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Fenretinide

Fenretinide

产品编号 T1872   CAS 65646-68-6
别名: 4-HPR, MK-4016, 芬维A胺, 4-hydroxy(phenyl)retinamide

Fenretinide (4-HPR) 是一种可口服的合成类维生素 A 衍生物,具有潜在的抗肿瘤和化学预防活性。

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Fenretinide Chemical Structure
Fenretinide, CAS 65646-68-6
规格 价格/CNY 货期 数量
5 mg ¥ 229 现货
10 mg ¥ 373 现货
50 mg ¥ 648 现货
100 mg ¥ 995 现货
200 mg ¥ 1,498 现货
1 mL * 10 mM (in DMSO) ¥ 385 现货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
Venetoclax限时半价
MG-132限时半价
产品目录号及名称: Fenretinide (T1872)
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纯度: 99.72%
纯度: 98%
纯度: 98%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Fenretinide (4-HPR) 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, MK-4016, 芬维A胺, 4-hydroxy(phenyl)retinamide
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 1 year

溶解度

DMSO: 39.2 mg/mL(100 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.554 mL 12.7698 mL 25.5395 mL 63.8488 mL
5 mM 0.5108 mL 2.554 mL 5.1079 mL 12.7698 mL
10 mM 0.2554 mL 1.277 mL 2.554 mL 6.3849 mL
20 mM 0.1277 mL 0.6385 mL 1.277 mL 3.1924 mL
50 mM 0.0511 mL 0.2554 mL 0.5108 mL 1.277 mL
100 mM 0.0255 mL 0.1277 mL 0.2554 mL 0.6385 mL

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TargetMol Library Books参考文献

1. Apraiz, Aintzane., et al. Dihydroceramide accumulation and reactive oxygen species are distinct and nonessential events in 4-HPR-mediated leukemia cell death. Biochemistry and Cell Biology (2012), 90(2), 209-223. 2. Bikman, Benjamin T., et al. Fenretinide Prevents Lipid-induced Insulin Resistance by Blocking Ceramide Biosynthesis. Journal of Biological Chemistry (2012), 287(21), 17426-17437. 3. Cooper JP, et al. Fenretinide metabolism in humans and mice: utilizing pharmacological modulation of its metabolic pathway to increase systemic exposure. Br J Pharmacol. 2011 Jul;163(6):1263-75. 4. Golubkov V, et al. Action of fenretinide (4-HPR) on ovarian cancer and endothelial cells. Anticancer Res. 2005 Jan-Feb;25(1A):249-53.
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相关化合物库

该产品包含在如下化合物库中:
抗癌药物库 药物功能重定位化合物库 抗癌活性化合物库 抗癌临床化合物库 抗乳腺癌化合物库 口服活性化合物库 免疫/炎症分子化合物库 抗衰老化合物库 儿童药物库 NO PAINS 化合物库

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母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Fenretinide 65646-68-6 Autophagy Metabolism Retinoid Receptor 4-HPR Retinoic acid receptors MK4016 MK-4016 Inhibitor 芬维A胺 RAR/RXR 4-hydroxy(phenyl)retinamide inhibit MK 4016 Retinoid X receptors inhibitor

 

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