1. Metabolic Enzyme/Protease Apoptosis NF-κB Immunology/Inflammation
  2. Lactate Dehydrogenase Apoptosis Reactive Oxygen Species (ROS)
  3. FX-11

FX-11  (Synonyms: LDHA Inhibitor FX11)

製品番号: HY-16214 純度: 99.21%
COA 取扱説明書 Technical Support

FX-11 is a potent, selective, reversible and competitive lactate dehydrogenase A (LDHA) inhibitor, with a Ki of 8 μM. FX-11 reduces ATP levels and induces oxidative stress, ROS production and cell death. FX-11 shows antitumor activity in lymphoma and pancreatic cancer xenografts.

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CAS 番号 : 213971-34-7

容量 価格(税別) 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 132 在庫あり
Solution
10 mM * 1 mL in DMSO USD 132 在庫あり
Solid
5 mg $120 在庫あり
10 mg $190 在庫あり
50 mg $850 在庫あり
100 mg $1550 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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カスタマーレビュー

Based on 28 publication(s) in Google Scholar

Top Publications Citing Use of Products
Cell Proliferation/Viability Assay
Cell Imaging/Staining
In Vivo Efficacy Study
In Vivo Imaging
RT-PCR

    FX-11 purchased from MedChemExpress. Usage Cited in: Sci Rep. 2023 Feb 24;13(1):3257.  [Abstract]

    FX11 (20 μM; pretreat for 1 h) decreases bTNF-α-induced COX-2 mRNA expression and PGE2 synthesis in bovine fibroblast-like synoviocyte.

    FX-11 purchased from MedChemExpress. Usage Cited in: Nat Metab. 2022 Dec;4(12):1830-1846.  [Abstract]

    FX11(1 mg/kg/day; i.p.) in combination with NSC23766 (NSC; 1.5 mg/kg/day; i.p.) for 2-3 weeks, displays a pronounced inhibitory effect on lung metastasis of Hs578T cells .

    FX-11 purchased from MedChemExpress. Usage Cited in: Cell Metab. 2021 Jan 5;33(1):51-64.e9.  [Abstract]

    Dose-response curves for FX-11 (0-100 μM; 72 hours). Results of cell viability assays in five organoid models derived from TNBC patients.

    FX-11 purchased from MedChemExpress. Usage Cited in: Cell Metab. 2021 Jan 5;33(1):51-64.e9.  [Abstract]

    FX-11 (11.1 μM; 5–6 days). Representative bright-field images of organoids from three selected cases after drug treatment.

    FX-11 purchased from MedChemExpress. Usage Cited in: Cell Metab. 2021 Jan 5;33(1):51-64.e9.  [Abstract]

    The effect of anti-LDH antibody FX-11 (2 mg/kg; twice a week for 24 days) combined with immune checkpoint inhibitor therapy on TS/A tumor growth.
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    製品説明

    FX-11 is a potent, selective, reversible and competitive lactate dehydrogenase A (LDHA) inhibitor, with a Ki of 8 μM. FX-11 reduces ATP levels and induces oxidative stress, ROS production and cell death. FX-11 shows antitumor activity in lymphoma and pancreatic cancer xenografts[1][2][3].

    IC50 & Target

    IC50: 23.3 μM (LDHA in HeLa cell) [1].

    体外実験

    FX-11 (9 μM, 24-48 h) shows activation of AMP kinase and phosphorylation of its substrate acetyl-CoA carboxylase[2].
    FX-11 (0-100 μM, 72 h) inhibits cell proliferation in BxPc-3 and MIA PaCa-2 cells[3].
    FX-11 inhibits glycolysis and alters cellular energy metabolism in P493 cells[2].

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

    Western Blot Analysis[2]

    Cell Line: P493 cells
    Concentration: 9 μM
    Incubation Time: 24 h, 48 h
    Result: Showed a decrease in ATP levels, accompanied by activation of AMP kinase and phosphorylation of its substrate acetyl-CoA carboxylase.

    Cell Proliferation Assay[3]

    Cell Line: BxPc-3 and MIA PaCa-2 cells
    Concentration: 0-100 µM
    Incubation Time: 72 h
    Result: Reduced cell metabolic activity in a concentration-dependent manner, showed a significant reduction in cell proliferation, with IC50 values of 49.27 µM and 60.54 µM for BxPc-3 and MIA PaCa-2 cells, respectively.
    体内実験

    FX-11 (42 μg/mouse; IP, daily for 10-14 days) inhibits P493 tumor growth[2].
    FX-11 (0-2 mg/kg, IP, daily, for 3 weeks) significantly delays tumor growth[3].

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

    Animal Model: Male SCID mice and RH-Foxn1nu mice (human P493 B-cell xenografts)[2]
    Dosage: 42 µg/mouse (2.1 mg/kg)
    Administration: IP; daily for 10-14 days
    Result: Resulted in a remarkable inhibition of tumor growth, inhibited tumor xenograft progression.
    Animal Model: Immunocompromised CD-1 mice (6-8 weeks; 20-25 g, n=5 per group)[3]
    Dosage: 2 mg/kg, 1 mg/kg+15 mg/kg TEPP-46, 2 mg/kg+30 mg/kg TEPP-46
    Administration: IP (100 µL), daily, for 3 weeks
    Result: Significantly lowered LDHA activity in plasma and tumor lysates; significantly lowered the expression of the proliferation marker Ki-67; significantly decreased proliferation indices were observed in tumor sections; significantly delayed tumor growth.
    分子量

    350.41

    分子式

    C22H22O4

    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C1=C2C=C(CC3=CC=CC=C3)C(C)=CC2=C(CCC)C(O)=C1O)O

    輸送条件

    Room temperature in continental US; may vary elsewhere.

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

    DMSO : 250 mg/mL (713.45 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 2.8538 mL 14.2690 mL 28.5380 mL
    5 mM 0.5708 mL 2.8538 mL 5.7076 mL
    10 mM 0.2854 mL 1.4269 mL 2.8538 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.

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    一般には略語で表示されます:C1V1 = C2V2

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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: ≥ 2.08 mg/mL (5.94 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% Corn Oil

      Solubility: ≥ 2.08 mg/mL (5.94 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

    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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    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, 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 2.8538 mL 14.2690 mL 28.5380 mL 71.3450 mL
    5 mM 0.5708 mL 2.8538 mL 5.7076 mL 14.2690 mL
    10 mM 0.2854 mL 1.4269 mL 2.8538 mL 7.1345 mL
    15 mM 0.1903 mL 0.9513 mL 1.9025 mL 4.7563 mL
    20 mM 0.1427 mL 0.7134 mL 1.4269 mL 3.5672 mL
    25 mM 0.1142 mL 0.5708 mL 1.1415 mL 2.8538 mL
    30 mM 0.0951 mL 0.4756 mL 0.9513 mL 2.3782 mL
    40 mM 0.0713 mL 0.3567 mL 0.7134 mL 1.7836 mL
    50 mM 0.0571 mL 0.2854 mL 0.5708 mL 1.4269 mL
    60 mM 0.0476 mL 0.2378 mL 0.4756 mL 1.1891 mL
    80 mM 0.0357 mL 0.1784 mL 0.3567 mL 0.8918 mL
    100 mM 0.0285 mL 0.1427 mL 0.2854 mL 0.7134 mL
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    • Molarity Calculator

    • Dilution Calculator

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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)
    × = ×
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    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.

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    製品名:
    FX-11
    製品番号:
    HY-16214
    数量:
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