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Biricodar (VX-710, Incel) is a clinically applicable modulator of P-glycoprotein (Pgp) with potential chemosensitizing activity. Biricodar blood concentration at the time of mitoxantrone administration averaged 4.52 microg/ml. In 8226/Dox6 cells (Pgp), Biricodar (VX-710) increased mitoxantrone and daunorubicin uptake by 55 and 100%, respectively, increased their retention by 100 and 60%, respectively, and increased their cytotoxicity 3.1- and 6.9-fold, respectively. Biricodar (VX-710) modulates Pgp, MRP-1, and BCRP(R482), and has potential as a clinical broad-spectrum MDR modulator in malignancies such as the acute leukemias in which these proteins are expressed.
| Cell Experiment | |
|---|---|
| Cell lines | HL60 cells line |
| Preparation method | Cytotoxicity Assays. To study cytotoxicity in suspension cell lines, cells were 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 was added to the culture medium to achieve final concentrations of 0.3 nm to 10 μm, with half-log increments, with and without VX-710 at a final concentration of 2.5 μM. The final volume of medium per well was 100 μl. Cells were incubated for 96 h at 37°C in a fully humidified atmosphere of 5% CO2 in air. Cell growth was assessed by the WST-1 colorimetric assay (Roche Diagnostics GmbH, Mannheim, Germany; Ref. 29 ), performed according to the manufacturer’s instructions. Briefly, 10 μl of WST-1 were added to each well, and culture plates were returned to the incubator for an additional 4 h. Subsequently, the absorbance at 450 nm (A450) and 600 nm (A600, background) was read for each well using a Microtek multiwell plate reader. Each drug exposure condition was assessed in quadruplicate. |
| Concentrations | 2.5 μM |
| Incubation time | 96 h |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 603.7 |
| Formula | C34H41N3O7 |
| CAS Number | 174254-13-8 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related P-glycoprotein Products |
|---|
| Zosuquidar
Zosuquidar (LY335979) is a P-glycoprotein (P-gp) inhibitor (Ki=59 nM). |
| Tariquidar dimesylate
Tariquidar dimesylate (XR9576 dimesylate) is a P-glycoprotein (P-gp) inhibitor. |
| Tariquidar dihydrochloride
Tariquidar dihydrochloride (XR9576 dihydrochloride) is a potent and specific inhibitor of P-glycoprotein (P-gp) with the high affinity (Kd=5.1 nM). |
| Reversin 121
Reversin 121 is a P-glycoprotein inhibitor. |
| Reversin 205
Reversin 205 ([Boc-Glu(Obzl)]2-Lys-Ome) is a P-glycoprotein (ABCB1) inhibitor. |
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