Fenretinide (Synonyms: 芬维A胺; 4-HPR)

目录号: HY-15373 纯度: 98.83%: Data Sheet SDS COA 产品使用指南
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Fenretinide (4-HPR) 是一种合成的类维生素A衍生物，能够结合视黄酸受体 (RAR) 诱导细胞死亡。

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Fenretinide Chemical Structure

CAS No. : 65646-68-6

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥500	In-stock
1 mg	￥140	In-stock
5 mg	￥281	In-stock
10 mg	￥450	In-stock
25 mg	￥630	In-stock
50 mg	￥780	In-stock
100 mg	￥1250	In-stock
200 mg		询价
500 mg		询价

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Customer Review

Other Forms of Fenretinide:

Fenretinide (Standard) 询价

MCE 顾客使用本产品发表的 9 篇科研文献

IHC

: Fenretinide purchased from MCE. Usage Cited in: Oncol Rep. 2018 Jul;40(1):518-526. [Abstract]; Western blot analyses reveal that the phosphorylation of p38 is significantly increased. Lane 1, cell control; lane 2, DMSO; lane 3, 5 μM ATRA; lane 4, 10 μM ATRA; lane 5, 5 μM 4-HPR; and lane 6, 10 μM 4-HPR.

: Fenretinide purchased from MCE. Usage Cited in: Cornea. 2018 Dec;37(12):1579-1585. [Abstract]; Compared with infected controls, LOX-1, phosphorylated JNK, and pro-IL-1b protein levels in corneas are significantly lower at 1 day after infection in fenretinide-pretreated mice.

: Fenretinide purchased from MCE. Usage Cited in: Cornea. 2018 Dec;37(12):1579-1585. [Abstract]; BAX, cytochrome c, cleaved-caspase-8, cleaved-caspase-9, and cleaved-caspase-3 protein levels in fenretinide-pretreated mice corneas are found to be significantly increased.

: Fenretinide purchased from MCE. Usage Cited in: Cornea. 2018 Dec;37(12):1579-1585. [Abstract]; Fenretinide pretreatment reduces neutrophils recruitment and MPO activity in the mouse Aspergillus fumigatus keratitis model. Positive staining (green) of NIMP-R14 in the corneas of pretreated mice is indicative of a decreased presence of neutrophils compared with control mice at 1 day after infection.

: Fenretinide purchased from MCE. Usage Cited in: Cornea. 2018 Dec;37(12):1579-1585. [Abstract]; Compared with stimulated controls, LOX-1, JNK, phosphorylated JNK, and pro-IL-1b protein levels in fenretinide-pretreated THP-1 macrophages are significantly lower at 16 hours with A. fumigatus stimulation. JNK was not affected by fenretinide pretreatment.

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Fenretinide (4-HPR) is a synthetic retinoid deriverative, binding to the retinoic acid receptors (RAR) at concentrations necessary to induce cell death.

