2. Vitamin D Related/Nuclear Receptor Autophagy
  3. Estrogen Receptor/ERR Autophagy
  4. XCT790

XCT-790 is a potent and selective inverse agonist for ERRα with an IC50 value of 0.37 μM. XCT-790 induces cell death in chemotherapeutic resistant cancer cells. XCT-790 (Compound 12) is inactive against ERRγ and the estrogen receptors ERα and ERβ.

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CAS 番号 : 725247-18-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 98 在庫あり
Solution
10 mM * 1 mL in DMSO USD 98 在庫あり
Solid
5 mg $75 在庫あり
10 mg $121 在庫あり
25 mg $242 在庫あり
50 mg $418 在庫あり
100 mg $620 在庫あり
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カスタマーレビュー

Based on 10 publication(s) in Google Scholar

Other Forms of XCT790:

XCT790 関連抗体

Top Publications Citing Use of Products

    XCT790 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Sep 5;37(1):218.  [Abstract]

    The proliferation proteins cMyc and cyclin D1 are identified and confirmed by Western blot analysis after the colon cancer cells are treated with the indicated concentrations of XCT790 or DMSO for 48 h.

    XCT790 purchased from MedChemExpress. Usage Cited in: Oncogene. 2016 Sep 22;35(38):5033-42.  [Abstract]

    Inhibition of the ERRα-dependent mitochondrial activity by XCT-790 is found to drastically inhibit decreased cell density and increase cell death induced by PLA2R1.

    Estrogen Receptor/ERR アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

    • 生物活性

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    XCT-790 is a potent and selective inverse agonist for ERRα with an IC50 value of 0.37 μM. XCT-790 induces cell death in chemotherapeutic resistant cancer cells. XCT-790 (Compound 12) is inactive against ERRγ and the estrogen receptors ERα and ERβ[1][2].

    IC50 & Target[1][2]

    ERRα

    0.37 μM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    CV-1 IC50
    0.37 3
    Compound: 2, XCT790
    Inverse agonist activity at GAL4-fused ERRalpha (unknown origin) transfected in african green monkey CV1 cells after 24 hrs by luciferase reporter gene assay
    Inverse agonist activity at GAL4-fused ERRalpha (unknown origin) transfected in african green monkey CV1 cells after 24 hrs by luciferase reporter gene assay
    		[PMID: 23656512]
    CV-1 IC50
    0.37 3
    Compound: 2, XCT790
    Inverse agonist activity at GAL4-fused ERRalpha (unknown origin) transfected in african green monkey CV1 cells after 24 hrs by luciferase reporter gene assay
    Inverse agonist activity at GAL4-fused ERRalpha (unknown origin) transfected in african green monkey CV1 cells after 24 hrs by luciferase reporter gene assay
    		[PMID: 23656512]
    CV-1 IC50
    0.37 3
    Compound: 2, XCT790
    Inverse agonist activity at GAL4-fused ERRalpha (unknown origin) transfected in african green monkey CV1 cells after 24 hrs by luciferase reporter gene assay
    Inverse agonist activity at GAL4-fused ERRalpha (unknown origin) transfected in african green monkey CV1 cells after 24 hrs by luciferase reporter gene assay
    		[PMID: 23656512]
    HEK293 IC50
    0.37 3
    Compound: 4, XCT790
    Antagonist activity at ERRalpha LBD expressed in HEK293 cells assessed as Gal4-SRC2 interaction by two hybrid luciferase reporter gene assay
    Antagonist activity at ERRalpha LBD expressed in HEK293 cells assessed as Gal4-SRC2 interaction by two hybrid luciferase reporter gene assay
    		[PMID: 21218783]
    HEK293 IC50
    0.37 3
    Compound: 4, XCT790
    Antagonist activity at ERRalpha LBD expressed in HEK293 cells assessed as Gal4-SRC2 interaction by two hybrid luciferase reporter gene assay
    Antagonist activity at ERRalpha LBD expressed in HEK293 cells assessed as Gal4-SRC2 interaction by two hybrid luciferase reporter gene assay
    		[PMID: 21218783]
    HEK293 IC50
    0.37 3
    Compound: 4, XCT790
    Antagonist activity at ERRalpha LBD expressed in HEK293 cells assessed as Gal4-SRC2 interaction by two hybrid luciferase reporter gene assay
    Antagonist activity at ERRalpha LBD expressed in HEK293 cells assessed as Gal4-SRC2 interaction by two hybrid luciferase reporter gene assay
    		[PMID: 21218783]
    体外実験

