| Description | Biricodar is a P-glycoprotein and MRP-1 modulator. |
| In vitro | Biricodar shows activity against both P-glycoprotein (Pgp) and MRP-1. It also has activity in increasing drug uptake and retention and reversing drug resistance mediated by wild-type BCRP (BCRPR482). Biricodar also increases the uptake, retention and cytotoxicity in HL60/Adr (MRP-1) and 8226/MR20 cells (BCRP(R482)). And it has little effect in MCF7 AdVP3000 cells (BCRP(R482T))[1]. 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]. 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. VX-710 is a non-macrocyclic pipecolinate derivative which binds the FK506 receptor protein and it has been shown to restore sensitivity in a range of multidrug-resistant cells, including myeloma, melanoma, carcinoma and leukaemia[2]. |
| Synonyms | VX-710 |
| molecular weight | 603.71 |
| Molecular formula | C34H41N3O7 |
| CAS | 159997-94-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 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. 2. Yanagisawa T, et al. BIRICODAR (VX-710; Incel): an effective chemosensitizer in neuroblastoma. Br J Cancer. 1999 Jun;80(8):1190-6. 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. |