2. Membrane Transporter/Ion Channel
  3. P-glycoprotein
  4. Biricodar

Biricodar (VX-710) is a modulator of P-glycoprotein and MRP-1; shows effective chemosensitizing activity in multidrug resistant cells.

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

Biricodar Chemical Structure

Biricodar Chemical Structure

CAS No. : 159997-94-1

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Based on 1 publication(s) in Google Scholar

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Top Publications Citing Use of Products

1 Publications Citing Use of MCE Biricodar

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Biricodar (VX-710) is a modulator of P-glycoprotein and MRP-1; shows effective chemosensitizing activity in multidrug resistant cells.

In Vitro

Biricodar shows activity against both P-glycoprotein (Pgp) and MRP-1 and also has activity in increasing drug uptake and retention and reversing drug resistance mediated by wild-type BCRP (BCRPR482). In 8226/Dox6 cells (Pgp), biricodar increases mitoxantrone and daunorubicin uptake by 55 and 100%, respectively, increases their retention by 100 and 60%, respectively, and increases their cytotoxicity 3.1- and 6.9-fold, respectively. Biricodar also increases the uptake, retention and cytotoxicity in HL60/Adr (MRP-1) and 8226/MR20 cells (BCRP(R482)), but has little effect in MCF7 AdVP3000 cells (BCRP(R482T))[1]. VX-710 is a non-macrocyclic pipecolinate derivative which binds the FK506 receptor protein. VX-710 has been shown to restore sensitivity in a range of multidrug-resistant cells, including myeloma, melanoma, carcinoma and leukaemia[2]. Biricodar effectively inhibits photoaffinity labeling of P-glycoprotein by [3H]azidopine or [125I]iodoaryl azido-prazosin with EC50 values of 0.75 and 0.55 μM[3].

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

603.71

Formula

C34H41N3O7
CAS No.
Appearance

Oil

Color

Light yellow to yellow

SMILES

O=C([C@H]1N(C(C(C2=CC(OC)=C(OC)C(OC)=C2)=O)=O)CCCC1)OC(CCCC3=CC=CN=C3)CCCC4=CC=CN=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (165.64 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Purity & Documentation
References
Cell Assay
[1]

To study cytotoxicity in suspension cell lines, cells are plated in 96-well tissue culture plates at a density of 10,000 cells/well in RPMI 1640 supplemented with 10% FCS, 2 mM l-glutamine, 20 units/mL penicillin, and 20 μg/mL streptomycin. Drug is added to the culture medium to achieve final concentrations of 0.3 nM to 10 μM, with half-log increments, with and without biricodar at a final concentration of 2.5 μM. The final volume of medium per well is 100 μL. Cells are incubated for 96 h at 37°C in a fully humidified atmosphere of 5% CO2 in air. Cell growth is assessed by the WST-1 colorimetric assay[1].

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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6564 mL 8.2821 mL 16.5642 mL 41.4106 mL
5 mM 0.3313 mL 1.6564 mL 3.3128 mL 8.2821 mL
10 mM 0.1656 mL 0.8282 mL 1.6564 mL 4.1411 mL
15 mM 0.1104 mL 0.5521 mL 1.1043 mL 2.7607 mL
20 mM 0.0828 mL 0.4141 mL 0.8282 mL 2.0705 mL
25 mM 0.0663 mL 0.3313 mL 0.6626 mL 1.6564 mL
30 mM 0.0552 mL 0.2761 mL 0.5521 mL 1.3804 mL
40 mM 0.0414 mL 0.2071 mL 0.4141 mL 1.0353 mL
50 mM 0.0331 mL 0.1656 mL 0.3313 mL 0.8282 mL
60 mM 0.0276 mL 0.1380 mL 0.2761 mL 0.6902 mL
80 mM 0.0207 mL 0.1035 mL 0.2071 mL 0.5176 mL
100 mM 0.0166 mL 0.0828 mL 0.1656 mL 0.4141 mL
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Biricodar Related Classifications

Keywords:

Biricodar159997-94-1VX-710VX710VX 710P-glycoproteinP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243Inhibitorinhibitorinhibit

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