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Dofequidar fumarate

Catalog No. T11071 CAS 153653-30-6

Synonyms: MS-209

Dofequidar fumarate (MS-209)(MS-209 fumarate), a quinoline-based compound administered orally, is known for counteracting multidrug resistance (MDR) through the inhibition of ABCB1/P-glycoprotein (P-gp) and ABCC1/MDR-associated protein 1.

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Dofequidar fumarate, CAS 153653-30-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 33.00
2 mg	In stock	$ 46.00
5 mg	In stock	$ 77.00
10 mg	In stock	$ 127.00
25 mg	In stock	$ 258.00
50 mg	In stock	$ 497.00
100 mg	In stock	$ 723.00
500 mg	In stock	$ 1,520.00
1 mL * 10 mM (in DMSO)	In stock	$ 97.00

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Purity: 99.43%

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Description	Dofequidar fumarate (MS-209)(MS-209 fumarate), a quinoline-based compound administered orally, is known for counteracting multidrug resistance (MDR) through the inhibition of ABCB1/P-glycoprotein (P-gp) and ABCC1/MDR-associated protein 1.
In vitro	Dofequidar fumarate effectively overcomes docetaxel resistance in MDR cancer cells, and this concentration reaches> 7 h in plasma without severe toxicity.Dofequidar fumarate restored the chemical sensitivity of SBC-3/ADM cells to VP-16, ADM and VCR in a dose-dependent manner in vitro. Dofequidar inhibits the outflow of chemotherapy drugs and increases the sensitivity of anti-cancer drugs to CSC-like side population (SP) cells isolated from various cancer cell lines. Dofequidar treatment greatly reduces the number of cells in the SP component. In 4-1St cells with strong resistance to ADM and VCR, Dofequidar fumarate at a concentration of 3 microM increased the cytotoxicity of ADM and VCR by 88-fold and 350-fold, respectively.
In vivo	Docetaxel alone at the maximum tolerated dose (MTD) has significant antitumor activity against intrinsically resistant HCT-15 tumor xenografts, while Dofequidar fumarate also enhances the antitumor effect of docetaxel active. For MCF-7/ADM tumor xenografts expressing large amounts of P-gp, docetaxel alone did not show antitumor activity at MTD, while the combination of MTD and Dofequidar fumarate for docetaxel greatly reduced MCF -7/ADM tumor growth. Intravenous injection of SBC-3 or SBC-3/ADM cells will produce metastatic colonies in the liver, kidneys, and lymph nodes in severe combined immunodeficiency (SCID) mice depleted by natural killer (NK) cells, although SBC-3/ ADM cells produce faster transfers than SBC-3 cells. The treatment of VP-16 and ADM reduced the formation of metastasis of SBC-3 cells, while the same treatment did not affect the metastasis of SBC-3/ADM cells. Although the use of MS-209 alone has no effect on the transfer of SBC-3 or SBC-3/ADM cells, the combined use of MS-209 and VP-16 or ADM can significantly inhibit the proliferation of SBC-3/ADM cells Metastasis to form an organ.

Synonyms	MS-209
Molecular Weight	597.66
Formula	C34H35N3O7
CAS No.	153653-30-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 1 mg/mL (1.67 mM), Sonication is recommended.

DMSO: 100 mg/mL (167.32 mM), Sonication is recommended.

References and Literature

1. Nakanishi O, et al. Potentiation of the antitumor activity by a novel quinoline compound, MS-209, in multidrug-resistant solid tumor cell lines. Oncol Res. 1997;9(2):61-9. 2. Naito M, et al. MS-209, a quinoline-type reversal agent, potentiates antitumor efficacy of docetaxel in multidrug-resistant solid tumor xenograft models. Clin Cancer Res. 2002 Feb;8(2):582-8. 3. Nokihara H, et al. A new quinoline derivative MS-209 reverses multidrug resistance and inhibits multiorgan metastases by P-glycoprotein-expressing human small cell lung cancer cells. Jpn J Cancer Res. 2001 Jul;92(7):785-92. 4. Katayama R, et al. Dofequidar fumarate sensitizes cancer stem-like side population cells to chemotherapeutic drugs by inhibiting ABCG2/BCRP-mediated drug export. Cancer Sci. 2009 Nov;100(11):2060-8.

Related compound libraries

This product is contained In the following compound libraries：

Membrane Protein-targeted Compound Library Anti-Cancer Drug Library Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library ReFRAME Related Library Orally Active Compound Library Ion Channel Inhibitor Library Neuronal Signaling Compound Library

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Keywords

Dofequidar fumarate 153653-30-6 Membrane transporter/Ion channel Neuroscience P-gp Dofequidar Inhibitor CD243 ABCB1 Dofequidar Fumarate Multidrug resistance protein 1 Cluster of differentiation 243 MS-209 P-glycoprotein MDR1 inhibit MS 209 MS209 Pgp inhibitor

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