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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEOxyphenisatineCat. No.: HY-B2102CAS No.: 125-13-3Synonyms: Oxyphenisatin分式: CHNO分量: 317.34作靶点: Others作通路: Others储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 28 mg/mL (88.23 mM)* means so

2、luble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.1512 mL 15.7560 mL 31.5119 mL5 mM 0.6302 mL 3.1512 mL 6.3024 mL10 mM 0.3151 mL 1.5756 mL 3.1512 mL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,并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Oxyphenisatine (Oxyphenisatin)种泻药。 Oxyphenisatin ace

3、tate是具有抗癌活性的氧联苯沙星的前体药。体外研究Oxyphenisatin has been shown to have antiproliferative activity. Oxyphenisatin acetate (OXY, NSC 59687) isthe pro-drug of oxyphenisatin. OXY inhibits the growth of the breast cancer cell lines MCF7, T47D, HS578T,1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEand MDA-MB-46

4、8 (IC50=0.8, 0.6, 2.1, 1.8 M). This effect is associated with selective inhibition of translationaccompanied by rapid phosphorylation of the nutrient sensing eIF2 kinases, GCN2 and PERK 1.体内研究 Toxicity studies demonstrate that mice tolerate IP administration of OXY at 300 mg/kg once daily or 200mg/k

5、g twice daily. Administration of OXY at 300 mg/kg IP once daily for 10 days results in significantlysmaller tumors from day 33 to day 52 1.PROTOCOLAnimal Mice: When tumors reaches 120 mg, mice are randomized into treatment groups and therapy is initiated.Administration 1 Asimple toxicity assessment

6、to determine tolerability to OXY is conducted by administering singleintraperitoneal (IP) doses of compound at 100, 200, and 400 mg/kg. The mice were observed for adverseeffects for 14 days postdose 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFE

7、RENCES1. Morrison BL, et al. Oxyphenisatin acetate (NSC 59687) triggers a cell starvation response leading to autophagy, mitochondrialdysfunction, and autocrine TNF-mediated apoptosis. Cancer Med. 2013 Oct;2(5):687-700.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use o

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