| CAS NO: | 121584-18-7 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 20mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| Physical Appearance | White solid |
| Storage | Store at -20°C |
| M.Wt | 1214.62 |
| Cas No. | 121584-18-7 |
| Formula | C63H111N11O12 |
| Synonyms | PSC 833;PSC-833;PSC833 |
| Solubility | insoluble in H2O; ≥15.77 mg/mL in DMSO; ≥46.8 mg/mL in EtOH |
| Chemical Name | PSC 833;PSC-833;PSC833 |
| Canonical SMILES | CC=CCC(C)C(=O)C1C(=O)NC(C(=O)N(CC(=O)N(C(C(=O)NC(C(=O)N(C(C(=O)NC(C(=O)NC(C(=O)N(C(C(=O)N(C(C(=O)N(C(C(=O)N1C)C(C)C)C)CC(C)C)C)CC(C)C)C)C)C)CC(C)C)C)C(C)C)CC(C)C)C)C)C(C)C |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次半岛bd体育手机客户端 溶解度各有差异，仅做参考。若实验所需浓度过大至半岛bd体育手机客户端 溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
Valspodar是一种有效的P-糖蛋白（P-gp）抑制剂，广泛用于临床前和临床研究[1]。
P-gp是位于细胞膜上的跨膜糖蛋白，其分布广泛，主要在某些细胞类型中表达，包括肝、结肠、肾和胰腺。P-gp也被称为多药耐药蛋白1（MDR1），将外来物质泵出细胞。P-gp减少细胞毒性药物净吸收进入细胞，介导这些药物流出细胞，这种作用是ATP依赖性的。P-gp在某些癌症中过表达。P-gp在介导抗癌药物的耐受性和减少多药耐药性癌细胞中药物的积累方面具有重要作用[1]。
Valspodar可扭转对mitoxantrane的耐受性，这是由于P-gp的表达。在用3 mg/ml PSC预处理的 MDA-MB-435mdr 细胞中，mitoxantrane的IC50值从1.6 ± 0.13 μM降至0.4 ± 0.02 μM。Valspodar通过减少药物外流，增加mitoxantrone的细胞净吸收，从而增加mitoxantrane的细胞内积累[1]。在T47D/TAMR-6细胞中，doxorubicin与valspodar治疗比doxorubicin单独治疗具有显著更高的细胞毒性。Doxorubicin与valspodar共同封装可呈现有前途的抗癌效应[2]。Valspodar可被快速吸收，在口服后的2小时内达到峰值。在大鼠中，valspodar具有分布范围广，低肝排出和42.8％的平均生物利用度等特性[3]。
参考文献：
[1]. Shen F, Bailey BJ, Chu S, Bence AK, Xue X, Erickson P, Safa AR, Beck WT, Erickson LC: Dynamic assessment of mitoxantrone resistance and modulation of multidrug resistance by valspodar (PSC833) in multidrug resistance human cancer cells. J Pharmacol Exp Ther 2009, 330(2):423-429.
[2]. Bajelan E, Haeri A, Vali AM, Ostad SN, Dadashzadeh S: Co-delivery of doxorubicin and PSC 833 (Valspodar) by stealth nanoliposomes for efficient overcoming of multidrug resistance. J Pharm Pharm Sci 2012, 15(4):568-582.
[3]. Binkhathlan Z, Hamdy DA, Brocks DR, Lavasanifar A: Pharmacokinetics of PSC 833 (valspodar) in its Cremophor EL formulation in rat. Xenobiotica 2010, 40(1):55-61.
| Cell experiment:[1] | |
Cell lines |
MDR-P388 murine leukemia cells |
Reaction Conditions |
26 ~ 70 μM valspodar |
Applications |
Valspodar restored sensitivity of MDR-P388 murine leukemia cells to cytostatic agents when used at concentrations of 70, 33, 45, 34, and 26 nM in combination with colchicine, vincristine, daunomycin, doxorubicin, and etoposide, respectively. |
| Animal experiment:[1] | |
Animal models |
MDR-P388 tumor-bearing B6D2FI mice |
Dosage form |
25 and 50 mg/kg Administered orally 4h before each doxorubicin treatment |
Applications |
The combined therapy resulted in a marked valspodar dose-dependent prolongation of the mean survival time (MST) of the MDR-P388 tumor-bearing mice. At the doses of 25 and 50 mg/kg, valspodar could extent the MST to 28.7 and 38.8 days, respectively, when administered 4 h before each doxorubicin intraperitoneal injection. Thus, valspodar could serve as a very promising chemosensitizer. |
Note |
The technical data provided above is for reference only. |
References: 1. Boesch D, Gavériaux C, Jachez B, et al. In vivo circumvention of P-glycoprotein-mediated multidrug resistance of tumor cells with SDZ PSC 833. Cancer Research, 1991, 51(16): 4226-4233. |
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