Biricodar
Based on 1 publication(s) in Google Scholar
Biricodar (VX-710) is a modulator of P-glycoprotein and MRP-1; shows effective chemosensitizing activity in multidrug resistant cells.
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- Purity: 99.31%
- CAS No.: 159997-94-1
- 화학식: C34H41N3O7
- 분자량:603.71
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보관:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Biricodar
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Biological Activity
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.
Chemical Information
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CAS No. 159997-94-1
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Appearance Oil
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분자량 603.71
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화학식 C34H41N3O7
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Color Light yellow to yellow
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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
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Synonyms
VX-710
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
용액&용해도
DMSO : 125 mg/mL (207.05 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
순도&문서
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Data Sheet (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Minderman H, et al. VX-710 (biricodar) increases drug retention and enhances chemosensitivity in resistant cells overexpressing P-glycoprotein, multidrug resistance protein, and breast cancer resistance protein. Clin Cancer Res. 2004 Mar 1;10(5):1826-34. [Content Brief]
[2]. Yanagisawa T, et al. BIRICODAR (VX-710; Incel): an effective chemosensitizer in neuroblastoma. Br J Cancer. 1999 Jun;80(8):1190-6. [Content Brief]
[3]. Germann UA, et al. Cellular and biochemical characterization of VX-710 as a chemosensitizer: reversal of P-glycoprotein-mediated multidrug resistance in vitro. Anticancer Drugs. 1997 Feb;8(2):125-40. [Content Brief]
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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