2. Immunology/Inflammation Metabolic Enzyme/Protease Stem Cell/Wnt JAK/STAT Signaling
  3. PD-1/PD-L1 HIF/HIF Prolyl-Hydroxylase STAT
  4. Fraxinellone

Fraxinellone is isolated from the root bark of the Rutaceae plant, Dictamnus dasycarpus. Fraxinellone is a PD-L1 inhibitor and inhibits HIF-1α protein synthesis without affecting HIF-1α protein degradation. Fraxinellone has the potential to be a valuable candidate for cancer treatment by targeting PD-L1.

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No. CAS : 28808-62-0

Tamaño Precio Stock Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 En stock
Solution
10 mM * 1 mL in DMSO En stock
Solid
5 mg En stock
10 mg En stock
25 mg En stock
50 mg En stock
100 mg En stock
200 mg   Obtener un presupuesto  
500 mg   Obtener un presupuesto  

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Revisión del cliente

Based on 4 publication(s) in Google Scholar

Other Forms of Fraxinellone:

Fraxinellone Related Antibodies

Top Publications Citing Use of Products

    Fraxinellone purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2024 Nov:180:117560.  [Abstract]

    mRNA content of IL6, TNFα and IL1β treated with Fraxinellone (FRA) (5 mg/kg, i.p.).

    Fraxinellone purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2024 Nov:180:117560.  [Abstract]

    Western blot analysis of Bax and BCL2 treated with Fraxinellone (FRA) (5 mg/kg, i.p.)

    Fraxinellone purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2024 Nov:180:117560.  [Abstract]

    Cell viability was measured by CCK8 treated with Fraxinellone (FRA) (20, 40, 80, 160 μM).

    Fraxinellone purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2024 Nov:180:117560.  [Abstract]

    The typical representative of TH and GAP43 immunohistochemical staining in myocardial tissue treated with Fraxinellone (FRA) (5 mg/kg, i.p.).

    Fraxinellone purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2024 Nov:180:117560.  [Abstract]

    The representative images of Cx43 immunofluorescence staining in myocardial tissue treated with Fraxinellone (FRA) (5 mg/kg, i.p.).

    Ver todos los productos específicos de isoformas HIF/HIF Prolyl-Hydroxylase:

    Ver todas las isoformas
    HIF-1α HIF

    Ver todos los productos específicos de isoformas STAT:

    Ver todas las isoformas
    STAT3 STAT5 STAT6 STAT1

    • Actividad biológica

    • Pureza y Documentación

    • Referencias

    • Revisión del cliente

    Descripciòn

    Fraxinellone is isolated from the root bark of the Rutaceae plant, Dictamnus dasycarpus. Fraxinellone is a PD-L1 inhibitor and inhibits HIF-1α protein synthesis without affecting HIF-1α protein degradation. Fraxinellone has the potential to be a valuable candidate for cancer treatment by targeting PD-L1[1].

    Cellular Effect
    Cell Line Type Value Description References
    CAL-27 IC50
    22.4 μg/mL
    Compound: Frax
    Antiproliferative activity against human CAL-27 cells assessed as cell viability measured after 72 hrs by MTT assay
    Antiproliferative activity against human CAL-27 cells assessed as cell viability measured after 72 hrs by MTT assay
    		[PMID: 34463097]
    SCC-9 IC50
    43.4 μg/mL
    Compound: Frax
    Antiproliferative activity against human SCC-9 cells assessed as cell viability measured after 72 hrs by MTT assay
    Antiproliferative activity against human SCC-9 cells assessed as cell viability measured after 72 hrs by MTT assay
    		[PMID: 34463097]
    In Vitro

    Fraxinellone (0-100 μM；12 hours) decreases the percent of PD-L1 positive cells from 20.4% to 11.4% in A549 cells[1].

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

    Fraxinellone Related Antibodies

    Cell Viability Assay[1]

    Cell Line: A549 cells
    Concentration: 0 μM, 10 μM, 30 μM, 100 μM
    Incubation Time: 12 hours
    Result: Inhibited the percent of PD-L1 positive cells.
    In Vivo

    Fraxinellone (oral gavage; 30 and 100?mg/kg; every three days; 30 days) significantly suppresses tumor growth, reduces HIF-1α, pTyr705 STAT3, PD-L1 and VEGF staining compared with the control group in female athymic BALB/c nude mice[1].

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

    Animal Model: BALB/c nude mice[1]
    Dosage: 30 and 100 mg/kg
    Administration: Oral gavage; 30 and 100 mg/kg; every three days; 30 days
    Result: Significantly suppressed tumor growth.
    Peso molecular

    232.28

    Fòrmula

    C14H16O3
    No. CAS
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C1O[C@@H](C2=COC=C2)[C@]3(C)CCCC(C)=C31
    Structure Classification
    Initial Source
    Envío

    Room temperature in continental US; may vary elsewhere.
    Almacenamiento
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvente y solubilidad
    In Vitro: 

    DMSO : 100 mg/mL (430.51 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 4.3051 mL 21.5257 mL 43.0515 mL
    5 mM 0.8610 mL 4.3051 mL 8.6103 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.

    • Calculadora de molaridad

    • Calculadora de dilución

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    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 (10.76 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% Corn Oil

      Solubility: ≥ 2.5 mg/mL (10.76 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    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.
    Pureza y Documentación

    Purity: 99.91%

    SDS (644 KB)

    COA (255 KB) HNMR (237 KB) LCMS (94 KB)

    Instrucciones de manejo (2659 KB)
    Referencias

    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 4.3051 mL 21.5257 mL 43.0515 mL 107.6287 mL
    5 mM 0.8610 mL 4.3051 mL 8.6103 mL 21.5257 mL
    10 mM 0.4305 mL 2.1526 mL 4.3051 mL 10.7629 mL
    15 mM 0.2870 mL 1.4350 mL 2.8701 mL 7.1752 mL
    20 mM 0.2153 mL 1.0763 mL 2.1526 mL 5.3814 mL
    25 mM 0.1722 mL 0.8610 mL 1.7221 mL 4.3051 mL
    30 mM 0.1435 mL 0.7175 mL 1.4350 mL 3.5876 mL
    40 mM 0.1076 mL 0.5381 mL 1.0763 mL 2.6907 mL
    50 mM 0.0861 mL 0.4305 mL 0.8610 mL 2.1526 mL
    60 mM 0.0718 mL 0.3588 mL 0.7175 mL 1.7938 mL
    80 mM 0.0538 mL 0.2691 mL 0.5381 mL 1.3454 mL
    100 mM 0.0431 mL 0.2153 mL 0.4305 mL 1.0763 mL
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    Fraxinellone Related Classifications

    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:

    Fraxinellone28808-62-0PD-1/PD-L1HIF/HIF Prolyl-HydroxylaseSTATPD-1/Programmed death-ligand 1Hypoxia-inducible factorsHIFsHIF-PHInhibitorinhibitorinhibit

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    Nombre del producto:
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    Cat. No.:
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