伐司扑达
伐司扑达结构式
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常用名 | 伐司扑达 | 英文名 | Valspodar |
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| CAS号 | 121584-18-7 | 分子量 | 1214.622 | |
| 密度 | 1.0±0.1 g/cm3 | 沸点 | 1290.1±65.0 °C at 760 mmHg | |
| 分子式 | C63H111N11O12 | 熔点 | N/A | |
| MSDS | 中文版 美版 | 闪点 | 734.0±34.3 °C |
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Potential role of acid ceramidase in conversion of cytostatic to cytotoxic end-point in pancreatic cancer cells.
Cancer Chemother. Pharmacol. 71(3) , 635-45, (2013) Acid ceramidase (AC) occupies an important place in the control of cancer cell proliferation. We tested the influence of AC inhibition on the effects of PSC 833, a P-glycoprotein antagonist with potent ceramide-generating capacity, to determine whether AC cou... |
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A tamoxifen derivative, N,N-diethyl-2-[4-(phenylmethyl) phenoxy] ethanamine, selectively targets P-glycoprotein-positive multidrug resistant Chinese hamster cells.
Biochem. Pharmacol. 90(2) , 107-14, (2014) DPPE, a tamoxifen derivative with antihistamine activity, was previously shown to potentiate the toxicity of chemotherapeutic drugs. Recently, a Phase III clinical study using doxorubicin with DPPE demonstrated significant increase in the overall survival of ... |
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Rapid detection of ABC transporter interaction: potential utility in pharmacology.
J. Pharmacol. Toxicol. Methods 63(3) , 217-22, (2011) The ATP-binding cassette (ABC) transporters P-glycoprotein (P-gp/ABCB1), multidrug resistance-associated protein 1 (MRP1/ABCC1), and breast cancer resistance protein (BCRP/ABCG2) are known to transport a wide range of structurally diverse compounds. Their hig... |
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Pituitary homeobox 2 (PITX2) protects renal cancer cell lines against doxorubicin toxicity by transcriptional activation of the multidrug transporter ABCB1.
Int. J. Cancer 133(3) , 556-67, (2013) The multidrug resistance (MDR) P-glycoprotein ABCB1 plays a major role in MDR of malignant cells and is regulated by various transcription factors, including Wnt/β-catenin/TCF4. The transcription factor PITX2 (Pituitary homeobox-2) is essential for embryonic ... |
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Quinidine as an ABCB1 probe for testing drug interactions at the blood-brain barrier: an in vitro in vivo correlation study.
J. Biomol. Screen. 16(8) , 886-94, (2011) This study provides evidence that quinidine can be used as a probe substrate for ABCB1 in multiple experimental systems both in vitro and in vivo relevant to the blood-brain barrier (BBB). The combination of quinidine and PSC-833 (valspodar) is an effective t... |
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Regional absorption of fexofenadine in rat intestine
Eur. J. Pharm. Sci. 41(5) , 670-4, (2010) Purpose Expression of Pgp along the GI-tract of rats increases towards distal segments. We assessed the in vivo relevance by determining the absorption of fexofenadine from proximal and distal parts of rat intestine. Since it has been reported that fexofenadi... |
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Co-delivery of doxorubicin and PSC 833 (Valspodar) by stealth nanoliposomes for efficient overcoming of multidrug resistance.
J. Pharm. Pharm. Sci. 15(4) , 568-82, (2012) This study was aimed at developing co-encapsulated stealth nanoliposomes containing PSC 833, an efficient MDR modulator, and doxorubicin (DOX) in order to increase the effectiveness and decrease adverse effects of the anticancer drug.In attempt to increase th... |
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Identification and characterization of ABCB1-mediated and non-apoptotic sebum secretion in differentiated hamster sebocytes.
Biochim. Biophys. Acta 1811(12) , 1090-6, (2011) Sebaceous glands secrete sebum onto the skin surface in a holocrine manner and as such a thin lipid layer is formed as a physiological barrier. In the present study, extracellular level of triacylglycerols (TG), a major sebum component, as well as intracellul... |
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P-glycoprotein modulation by valspodar and cyclosporin does not increase tumor uptake of doxorubicin administered via isolated lung perfusion to rats bearing sarcoma lung metastases.
Anticancer Res. 31(6) , 2121-8, (2011) Isolated lung perfusion (ILP) with doxorubicin allows a regional increase in drug exposure while sparing unaffected tissues, but clinical results have so far been disappointing, presumably in part because of the limited tumor penetration of doxorubicin. The a... |
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P-glycoprotein is functionally expressed in the placenta-derived bovine caruncular epithelial cell line 1 (BCEC-1).
Placenta 32(2) , 146-52, (2011) Drug treatment is critical in pregnant cows due to the possibility of a maternal-to-fetal drug transfer across the placenta. Since the (syn)epitheliochorial bovine placental barrier includes an intact uterine epithelium, which in general limits drug transfer ... |