| Identification | Back Directory | [Name]
XR9576 | [CAS]
625375-83-9 | [Synonyms]
XR 9576;XR-9576;XR9576
XR9576 methanesulfonate, hydrate
Tariquidar (Methanesulfonate, hydrate)
Tariquidar dimethanesulfonate hexahydrate
TARIQUIDAR METHANESULFONATE HYDRATE;XR 9576;XR-9576
N-[2-({4-[2-(6,7-Dimethoxy-3,4-dihydro-2(1H)-isoquinolinyl)ethyl]phenyl}carbamoyl)-4,5-dimethoxyphenyl]-3-quinolinecarboxamide | [Molecular Formula]
C40H52N4O15S2 | [MDL Number]
MFCD25372040 | [MOL File]
625375-83-9.mol | [Molecular Weight]
892.989 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
insoluble in H2O; insoluble in EtOH; ≥56.2 mg/mL in DMSO | [form ]
Powder | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
Tariquidar methanesulfonate, hydrate (XR9576 methanesulfonate, hydrate) is a potent and specific inhibitor of P-glycoprotein (P-gp) with a Kd of 5.1 nM. | [in vivo]
In mice bearing the intrinsically resistant MC26 colon tumors, coadministration of Tariquidar methanesulfonate, hydrate (XR9576 methanesulfonate, hydrate) potentiates the antitumor activity of Doxorubicin without a significant increase in toxicity; maximum potentiation is observed at 2.5-4.0 mg/kg dosed either i.v. or p.o. In addition, coadministration of Tariquidar (6-12 mg/kg p.o.) fully restores the antitumor activity of Paclitaxel, Etoposide, and Vincristine against two highly resistant MDR human tumor xenografts (2780AD, H69/LX4) in nude mice. Tariquidar is found to also significantly potentiate the antitumor activity of doxorubicin against s.c. MC26 tumors in vivo[2]. | [References]
[1] Martin C, et al. The molecular interaction of the high affinity reversal agent XR9576 with P-glycoprotein. Br J Pharmacol, 1999, 128(2), 403-411. DOI:10.1038/sj.bjp.0702807
[2] Mistry P, et al. In vitro and in vivo reversal of P-glycoprotein-mediated multidrug resistance by a novel potent modulator, XR9576. Cancer Res, 2001, 61(2), 749-758. PMID:11212278
[3] Vraka C, et al. A new method measuring the interaction of radiotracers with the human P-glycoprotein (P-gp) transporter. Nucl Med Biol. 2018 Feb 14;60:29-36. DOI:10.1016/j.nucmedbio.2018.02.002 |
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| Company Name: |
Musechem
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| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
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