A reactivator of p53Y220C
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Rezatapopt

Item No. 44358

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[[3-[4-[[(3S,4R)-3-fluoro-1-methyl-4-piperidinyl] amino]-1-(2,2,2-trifluoroethyl)-1H-indol-2-yl]-2-propyn-1-yl]amino]- 3-methoxy-N-methyl-benzamide
CAS Number
2636846-41-6
Synonyms
  • PC14586
Molecular Formula
C28H31F4N5O2
Formula Weight
545.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥ 10 mg/mlEthanol: Sparingly soluble: 1-10 mg/ml
SMILES
CN1CC[C@@H](NC(C=CC=C2N3CC(F)(F)F)=C2C=C3C#CCNC4=CC=C(C(NC)=O)C=C4OC)[C@@H](F)C1
InChi Code
InChI=1S/C28H31F4N5O2/c1-33-27(38)18-9-10-24(26(14-18)39-3)34-12-5-6-19-15-20-22(35-23-11-13-36(2)16-21(23)29)7-4-8-25(20)37(19)17-28(30,31)32/h4,7-10,14-15,21,23,34-35H,11-13,16-17H2,1-3H3,(H,33,38)/t21-,23+/m0/s1
InChi Key
NKRKBSQLUPEVCZ-JTHBVZDNSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    10 mg

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    25 mg

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    Cayman Chemical
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    Product Description

    Rezatapopt is a reactivator of p53 containing a tyrosine-to-cysteine substitution at position 220 (p53Y220C).1 It stabilizes the conformation of p53Y220C, induces sequence-specific DNA binding, and restores wild-type p53 function.2 Rezatapopt decreases the proliferation of NUGC-3 gastric carcinoma cells (IC50 = 504 nM).1 It also reduces tumor growth in an NUGC-3 mouse xenograft model at 25 and 50 mg/kg and induces tumor regression at 100 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Vu, B.T., Dominique, R., Fahr, B.J., et al. Discovery of rezatapopt (PC14586), a first-in-class, small-molecule reactivator of p53 Y220C mutant in development. ACS Med. Chem. Lett. 16(1), 34-39 (2024).

    2. Puzio-Kuter, A.M., Xu, L., McBrayer, M.K., et al. Restoration of the tumor suppressor function of Y220C-Mutant p53 by Rezatapopt, a small-molecule reactivator. Cancer Discov. 15(6), 1159-1179 (2025).