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
Astrocyte	EC₅₀	2.399 μM Compound: 11	Antiproliferative activity against mouse astrocyte cells by MTT assay Antiproliferative activity against mouse astrocyte cells by MTT assay	[PMID: 17417631]
BHK-21	CC₅₀	31.5 μM Compound: 192	Cytotoxicity against BHK21 cells in presence of ATP by Celltiter-Glo assay Cytotoxicity against BHK21 cells in presence of ATP by Celltiter-Glo assay	[PMID: 28689975]
CWR22R	GI₅₀	3.23 μM Compound: 4-HPR, fenretinide	Growth inhibition of human CWR22Rv1 cells by MTT assay Growth inhibition of human CWR22Rv1 cells by MTT assay	[PMID: 25634130]
Daoy	GI₅₀	5 μM Compound: Fenretinide	Antiproliferative activity against human Daoy cells assessed as inhibition of cell growth incubated for 24 to 96 hrs by MTT assay Antiproliferative activity against human Daoy cells assessed as inhibition of cell growth incubated for 24 to 96 hrs by MTT assay	[PMID: 33636537]
G-401	IC₅₀	5 μM Compound: 1	Cytotoxicity against human G401 cells assessed as cell survival after 3 days by MTS assay Cytotoxicity against human G401 cells assessed as cell survival after 3 days by MTS assay	[PMID: 18556204]
HEK-293T	IC₅₀	18.7 μM Compound: Fenretinide	Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis	[PMID: 23122865]
HEK-293T	IC₅₀	59.9 μM Compound: Fenretinide	Inhibition of mouse Ido1 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis Inhibition of mouse Ido1 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis	[PMID: 23122865]
HuCCT-1	IC₅₀	6 μM Compound: 3, Fenretinide	Cytotoxicity against human HuCCT1 cells after 72 hrs by MTT assay Cytotoxicity against human HuCCT1 cells after 72 hrs by MTT assay	[PMID: 22440084]
LNCaP	GI₅₀	2.69 μM Compound: 4-HPR, fenretinide	Growth inhibition of human LNCAP cells by MTT assay Growth inhibition of human LNCAP cells by MTT assay	[PMID: 25634130]
LNCaP	IC₅₀	7.5 μM Compound: 4-HPR	Growth inhibition of human LNCaP cells after 6 days by MTT assay Growth inhibition of human LNCaP cells after 6 days by MTT assay	[PMID: 15615521]
MCF7	IC₅₀	0.15 μM Compound: 4-HPR	Growth inhibition of human MCF7 cells after 6 days by MTT assay Growth inhibition of human MCF7 cells after 6 days by MTT assay	[PMID: 15615521]
MCF7	GI₅₀	4.65 μM Compound: 4-HPR, fenretinide	Growth inhibition of human MCF7 cells by MTT assay Growth inhibition of human MCF7 cells by MTT assay	[PMID: 25634130]
MDA-MB-231	GI₅₀	11.05 μM Compound: 4-HPR, fenretinide	Growth inhibition of human MDA-MB-231 cells by MTT assay Growth inhibition of human MDA-MB-231 cells by MTT assay	[PMID: 25634130]
MDA-MB-231	IC₅₀	7.7 μM Compound: 4-HPR	Growth inhibition of human MDA-MB-231 cells after 6 days by MTT assay Growth inhibition of human MDA-MB-231 cells after 6 days by MTT assay	[PMID: 15615521]
MDA-MB-468	GI₅₀	6.02 μM Compound: 4-HPR, fenretinide	Growth inhibition of human MDA-MB-468 cells by MTT assay Growth inhibition of human MDA-MB-468 cells by MTT assay	[PMID: 25634130]
Medulloblastoma cell	EC₅₀	0.204 μM Compound: 11	Antiproliferative activity against mouse medulloblastoma cells harboring heterozygous ptch1 gene by MTT assay Antiproliferative activity against mouse medulloblastoma cells harboring heterozygous ptch1 gene by MTT assay	[PMID: 17417631]
MIA PaCa-2	IC₅₀	7 μM Compound: 3, Fenretinide	Cytotoxicity against human MIAPaCa2 cells after 72 hrs by MTT assay Cytotoxicity against human MIAPaCa2 cells after 72 hrs by MTT assay	[PMID: 22440084]
ONS-76	GI₅₀	2 μM Compound: Fenretinide	Antiproliferative activity against human ONS-76 cells assessed as inhibition of cell growth incubated for 24 to 96 hrs by MTT assay Antiproliferative activity against human ONS-76 cells assessed as inhibition of cell growth incubated for 24 to 96 hrs by MTT assay	[PMID: 33636537]
PC-3	GI₅₀	2 μM Compound: 43	Cytotoxicity against human PC3 cells after 72 hrs by MTT assay Cytotoxicity against human PC3 cells after 72 hrs by MTT assay	[PMID: 26780304]
PC-3	GI₅₀	3.54 μM Compound: 4-HPR, fenretinide	Growth inhibition of human PC3 cells by MTT assay Growth inhibition of human PC3 cells by MTT assay	[PMID: 25634130]
PC-3	IC₅₀	3.6 μM Compound: 4-HPR	Growth inhibition of human PC3 cells after 6 days by MTT assay Growth inhibition of human PC3 cells after 6 days by MTT assay	[PMID: 15615521]
SK-BR-3	GI₅₀	3.98 μM Compound: 4-HPR, fenretinide	Growth inhibition of human SKBR3 cells by MTT assay Growth inhibition of human SKBR3 cells by MTT assay	[PMID: 25634130]

体外研究
(In Vitro)