    XCT-790 (0-40 μM; 48 hours and 72 hours) reduces the viability of MES-SA, MES-SA/DX5, and HepG2 cells in a dose-dependent manner[1].
    XCT-790 (10 μM; 24 hours and 48 hours) reduces the protein levels of ERRα in HepG2 and R-HepG2 cell lines after 24 hours and maintains these reduced levels after 48 hours[1].
    XCT-790 (10 μM; 48 hours) induces apoptosis in the two cell lines with HepG2 being more sensitive compared to R-HepG2[1].

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

    XCT790 関連抗体

    Cell Viability Assay[1]

    Cell Line: MES-SA, MES-SA/DX5, HepG2 and R-HepG2 cells
    Concentration: 0 μM, 5 μM, 10 μM, 20 μM, and 40 μM
    Incubation Time: 48 hours and 72 hours
    Result: The cells proliferation were decreased in a dose-dependent fashion.

    Western Blot Analysis[1]

    Cell Line: HepG2 and R-HepG2 cells
    Concentration: 10 μM
    Incubation Time: 24 hours and 48 hours
    Result: Reduced the protein levels of ERRα.

    Apoptosis Analysis[1]

    Cell Line: HepG2 and R-HepG2 cells
    Concentration: 10 μM
    Incubation Time: 48 hours
    Result: Induced apoptosis in HepG2 and R-HepG2 cells.
    体内実験

    XCT-790 (XCT790; 4 mg/kg; intravenous injection; every three days; for 3 weeks; BALB/c mice) significantly inhibits tumor growth and angiogenesis, and induces apoptosis without a reduction in body weight, in xenograft models[3].

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

    Animal Model: Female BALB/c mice (4 weeks of age) with HEC-1A xenograft[3]
    Dosage: 4 mg/kg
    Administration: Intravenous injection; every three days; for 3 weeks
    Result: Suppressed endometrial cancer growth and angiogenesis, and induced apoptosis.
    分子量

    596.42

    分子式

    C23H13F9N4O3S
    CAS 番号
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C(NC1=NN=C(C(F)(F)F)S1)/C(C#N)=C/C2=CC=C(OCC3=C(C(F)(F)F)C=C(C(F)(F)F)C=C3)C(OC)=C2
    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 : 16.67 mg/mL (27.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.6767 mL 8.3834 mL 16.7667 mL
    5 mM 0.3353 mL 1.6767 mL 3.3533 mL
    10 mM 0.1677 mL 0.8383 mL 1.6767 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

    ×
    体積 （開始）

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    濃度 （終了）

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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: 1.67 mg/mL (2.80 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 1.67 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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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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    +
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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
    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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.6767 mL 8.3834 mL 16.7667 mL 41.9168 mL
    5 mM 0.3353 mL 1.6767 mL 3.3533 mL 8.3834 mL
    10 mM 0.1677 mL 0.8383 mL 1.6767 mL 4.1917 mL
    15 mM 0.1118 mL 0.5589 mL 1.1178 mL 2.7945 mL
    20 mM 0.0838 mL 0.4192 mL 0.8383 mL 2.0958 mL
    25 mM 0.0671 mL 0.3353 mL 0.6707 mL 1.6767 mL
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    XCT790 Related Classifications

    • Molarity Calculator

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    質量   濃度   体積   分子量 *
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    The dilution calculator equation

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    Help & FAQs
    • Do most proteins show cross-species activity?

      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:

    XCT790725247-18-7XCT 790XCT-790Estrogen Receptor/ERRAutophagyInhibitorinhibitorinhibit

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    製品名:
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    製品番号:
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