2. Apoptosis
  3. MDM-2/p53
  4. Rezatapopt

Rezatapopt (PC14586) is an orally active antineoplastic agent. Rezatapopt binds to a pocket created by the TP53 Y220C mutation. Rezatapopt restores p53 tumor suppressor functions by stabilization of the p53 protein structure. Rezatapopt demonstrates tumor inhibition and regression in mouse models with established human tumor xenografts harboring the TP53 Y220C mutation.

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No. CAS : 2636846-41-6

Tamaño Precio Stock Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Revisión del cliente

Based on 3 publication(s) in Google Scholar

Rezatapopt Related Antibodies

Top Publications Citing Use of Products
Cell Proliferation/Viability Assay
RT-PCR
WB

    Rezatapopt purchased from MedChemExpress. Usage Cited in: Genes Dev. 2025 Nov 5.  [Abstract]

    Rezatapopt (10 µM; 7 d) decreased the colony-forming ability of SKOV3 cells stably transfected with the Y220C mutant but not of parental cells transfected with vector alone.

    Rezatapopt purchased from MedChemExpress. Usage Cited in: Genes Dev. 2025 Nov 5.  [Abstract]

    Treatment with Rezatapopt (3-10 µM; 48 h) led to robust induction of the p53 target genes CDKN1A in SKOV3-Y220C cells.

    Rezatapopt purchased from MedChemExpress. Usage Cited in: Genes Dev. 2025 Nov 5.  [Abstract]

    Treatment with Rezatapopt (3 to 10 µM; 48 h) induced the expression of the p53 target genes p21 and MDM2 in SKOV3-Y220C cells.

    Rezatapopt purchased from MedChemExpress. Usage Cited in: Genes Dev. 2025 Nov 5.  [Abstract]

    IC50 analysis of Fulvestrant in SKOV3-Y220C cells with or without Rezatapopt (3 µM; 5 d).

    Rezatapopt purchased from MedChemExpress. Usage Cited in: Genes Dev. 2025 Nov 5.  [Abstract]

    Rezatapopt (3 µM) showed little inhibition in colony-forming assays and led to significantly increased sensitivity to fulvestrant (10 µM) in SKOV3 cells harboring the Y220C mutant.

    • Actividad biológica

    • Pureza y Documentación

    • Referencias

    • Revisión del cliente

    Descripciòn

    Rezatapopt (PC14586) is an orally active antineoplastic agent. Rezatapopt binds to a pocket created by the TP53 Y220C mutation. Rezatapopt restores p53 tumor suppressor functions by stabilization of the p53 protein structure. Rezatapopt demonstrates tumor inhibition and regression in mouse models with established human tumor xenografts harboring the TP53 Y220C mutation[1][2][3][4].

    In Vivo

    Rezatapopt induces complete regression of tumors in mice and potentiated checkpoint therapy[3].

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

    545.57

    Fòrmula

    C28H31F4N5O2
    No. CAS
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    FC(F)(F)CN1C2=CC=CC(N[C@H]3[C@H](CN(CC3)C)F)=C2C=C1C#CCNC4=C(C=C(C=C4)C(NC)=O)OC
    Envío

    Room temperature in continental US; may vary elsewhere.
    Almacenamiento

    4°C, protect from light, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

    Solvente y solubilidad
    In Vitro: 

    DMSO : 50 mg/mL (91.65 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 1.8329 mL 9.1647 mL 18.3295 mL
    5 mM 0.3666 mL 1.8329 mL 3.6659 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 (protect from light, stored under nitrogen). 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    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (4.58 mM); Suspended solution

      This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.

      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
    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).

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

    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: 99.78%

    SDS (252 KB)

    COA (248 KB) HNMR (249 KB) RP-HPLC (257 KB) LCMS (139 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 (protect from light, stored under nitrogen). 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 1.8329 mL 9.1647 mL 18.3295 mL 45.8236 mL
    5 mM 0.3666 mL 1.8329 mL 3.6659 mL 9.1647 mL
    10 mM 0.1833 mL 0.9165 mL 1.8329 mL 4.5824 mL
    15 mM 0.1222 mL 0.6110 mL 1.2220 mL 3.0549 mL
    20 mM 0.0916 mL 0.4582 mL 0.9165 mL 2.2912 mL
    25 mM 0.0733 mL 0.3666 mL 0.7332 mL 1.8329 mL
    30 mM 0.0611 mL 0.3055 mL 0.6110 mL 1.5275 mL
    40 mM 0.0458 mL 0.2291 mL 0.4582 mL 1.1456 mL
    50 mM 0.0367 mL 0.1833 mL 0.3666 mL 0.9165 mL
    60 mM 0.0305 mL 0.1527 mL 0.3055 mL 0.7637 mL
    80 mM 0.0229 mL 0.1146 mL 0.2291 mL 0.5728 mL
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    Rezatapopt 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:

    Rezatapopt2636846-41-6PC14586PC 14586PC-14586MDM-2/p53Inhibitorinhibitorinhibit

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    Nombre del producto:
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    Cat. No.:
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