, Tsuruo T. J Clin Oncol. 2007 Feb 1;25(4):411-7. Epub 2006 Dec 18.
PURPOSE: To evaluate the efficacy and tolerability of dofequidar plus cyclophosphamide, doxorubicin, and fluorouracil (CAF) therapy in comparison with CAF alone, in patients with advanced or recurrent breast cancer. Dofequidar is a novel, orally active quinoline derivative that reverses multidrug resistance.
2.Dofequidar fumarate sensitizes cancer stem-like side population cells to chemotherapeutic drugs by inhibiting ABCG2/BCRP-mediated drug export.
Katayama R1, Koike S, Sato S, Sugimoto Y, Tsuruo T, Fujita N. Cancer Sci. 2009 Nov;100(11):2060-8. doi: 10.1111/j.1349-7006.2009.01288.x. Epub 2009 Jul 17.
The ATP-binding cassette (ABC) transporters (ABC-T) actively efflux structurally and mechanistically unrelated anticancer drugs from cells. As a consequence, they can confer multidrug resistance (MDR) to cancer cells. ABC-T are also reported to be phenotypic markers and functional regulators of cancer stem/initiating cells (CSC) and believed to be associated with tumor initiation, progression, and relapse. Dofequidar fumarate, an orally active quinoline compound, has been reported to overcome MDR by inhibiting ABCB1/P-gp, ABCC1/MDR-associated protein 1, or both. Phase III clinical trials suggested that dofequidar had efficacy in patients who had not received prior therapy. Here we show that dofequidar inhibits the efflux of chemotherapeutic drugs and increases the sensitivity to anticancer drugs in CSC-like side population (SP) cells isolated from various cancer cell lines. Dofequidar treatment greatly reduced the cell number in the SP fraction.
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CAS 129716-58-1 Dofequidar

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