Rezatapopt analog-1
Rezatapopt analog-1 (PC14586 analog-1) (1919) is a Rezatapopt (HY-156633) analog. Rezatapopt binds to a pocket created by the TP53 Y220C mutation. Rezatapopt restores p53 tumor suppressor functions by stabilization of the p53 protein structure.
For research use only. We do not sell to patients.
- CAS No.: 2636846-37-0
- Formula: C27H28F4N4O3
- Molecular Weight:532.53
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NUGC-3 | IC50 |
0.99 μM
Compound: 24
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Cytotoxicity against human NUGC-3 cells harboring TP53 Y220C mutant assessed as reduction in cell viability incubated for 5 days by MTT assay
Cytotoxicity against human NUGC-3 cells harboring TP53 Y220C mutant assessed as reduction in cell viability incubated for 5 days by MTT assay
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[PMID: 39811143] |
Chemical Information
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CAS No. 2636846-37-0
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Molecular Weight 532.53
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Formula C27H28F4N4O3
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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(O)=O)OC
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Synonyms
PC14586 analog-1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Genotoxicity/Mutagenicity Study
The bacterial reverse mutation assay detects point mutations that restore amino-acid prototrophy in auxotrophic Salmonella typhimurium or Escherichia coli tester strains; after exposure to a test article, mutagenic activity is read out as an increased number of revertant colonies on minimal agar compared with the vehicle control. The assay uses tester strains with different mutation targets so that base-substitution and frameshift mutagens can be detected, and testing is performed with and without exogenous mammalian metabolic activation because some chemicals require biotransformation to become mutagenic.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)