Fenretinide (4-HPR) 在选定的 T-ALL 细胞系中不仅发挥急性抗肿瘤活性，而且发挥长期抗肿瘤活性。Fenretinide 以剂量和时间依赖性方式抑制 CCRF-CEM 白血病细胞中的 DES 活性，导致内源性细胞 dhCer 含量同时增加。Fenretinide (3 μM) 诱导 CCRF-CEM 和 Jurkat 细胞中的 dhCer 积累^[1]。Fenretinide 抑制神经酰胺可保护胰岛素信号传导。Fenretinide 可防止脂质诱导的胰岛素刺激葡萄糖摄取减少^[2]。浓度高于 1 μM 时，Fenretinide 可抑制 OVCAR-5 细胞增殖和活力，浓度为 10 μM 时生长抑制率为 70-90%。Fenretinide (1 μM ) 在 3 天预孵育后显著抑制 OVCAR-5 侵袭。用 1 μM 4-HPR 处理的内皮细胞无法形成管道，但会形成小的细胞聚集体^[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Fenretinide (4-HPR) (10 mg/kg，腹腔注射) 选择性抑制 HFD 喂养的雄性 C57Bl/6 小鼠的神经酰胺蓄积。Fenretinide 治疗可改善葡萄糖耐量和胰岛素敏感性，这通过葡萄糖和胰岛素耐量试验确定^[2]。
在NOD/SCID小鼠中，将 25 mg/kg Ketoconazole 与 Fenretinide 一起添加可提高 Fenretinide 血浆水平^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

391.55

Formula

C₂₆H₃₃NO₂

CAS 号

65646-68-6

性状

固体

颜色

Light yellow to yellow

中文名称

芬维A胺

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : 100 mg/mL (255.40 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5540 mL	12.7698 mL	25.5395 mL
5 mM	0.5108 mL	2.5540 mL	5.1079 mL
10 mM	0.2554 mL	1.2770 mL	2.5540 mL

查看完整储备液配制表

* 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；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

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计算结果

工作液所需浓度 : mg/mL

纯度 & 产品资料

纯度: 98.83%

选择批次：

Data Sheet (627 KB) SDS (419 KB)

COA (278 KB) RP-HPLC (99 KB)

产品使用指南 (1538 KB)

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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Cell Assay ^[1]	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). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Male mice (C57Bl6) are fed a standard chow or a high-fat diet (HFD) from 5 to 17 weeks, at which point half of the HFD-fed mice begin receiving fenretinide in drinking water for 4 weeks. Fenretinide is dissolved in 100% ethanol and diluted in water to 10 μg/mL. Control treatment water receives an equal amount of ethanol (0.5%). FEN water is prepared in low-light conditions and administered in light-protective bottles. Water is replaced every 1-2 days, and no precipitation of FEN is noted at any time. Animal weights are recorded at the beginning and end of the treatment period. Following a 4-week FEN treatment, mice undergo intraperitoneal glucose and insulin tolerance tests. For both tests, mice are fasted for 6 h andreceive an injection of either glucose (1 g/kg of body weight) or insulin (0.75 units/kg of body weight). Blood glucose is determined at the times indicated by the Bayer Contour^® glucose meter, and insulin is measured with the rat/mouse insulin ELISA kit. The insulin resistance index is assessed by using fasting blood glucose and insulin levels to compute the homeostatic model assessment of insulin resistance (HOMA-IR), where a higher number represents greater insulin resistance. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. [Content Brief] [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. [Content Brief] [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. [Content Brief] [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. [Content Brief]

Fenretinide 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.5540 mL	12.7698 mL	25.5395 mL	63.8488 mL
	5 mM	0.5108 mL	2.5540 mL	5.1079 mL	12.7698 mL
	10 mM	0.2554 mL	1.2770 mL	2.5540 mL	6.3849 mL
	15 mM	0.1703 mL	0.8513 mL	1.7026 mL	4.2566 mL
	20 mM	0.1277 mL	0.6385 mL	1.2770 mL	3.1924 mL
	25 mM	0.1022 mL	0.5108 mL	1.0216 mL	2.5540 mL
	30 mM	0.0851 mL	0.4257 mL	0.8513 mL	2.1283 mL
	40 mM	0.0638 mL	0.3192 mL	0.6385 mL	1.5962 mL
	50 mM	0.0511 mL	0.2554 mL	0.5108 mL	1.2770 mL
	60 mM	0.0426 mL	0.2128 mL	0.4257 mL	1.0641 mL
	80 mM	0.0319 mL	0.1596 mL	0.3192 mL	0.7981 mL
	100 mM	0.0255 mL	0.1277 mL	0.2554 mL	0.6385 mL

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Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Fenretinide65646-68-64-HPR芬维A胺RAR/RXRAutophagyRetinoic acid receptorsRetinoid X receptorsInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

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营业执照（三证合一）

Fenretinide (Synonyms: 芬维A胺; 4-HPR)

Customer Review

Other Forms of Fenretinide:

MCE 顾客使用本产品发表的 9 篇科研文献