Fenretinide
作者：齐岳
发布时间：2023-09-08
09:07:50
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产品名称：Fenretinide
产品描述：
| 产品描述 | Fenretinide is an orally-active synthetic retinoid derivative with potential antineoplastic and chemopreventive activities. |
| 体外活性 | Fenretinide exerts not just acute but also long term antitumor activity in selected T-ALL cell lines. Fenretinide inhibits DES activity in CCRF-CEM leukemia cells in a dose and time-dependent manner which leading to a concomitant increase of the endogenous cellular dhCer content. Fenretinide (3 μM)-induced dhCer accumulation in both CCRF-CEM and Jurkat cells[1]. Ceramide inhibition with fenretinide protects insulin signaling. Fenretinide prevents lipid-induced reductions in insulin-stimulated glucose uptake[2]. Fenretinide inhibits OVCAR-5 cell proliferation and viability at concentrations higher than 1 microM, with 70-90% growth inhibition at 10 microM. Fenretinide (1 microM) significantly inhibits OVCAR-5 invasion after 3 days preincubation. Endothelial cells treated with 1 microM 4-HPR fails to form tubes, but forms small cellular aggregates[4]. |
| 体内活性 | Fenretinide (10 mg/kg, i.p.) selectively inhibits ceramide accumulation HFD-fed male C57Bl/6 mice. Fenretinide treatment improves glucose tolerance and insulin sensitivity as determined by both glucose and insulin tolerance tests[2]. The addition of 25 mg/kg ketoconazole to Fenretinide increased 4-HPR plasma levels in NOD/SCID mice[3]. |
| 细胞实验 | Fenretinide is dissolved in DMSO. Standard XTT assay is used to determine cell viability. For fenretinide-only treatments, cells are plated in 96-well plates at 750,000 cells/mL and 100 μL/well. After 4 h, treatments are added on 50 μL/well obtaining a final density of 500,000 cells/mL and final volume of 150 μL/well. Four replicates are used per experimental condition. XTT reagent mixture is added 4 h before the end of selected treatment period and absorbance at 490 nm is determined per each well. A slightly modified protocol is used for analysis of the effect of myriocin (final concentration of 100 nM) or antioxidant on Fenretinide treatment. Briefly, cells are seeded on 60 mm culture dishes and myriocin or antioxidants added after 4 h. Fenretinide treatment is added 2 h later and cells are plated in quadruplicates in 96 well plates (150 μL/well). |
| 别名 | 4-HPR, 4-hydroxy(phenyl)retinamide, 芬维A胺, MK-4016 |
| 分子量 | 391.55 |
| 分子式 | C26H33NO2 |
| CAS No. | 65646-68-6 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 39.2 mg/mL(100 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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