Biricodar dicitrate

SKU: orb1741435

Description

Biricodar dicitrate (VX-710) is a potent, non-cytotoxic multidrug resistance (MDR) inhibitor. It is widely used in prostate cancer research to sensitize resistant tumor cells to chemotherapeutic agents in both in vitro and in vivo experimental models.

Research Area

Neuroscience, Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 174254-13-8
• MW: 987.95
• Purity: 99.78% (May vary between batches)
• Formula: C₄₆H₅₇N₃O₂₁
• SMILES: OC(CC(C(O)=O)(O)CC(O)=O)=O.O=C(C1=CC(OC)=C(C(OC)=C1)OC)C(N2[C@@H](CCCC2)C(OC(CCCC3=CN=CC=C3)CCCC4=CN=CC=C4)=O)=O.OC(CC(C(O)=O)(O)CC(O)=O)=O
• Target: P-gp,AChR,NF-κB

Bioactivity

• Target IC50:
  P-gp:0.75uM(EC50)|Iodoaryl azido-prazosin:0.55 μM(EC50)
• In Vitro:
  Biricodar exhibits activity against both P-glycoprotein (Pgp) and MRP-1, enhancing drug uptake and retention while reversing drug resistance mediated by wild-type BCRP (BCRPR482). In Pgp-expressing 8226/Dox6 cells, biricodar increases the uptake of mitoxantrone and daunorubicin by 55% and 100%, respectively. It enhances their retention by 100% and 60%, respectively, and boosts their cytotoxicity by 3.1- and 6.9-fold, respectively. Furthermore, biricodar has similar effects on HL60/Adr cells (MRP-1) and 8226/MR20 cells (BCRP(R482)), but it has little impact on MCF7 AdVP3000 cells (BCRP(R482T)). VX-710, a non-macrocyclic pipecolinate derivative binding to the FK506 receptor protein, has been shown to restore sensitivity in various multidrug-resistant cells, including myeloma, melanoma, carcinoma, and leukemia. Additionally, biricodar effectively inhibits the photoaffinity labeling of P-glycoprotein by [3H]azidopine or [125I]iodoaryl azido-prazosin, with EC50 values of 0.75 and 0.55 μM.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Biricodar, Biricodar Dicitrate, NF-kB, NFkB, NFκB, NF-κB, α4β2 nAChR, VX710, VX-710, VX 710-3

Compound Identifiers

PubChem CID

9963148