Tariquidar dihydrochloride (Synonyms: XR9576 dihydrochloride)

Cat. No.: HY-110377: FAQs
Data Sheet Handling Instructions

Molarity Calculator

Tariquidar dihydrochloride (XR9576 dihydrochloride) is a potent and specific inhibitor of P-glycoprotein (P-gp) with the high affinity (K_d=5.1 nM).

For research use only. We do not sell to patients.

Tariquidar dihydrochloride Chemical Structure

CAS No. : 1992047-62-7

Size		Stock
50 mg		Get quote
100 mg		Get quote
250 mg		Get quote
Other size		Get quote

Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Other In-stock Forms of Tariquidar dihydrochloride:

Tariquidar Tariquidar methanesulfonate, hydrate

Other Forms of Tariquidar dihydrochloride:

Tariquidar In-stock
Tariquidar methanesulfonate, hydrate In-stock

46 Publications Citing Use of MCE Tariquidar dihydrochloride

: Tariquidar dihydrochloride purchased from MedChemExpress. Usage Cited in: Eur J Med Chem. 2017 Feb 15;127:586-598. [Abstract]; Fluorescence ratio values in K562/DOX cells incubated with Rhd 123 in the absence (control) and in the presence of Verapamil (ver.) and Tariquidar (tar.) tested at 3.0 μM and 1.0 μM concentrations respectively.

: Tariquidar dihydrochloride purchased from MedChemExpress. Usage Cited in: RSC Adv. 2016,6, 69083-69093.; Western blot analysis on MCF-7/ADR cells after being treated by (A) control (without treatment), (B) free DOX, (C) CMC/CaCO₃/DOX, (D) BCMC/CaCO₃/DOX, (E) CMC/CaCO₃/DOX/TQR, and (F) BCMC/CaCO₃/DOX/TQR for 24 h.

Featured Recommendations

•Related Small Molecules:

•Related Proteins:

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

Tariquidar dihydrochloride (XR9576 dihydrochloride) is a potent and specific inhibitor of P-glycoprotein (P-gp) with the high affinity (K_d=5.1 nM)^[1].

IC₅₀ & Target

Kd: 5.1 nM (P-gp)^[1]

In Vitro

Tariquidar (XR9576) is a potent modulator of P-gp mediated [³H]-Vinblastine and [³H]-Paclitaxel transport as it increases the steady-state accumulation of these cytotoxics in CH^rB30 cells to levels observed in non-P-gp-expressing AuxB1 cells (EC₅₀=487±50 nM). [³H]-Tariquidar binds to CH^rB30 membranes with the highest affinity (K_d=5.1±0.9 nM, n=7) and a binding capacity (B_max) of 275±15 pmol/mg membrane protein. In contrast to the parental cell line, the accumulation of [³H]-Vinblastine is increased in a dose-dependent fashion by the modulators Tariquidar (EC₅₀=487±50 nM). The MDR modulator Tariquidar is able to inhibit 60-70% of the vanadate-sensitive ATPase activity, with potent IC₅₀ value of 43±9 nM^[1]. Tariquidar (XR9576) potentiates the cytotoxicity of several drugs including Doxorubicin, Paclitaxel, Etoposide, and Vincristine; complete reversal of resistance is achieved in the presence of 25-80 nM XR9576. Tariquidar is a potent inhibitor of photoaffinity labeling of P-gp by [³H]Azidopine implying a direct interaction with the protein^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

In mice bearing the intrinsically resistant MC26 colon tumors, coadministration of Tariquidar (XR9576) 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

719.65

Formula

C₃₈H₄₀Cl₂N₄O₆

CAS No.

1992047-62-7

SMILES

[H]Cl.[H]Cl.O=C(C1=CC2=CC=CC=C2N=C1)NC3=CC(OC)=C(OC)C=C3C(NC4=CC=C(CCN5CC6=C(C=C(OC)C(OC)=C6)CC5)C=C4)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

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. [Content Brief]

[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. [Content Brief]

Cell Assay ^[2]	Cells (EMT6 AR1.0 8×10²/well; A2780 5×10³/well; 2780AD 6×10³/well) are seeded into 96-well plates. After ~4 h, varying concentrations of Tariquidar are added, and cells are incubated for an additional 4 days (EMT6 AR1.0) or 6 days (2780AD) before quantification of cell growth and calculation of IC₁₀ values (concentration resulting in 10% inhibition of cell growth)^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Mice^[2] MC26 tumor slurry is implanted s.c. in BALB/c mice (day 0). The animals are then randomized, 24 h later, into groups of 15-18 and treated once with various regimens. Tariquidar or vehicle is administered either i.v. via a lateral tail vein or p.o. with Doxorubicin (5 mg/kg) or vehicle i.v. The modulator is administered either i.v. at 2-4 mg/kg (10 mL/kg) at the same time as Doxorubicin or p.o. at 2-8 mg/kg (10 mL/kg) 1 h before the Cytotoxic drug. GG918 is administered p.o. 1 h before doxorubicin. All of the animals are weighed twice weekly. The animals are killed by cervical dislocation on day 14, and the tumors are excised and weighed. The data are analyzed by Student’s t test. Rats^[2] Male CD rats (3 animals per time point) are dosed i.v. with paclitaxel alone [15 min infusion at 10 mg/kg in Tween 80:ethanol:5% dextrose (5:10:85% v/v/v)] or in combination with Tariquidar (10 mg/kg). Tariquidar is administered as a bolus (i.v.) dose 15 min before infusion of Paclitaxel. Blood samples are collected by cardiac puncture using heparinized syringes at various times between 0.083 and 48 h and are centrifuged to prepare plasma, which is stored at −20°C until analysis. Paclitaxel concentration in plasma samples is measured by a LC-MS/MS assay. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. [Content Brief] [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. [Content Brief]

Tariquidar dihydrochloride Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tariquidar1992047-62-7XR9576XR 9576XR-9576P-glycoproteinP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Salutation

Applicant Name *

Email Address *

Phone Number *

Organization Name *

Department *

Requested quantity *

Country or Region *

Remarks