Biricodar (VX-710)
(Synonyms: VX-710) 目录号 : GC33338
Biricodar (VX-710) (VX-710) 是 P-糖蛋白和 MRP-1 的调节剂；在多重耐药细胞中显示出有效的化学增敏活性。
Cas No.:159997-94-1
Sample solution is provided at 25 µL, 10mM.
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Biricodar (VX-710) is a modulator of P-glycoprotein and MRP-1; shows effective chemosensitizing activity in multidrug resistant cells.
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 (BCRPR482). 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))[1]. 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[2]. 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].
[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.
Cell experiment: | To study cytotoxicity in suspension cell lines, cells are 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 is added to the culture medium to achieve final concentrations of 0.3 nM to 10 μM, with half-log increments, with and without biricodar at a final concentration of 2.5 μM. The final volume of medium per well is 100 μL. Cells are incubated for 96 h at 37°C in a fully humidified atmosphere of 5% CO2 in air. Cell growth is assessed by the WST-1 colorimetric assay[1]. |
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. | |
| Cas No. | 159997-94-1 | SDF | |
| 别名 | VX-710 | ||
| Canonical SMILES | O=C([C@H]1N(C(C(C2=CC(OC)=C(OC)C(OC)=C2)=O)=O)CCCC1)OC(CCCC3=CC=CN=C3)CCCC4=CC=CN=C4 | ||
| 分子式 | C34H41N3O7 | 分子量 | 603.71 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.6564 mL | 8.2821 mL | 16.5642 mL |
| 5 mM | 0.3313 mL | 1.6564 mL | 3.3128 mL |
| 10 mM | 0.1656 mL | 0.8282 mL | 1.6564 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet