159997-94-1
基本信息
VX-710(biricodar)
2-Piperidinecarboxylic acid, 1-[2-oxo-2-(3,4,5-trimethoxyphenyl)acetyl]-, 4-(3-pyridinyl)-1-[3-(3-pyridinyl)propyl]butyl ester, (2S)-
物理化学性质
| 沸点 | 752.1±70.0 °C(Predicted) |
| 密度 | 1.195±0.06 g/cm3(Predicted) |
| 储存条件 | -20°C储存 |
| 溶解度 | 溶于二甲基亚砜 |
| 酸度系数(pKa) | 5.80±0.10(Predicted) |
| 形态 | Oil |
| 颜色 | Colorless to light yellow |
常见问题列表
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 (BCRPR 482 ). 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)). 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. Biricodar effectively inhibits photoaffinity labeling of P-glycoprotein by [ 3 H]azidopine or [ 125 I]iodoaryl azido-prazosin with EC 50 values of 0.75 and 0.55 μM.