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Biricodar

Cat. No. M1853

Biricodar Structure

Synonym: VX-710, Incel

Size Price Availability
10mg USD 380 Out of stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

Protocol
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 603.7
Formula C34H41N3O7
CAS Number 174254-13-8
Purity >99%
Solubility DMSO
Storage at -20°C
References

P-glycoprotein antagonists confer synergistic sensitivity to short-chain ceramide in human multidrug-resistant cancer cells.
Chapman et al. Exp Cell Res. 2011 Jul 15;317(12):1736-45. PMID: 21396934.

Inhibition of antibiotic efflux in bacteria by the novel multidrug resistance inhibitors biricodar (VX-710) and timcodar (VX-853).
Mullin et al. Antimicrob Agents Chemother. 2004 Nov;48(11):4171-6. PMID: 15504837.

VX-710 (biricodar) increases drug retention and enhances chemosensitivity in resistant cells overexpressing P-glycoprotein, multidrug resistance protein, and breast cancer resistance protein.
Minderman et al. Clin Cancer Res. 2004 Mar 1;10(5):1826-34. PMID: 15014037.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Biricodar, VX-710, Incel supplier, P-gp, inhibitors

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