1. Epigenetics
  2. Histone Acetyltransferase
  3. PF-9363

PF-9363 (CTx-648) is a first-in-class potent and high selective KAT6A/KAT6B inhibitor. PF-9363 can be used for the research of cancer.

For research use only. We do not sell to patients.

CAS No. : 2569009-58-9

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 4 publication(s) in Google Scholar

Top Publications Citing Use of Products

    PF-9363 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Jul 2:2025.07.01.662644.  [Abstract]

    Western blot analysis using antibodies to the indicated histones that were extracted from neuroblastoma cell line KELLY after treatment with the indicated doses of PF-9363 (0-10 μM) for 1, 3 and 6 days. Total H3 served as a loading control.

    PF-9363 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Jul 2:2025.07.01.662644.  [Abstract]

    Flow cytometry showing GD2 expression levels in the GD2low cell lines BE2C, NGP and NB1 treated for 14 days with DMSO, isotretinoin alone, PF9363 (1 μM) alone, or isotretinoin plus PF-9363.

    PF-9363 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Jul 2:2025.07.01.662644.  [Abstract]

    Cell viability of BE2C and NB1 cells following both treatment with either DMSO, isotretinoin alone, PF-9363 alone, or isotretinoin plus PF-9363 (1 μM) for 14 days and subsequent, co-culture with NK cells and dinutuximab for 24 hours.

    PF-9363 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Jul 2:2025.07.01.662644.  [Abstract]

    Scatter plot of log2 fold-changes in H3K27me3 CUT&RUN signal at significant islands with lfc > 0.5 versus their fold-change rank. Experiments obtained from BE2C cells treated with PF-9363, isotretinoin or isotretinoin plus PF-9363 for 14 days at a concentration of 1 μM compared to control DMSO-treated BE2C cells. Significant islands associated with PHOX2B and GATA3 are noted.

    PF-9363 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Jul 2:2025.07.01.662644.  [Abstract]

    Western-blot assay for transcription factors GATA3, PHOX2B and MYCN in BE2C cells treated with isotretinoin plus PF-9363 (1 μM) for 14 days followed by PF-9363 alone for 28 days.

    PF-9363 purchased from MedChemExpress. Usage Cited in: Nat Cell Biol. 2023 Sep;25(9):1346-1358.  [Abstract]

    Immunoblot analysis of 1014 Kdm6a isogenic cells treated with inhibitors that block the function of epigenetic modifiers that normally maintain gene expression including VTP50469 (500 nM), EPZ-5676 (1 μM), PF-9363 (100 nM), JQAD1 or DMSO for 6 days.

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    PF-9363 (CTx-648) is a first-in-class potent and high selective KAT6A/KAT6B inhibitor. PF-9363 can be used for the research of cancer[1][2].

    IC50 & Target

    MOZ/MORF

     

    In Vitro

    PF-9363 (0~1 μM; 1 day; ZR75-1, T47D and MCF7 cells) down-regulates the expression of H3K23Ac biomarker[1].
    PF-9363 leads to down regulation of a specific set of genes involved in ESR1 pathway, cell cycle and stem cell pathways. PF-9363 shows that the IC50 values for ZR75-1 and T47D are 0.3 nM and 0.9 nM[1].

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

    Western Blot Analysis[1]

    Cell Line: ZR75-1, T47D and MCF7 cells
    Concentration: 0~1 μM
    Incubation Time: 1 day
    Result: Down-regulated the expression of H3K23Ac biomarker.
    In Vivo

    PF-9363 shows strong anti-tumor activity in patient-derived xenograft models[1].

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

    Molecular Weight

    444.46

    Formula

    C20H20N4O6S

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=S(C1=C(OC)C=CC=C1OC)(NC2=NOC3=C2C(OC)=CC(CN4N=CC=C4)=C3)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (112.50 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 2.2499 mL 11.2496 mL 22.4992 mL
    5 mM 0.4500 mL 2.2499 mL 4.4998 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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    Concentration
    ×
    Volume
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    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: ≥ 2.08 mg/mL (4.68 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% (20% SBE-β-CD in Saline)

      Solubility: 2.08 mg/mL (4.68 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.08 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 (20.8 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
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    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.
    Purity & Documentation

    Purity: 99.64%

    References

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

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2499 mL 11.2496 mL 22.4992 mL 56.2480 mL
    5 mM 0.4500 mL 2.2499 mL 4.4998 mL 11.2496 mL
    10 mM 0.2250 mL 1.1250 mL 2.2499 mL 5.6248 mL
    15 mM 0.1500 mL 0.7500 mL 1.4999 mL 3.7499 mL
    20 mM 0.1125 mL 0.5625 mL 1.1250 mL 2.8124 mL
    25 mM 0.0900 mL 0.4500 mL 0.9000 mL 2.2499 mL
    30 mM 0.0750 mL 0.3750 mL 0.7500 mL 1.8749 mL
    40 mM 0.0562 mL 0.2812 mL 0.5625 mL 1.4062 mL
    50 mM 0.0450 mL 0.2250 mL 0.4500 mL 1.1250 mL
    60 mM 0.0375 mL 0.1875 mL 0.3750 mL 0.9375 mL
    80 mM 0.0281 mL 0.1406 mL 0.2812 mL 0.7031 mL
    100 mM 0.0225 mL 0.1125 mL 0.2250 mL 0.5625 mL
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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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    Product Name:
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