Rezatapopt
Based on 3 publication(s) in Google Scholar
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.62%
- No. CAS: 2636846-41-6
- Fòrmula: C28H31F4N5O2
- Peso molecular:545.57
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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)
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Publications Citing Use of MedChemExpress (MCE) Rezatapopt
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Cell Proliferation/Viability Assay
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RT-PCR
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WB
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
Actividad biológica
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2636846-41-6
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Appearance Solid
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Peso molecular 545.57
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Fòrmula C28H31F4N5O2
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Color Light yellow to yellow
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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
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Synonyms
PC14586
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Envío
Room temperature in continental US; may vary elsewhere.
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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)
Publications (3)
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Journal Impact Factor
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Most Recent
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J Adv Res
Targeting class I HDACs suppresses oncogenic vulnerabilities and potentiates KRAS/MAPK pathway inhibitors in KRAS-mutant cancers. [Abstract]2026 Feb 13:S2090-1232(26)00144-X. PMID: 41692243 -
Cell Death Dis
Targeting the p53 cancer mutants Y220C, Y220N, and Y220S with the small-molecule stabilizer rezatapopt. [Abstract]2026 Feb 26. PMID: 41748563 -
Genes Dev
Mutant p53 binds and controls estrogen receptor activity to drive endocrine resistance in ovarian cancer. [Abstract]2025 Nov 5. PMID: 41193244
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.
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Ficha de datos (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[2]. Vu BT, et al. Discovery of Rezatapopt (PC14586), a First-in-Class, Small-Molecule Reactivator of p53 Y220C Mutant in Development. ACS Med Chem Lett. 2024 Nov 4;16(1):34-39. [Content Brief]
[3]. Spiegelberg D, et al. Targeting mutant p53: Evaluation of novel anti-p53R175H monoclonal antibodies as diagnostic tools. Sci Rep. 2025 Jan 6;15(1):1000. [Content Brief]
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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