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Other Sizes |
Targets |
Kd: 5.1 nM (P-gp)[1]
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ln Vitro |
In CHrB30 cells, tariquidar (XR9576) raises the steady-state accumulation of [3H]-Vinblastine and [3H]-Paclitaxel to levels seen in non-P-gp-expressing AuxB1 cells (EC50=487±50 nM), demonstrating its potency as a regulator of P-gp mediated [3H]-Methionine transport. [3H]-Tariquidar has the strongest affinity (Kd=5.1±0.9 nM, n=7) and the maximum binding capacity (Bmax) of 275±15 pmol/mg membrane protein when it comes to CHrB30 membranes. Unlike the parent cell line, the modulators Tariquidar (EC50=487±50 nM) increase the accumulation of [3H]-Vinblastine in a dose-dependent manner. With a strong IC50 value of 43±9 nM, the MDR modulator Tariquidar can inhibit 60–70% of the activity of the vanadate-sensitive ATPase[1]. Tariquidar (XR9576) enhances the cytotoxicity of several medications, including as Vincristine, Etoposide, Paclitaxel, and Doxorubicin; 25–80 nM XR9576 completely reversals resistance. Strong photoaffinity labeling of P-gp by [3H]Azidopine is inhibited by tariquidar, suggesting a direct interaction with the protein[2].
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ln Vivo |
Additionally, coadministration of Tariquidar (6-12 mg/kg po) fully restores the antitumor activity of Paclitaxel, Etoposide, and Vincristine against two highly resistant MDR human tumor xenografts (2780AD, H69/LX4) in nude mice. These mice bear the intrinsically resistant MC26 colon tumors, and coadministration of Tariquidar (XR9576) potentiates the antitumor activity of Doxorubicin without causing a significant increase in toxicity. It has also been discovered that tariquidar dramatically increases the anticancer efficacy of doxorubicin against sc MC26 tumors in vivo[2].
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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.
[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 |
Molecular Formula |
C38H40CL2N4O6
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Molecular Weight |
719.65
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CAS # |
1992047-62-7
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Related CAS # |
Tariquidar;206873-63-4;Tariquidar methanesulfonate, hydrate;625375-83-9
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SMILES |
Cl.Cl.O(C)C1C(=CC2=C(C=1)CN(CCC1C=CC(=CC=1)NC(C1=CC(=C(C=C1NC(C1=CN=C3C=CC=CC3=C1)=O)OC)OC)=O)CC2)OC
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.3896 mL | 6.9478 mL | 13.8956 mL | |
5 mM | 0.2779 mL | 1.3896 mL | 2.7791 mL | |
10 mM | 0.1390 mL | 0.6948 mL | 1.3896 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.