| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Biricodar dicitrate targets P-glycoprotein (P-gp, ABCB1) and other ABC transporters, including multidrug resistance-associated protein 1 (MRP1, ABCC1) and breast cancer resistance protein (BCRP, ABCG2). By binding to these transporters, biricodar dicitrate inhibits the efflux of chemotherapeutic agents from cancer cells, increasing intracellular drug concentrations and restoring the efficacy of chemotherapy. The compound's inhibition of ABC transporters makes it a valuable tool for studying multidrug resistance and for developing strategies to overcome chemotherapy resistance.
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| ln Vitro |
In vitro, biricodar dicitrate inhibits P-glycoprotein (P-gp) and other ABC transporters, reversing multidrug resistance in cancer cell lines. In cell-based assays, biricodar dicitrate treatment results in increased intracellular accumulation of chemotherapeutic agents, such as doxorubicin or paclitaxel, and restored sensitivity to these agents. The compound's effects on drug accumulation and cytotoxicity are assessed using fluorescence-based assays or cell viability assays. These studies confirm the compound's mechanism of action as an ABC transporter inhibitor.
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| ln Vivo |
In vivo, biricodar dicitrate has been studied for its potential in combination with chemotherapy for the treatment of drug-resistant cancers. By inhibiting ABC transporters, the compound can increase the efficacy of chemotherapeutic agents in animal models of cancer. Biricodar dicitrate has been evaluated in preclinical and clinical studies, where it demonstrates the ability to reverse multidrug resistance. Comprehensive in vivo efficacy studies are needed to fully characterize its therapeutic potential.
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| Enzyme Assay |
In vitro transporter assays for biricodar dicitrate involve measuring the inhibition of P-glycoprotein-mediated efflux of fluorescent or radiolabeled substrates. Membrane vesicles or cells expressing P-gp are incubated with the substrate and varying concentrations of biricodar dicitrate. The accumulation of the substrate is measured, and the IC₅₀ for inhibition is calculated. These assays confirm the compound's mechanism of action as an ABC transporter inhibitor.
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| Cell Assay |
In vitro cell-based assays for biricodar dicitrate evaluate its effects on drug accumulation and cytotoxicity. Drug-resistant cancer cells are cultured and treated with biricodar dicitrate in the presence of chemotherapeutic agents. Intracellular drug accumulation is measured using fluorescence or mass spectrometry. Cell viability is assessed using MTT or CellTiter-Glo assays. These assays confirm the compound's functional activity in reversing multidrug resistance.
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| Animal Protocol |
In vivo animal experiments for biricodar dicitrate have been conducted in mouse xenograft models of drug-resistant cancer. Tumor-bearing mice are treated with biricodar dicitrate in combination with chemotherapeutic agents. Tumor growth is monitored by caliper measurements, and tumor growth inhibition is calculated. Pharmacokinetic studies are conducted to determine the compound's half-life, clearance, and tissue distribution. Comprehensive in vivo studies are available from clinical development.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) data for biricodar dicitrate are available from preclinical and clinical studies. The compound has a molecular weight of 786.78 g/mol. It is typically administered intravenously. The compound's half-life, bioavailability, and excretion profile have been characterized in the context of its development for reversing multidrug resistance. Comprehensive PK data are available from pharmaceutical studies.
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| Toxicity/Toxicokinetics |
The toxicity profile of biricodar dicitrate has been evaluated in preclinical and clinical studies. The compound is generally well-tolerated at therapeutic doses. Common side effects may include gastrointestinal disturbances and myelosuppression. The compound should be used under medical supervision. Comprehensive toxicological studies are available from clinical development. Biricodar dicitrate is for research use only.
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| References | |
| Additional Infomation |
Biricodar dicitrate is a dicitrate of a synthetic piperidine ester derivative with potential chemosensitizing activity. Biricodar directly binds to and inhibits the activity of the plasma membrane drug efflux pump P-glycoprotein (P-gp) and multidrug resistance protein 1 (MRP-1), which may lead to increased intracellular accumulation and retention of cytotoxic drugs.
Biricodar dicitrate (VX-710 dicitrate) is a small-molecule inhibitor of P-glycoprotein (P-gp) and other ABC transporters that mediate multidrug resistance. It has a molecular formula of C₃₈H₄₆N₂O₁₆ and a molecular weight of 786.78 g/mol. Biricodar dicitrate inhibits the efflux of chemotherapeutic agents from cancer cells, reversing multidrug resistance and restoring chemotherapy efficacy. The compound has been studied for its potential in combination with chemotherapy for drug-resistant cancers. |
| Molecular Formula |
C34H41N3O7
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|---|---|
| Molecular Weight |
603.705
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| Exact Mass |
603.294
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| CAS # |
174254-13-8
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| Related CAS # |
159997-94-1;174254-13-8 (dicitrate);
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| PubChem CID |
9963148
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
4.961
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| Hydrogen Bond Donor Count |
8
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| Hydrogen Bond Acceptor Count |
23
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| Rotatable Bond Count |
26
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| Heavy Atom Count |
70
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| Complexity |
1090
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| Defined Atom Stereocenter Count |
1
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| SMILES |
COC1=C(C(=CC(=C1)C(=O)C(=O)N2CCCC[C@H]2C(=O)OC(CCCC3=CN=CC=C3)CCCC4=CN=CC=C4)OC)OC.C(C(=O)O)C(CC(=O)O)(C(=O)O)O.C(C(=O)O)C(CC(=O)O)(C(=O)O)O
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| InChi Key |
VDMKJSJJXQDICL-ZXVJYWQYSA-N
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| InChi Code |
InChI=1S/C34H41N3O7.2C6H8O7/c1-41-29-20-26(21-30(42-2)32(29)43-3)31(38)33(39)37-19-5-4-16-28(37)34(40)44-27(14-6-10-24-12-8-17-35-22-24)15-7-11-25-13-9-18-36-23-25;2*7-3(8)1-6(13,5(11)12)2-4(9)10/h8-9,12-13,17-18,20-23,27-28H,4-7,10-11,14-16,19H2,1-3H3;2*13H,1-2H2,(H,7,8)(H,9,10)(H,11,12)/t28-;;/m0../s1
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| Chemical Name |
1,7-dipyridin-3-ylheptan-4-yl (2S)-1-[2-oxo-2-(3,4,5-trimethoxyphenyl)acetyl]piperidine-2-carboxylate;2-hydroxypropane-1,2,3-tricarboxylic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6564 mL | 8.2821 mL | 16.5642 mL | |
| 5 mM | 0.3313 mL | 1.6564 mL | 3.3128 mL | |
| 10 mM | 0.1656 mL | 0.8282 mL | 1.6564 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.
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