| Identification | Back Directory | [Name]
Rezatapopt | [CAS]
2636846-41-6 | [Synonyms]
Rezatapopt
4-((3-(4-(((3S,4R)-3-fluoro-1-methylpiperidin-4-yl)amino)-1-(2,2,2-trifluoroethyl)-1H-indol-2-yl)prop-2-yn-1-yl)amino)-3-methoxy-N-methylbenzamide | [Molecular Formula]
C28H31F4N5O2 | [MOL File]
2636846-41-6.mol | [Molecular Weight]
545.57 |
| Chemical Properties | Back Directory | [Boiling point ]
684.8±55.0 °C(predicted) | [density ]
1.29±0.1 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted) | [form ]
Solid | [pka]
15.09±0.46(predicted) | [color ]
Light yellow to yellow | [InChIKey]
NKRKBSQLUPEVCZ-JTHBVZDNSA-N | [SMILES]
N([C@@H]1CCN(C[C@@H]1F)C)C1C=CC=C2N(C(=CC2=1)C#CCNC1C=CC(=CC=1OC)C(=O)NC)CC(F)(F)F |
| Hazard Information | Back Directory | [Uses]
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].
| [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.
[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. DOI:10.1021/acsmedchemlett.4c00379
[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. DOI:10.1038/s41598-024-83871-w
[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. |
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