| Field | Specification |
|---|---|
| Alternative names | PC14586 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C28H31F4N5O2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Rezatapopt (PC14586) is an orally active antineoplastic agent that binds to a pocket created by the TP53 Y220C mutation. It restores p53 tumor suppressor function by stabilizing the p53 protein structure, and it demonstrates tumor inhibition and regression in mouse models bearing established human tumor xenografts that harbor the TP53 Y220C mutation[1][2][3][4]. It is supplied as an off-white to yellow solid (C28H31F4N5O2, MW 545.57) at 99.62% purity.
Physical & Chemical Properties
| CAS Number | 2636846-41-6 |
|---|---|
| Molecular Formula | C28H31F4N5O2 |
| Molecular Weight | 545.57 g/mol |
| Purity | 99.62% |
| Appearance | Solid |
| Color | Off-white 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 |
| Signaling Pathway | Apoptosis |
| Solubility | In Vitro: DMSO: 50 mg/mL (91.65 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | 4°C, protect from light, stored under nitrogen. In solvent: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
[1]. Li Sujing, et al. Heteroarylalkyne compounds for targeting mutant of p53 and their preparation. World Intellectual Property Organization, WO2023016434 A1. 2023-02-16.
[4]. Schram A M, et al. 691TiP PYNNACLE phase II trial of rezatapopt (PC14586) in solid tumors with a TP53 Y220C mutation[J]. Annals of oncology, 2024, 35: S535-S536.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 50 mg/mL (91.65 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); protect from light, stored under nitrogen; avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.5 mg/mL (4.58 mM); suspension |
| How to prepare | Gives a suspension at ≥ 2.5 mg/mL (saturation not determined). The suspension is suitable for oral and intraperitoneal dosing. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Data provided by the manufacturer.
In Vivo
Rezatapopt causes complete regression of tumors in mice and potentiates checkpoint therapy[3].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Targeting class I HDACs suppresses oncogenic vulnerabilities and potentiates KRAS/MAPK pathway inhibitors in KRAS-mutant cancers. J Adv Res 2026 Feb 13:S2090-1232(26)00144-X. PMID: 41692243
Targeting the p53 cancer mutants Y220C, Y220N, and Y220S with the small-molecule stabilizer rezatapopt. Cell Death Dis 2026 Feb 26. PMID: 41748563
Mutant p53 binds and controls estrogen receptor activity to drive endocrine resistance in ovarian cancer. Genes Dev 2025 Nov 5. PMID: 41193244
