1. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor Autophagy
  2. RAR/RXR Autophagy
  3. Fenretinide

Fenretinide  (Synonyms: 4-HPR; フェンレチニド)

製品番号: HY-15373 純度: 98.34%
COA 取扱説明書 Technical Support

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

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CAS 番号 : 65646-68-6

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>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 46 在庫あり
Solution
10 mM * 1 mL in DMSO USD 46 在庫あり
Solid
5 mg $42 在庫あり
10 mg $66 在庫あり
25 mg $92 在庫あり
50 mg $118 在庫あり
100 mg $158 在庫あり
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カスタマーレビュー

Based on 9 publication(s) in Google Scholar

Other Forms of Fenretinide:

Top Publications Citing Use of Products

    Fenretinide purchased from MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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.

    Fenretinide purchased from MedChemExpress. 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.

    RAR/RXR アイソフォーム固有の製品をすべて表示:

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    • プロトコル

    • 純度とドキュメンテーション

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    製品説明

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

    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]
    Huh-7 CC50
    <= 10 μM
    Compound: 4-HPR
    Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability measured after 48 hrs by Celltiter-glo assay
    Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability measured after 48 hrs by Celltiter-glo assay
    [PMID: 37159959]
    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 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]
    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]
    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]
    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]
    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]
    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]
    体外実験

    Fenretinide (4-HPR) 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, 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].

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

    体内実験

    Fenretinide (4-HPR) (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]. Addition of 25 mg/kg ketoconazole to Fenretinide in NOD/SCID mice increased 4-HPR plasma levels[3].

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

    臨床実験
    分子量

    391.55

    分子式

    C26H33NO2

    CAS 番号
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    CC(/C=C/C=C(/C=C/C1=C(CCCC(C)1C)C)C)=C\C(NC2=CC=C(O)C=C2)=O

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : ≥ 100 mg/mL (255.40 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

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    一般には略語で表示されます:C1V1 = C2V2

    濃度 (開始)

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    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (6.38 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (6.38 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション

    純度: 98.34%

    参考文献
    細胞実験
    [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).

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。

    動物実験
    [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.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。

    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 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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    一般には略語で表示されます:C1V1 = C2V2

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    製品名:
    Fenretinide
    製品番号:
    HY-15373
    数量:
    MCE 日本正規代理店: