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Rezatapopt p53 activator

Name: Rezatapopt
Brand: Selleck Chemicals
SKU: E1971
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.E1971

Rezatapopt(PC14586) is a first-in-class p53 reactivator. It selectively binds to the mutated p53 Y220C protein and restores its wild-type activity. It can also be used to inhibit solid tumor with p53 mutation.

Chemical Structure

Molecular Weight: 545.57

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Quality Control

Batch: E197101 DMSO]100 mg/mL]false]Ethanol]25 mg/mL]false]Water]Insoluble]false Purity: 95.10%

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS/MSDS
Datasheet

95.10

Related Targets	Bcl-2 Caspase PD-1/PD-L1 Ferroptosis Apoptosis related Synthetic Lethality STAT TNF-alpha Ras KRas
Other p53 Inhibitors	Eprenetapopt (APR-246) CBL0137 Hydrochloride Pifithrin-α (PFTα) Hhydrobromide Pifithrin-μ RITA Serdemetan (JNJ-26854165) PRIMA-1 NSC 319726 (ZMC1) NSC59984 NSC348884

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (183.29 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 25 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (9.16mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.650mg/ml (1.19mM)	Taking the 1 mL working solution as an example, add 50 μL of 13 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	545.57	Formula	C₂₈H₃₁F₄N₅O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	2636846-41-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Read more about storage stability stock solution CAS number

Mechanism of Action

Targets/IC₅₀/Ki	p53
References	[1] https://pubmed.ncbi.nlm.nih.gov/36139658/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-08-20)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06616636	RECRUITING	Myelodysplastic Syndrome; Acute Myeloid Leukemia	M.D. Anderson Cancer Center	2025-01-30	PHASE1
NCT07372625	RECRUITING	TP53 Y220C Mutation; Advanced Solid Tumors	PMV Pharmaceuticals, Inc	2026-02-04	PHASE1
NCT04585750	RECRUITING	Advanced Solid Tumor; Advanced Malignant Neoplasm; Metastatic Cancer; Metastatic Solid Tumor; Lung Cancer; Ovarian Cancer; Endometrial Cancer; Prostate Cancer; Colorectal Cancer; Breast Cancer; Other Cancer; Locally Advanced; Head and Neck Cancer; Gall Bladder Cancer; Small Cell Lung Cancer; Small Cell Lung Cancer ( SCLC ); Small Cell Lung Carcinoma; NSCLC; NSCLC (Non-small Cell Lung Cancer); SCLC; Non-Small Cell Lung Carcinoma; Triple Negative Breast Cancer; TNBC; HER2+ Breast Cancer; Non-Small Cell Lung Cancer; ER/PR Positive Breast Cancer; HER2- Breast Cancer; HER2-positive Breast Cancer; HER2-negative Breast Cancer; ER/PR(+), Her2(-) Breast Cancer	PMV Pharmaceuticals, Inc	2020-10-29	PHASE1; PHASE2

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Handling Instructions

Tel: +1-832-582-8158 Ext:3

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