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Evaluation of the cytotoxicity of compounds AG1, AG2, AG3, and RK349 . a ) MTT assays for AGS and NUGC3 cells treated with increasing concentrations of AG2 (top) and AG3 (bottom) for 48 h ( n = 3). b ) Mean (-/+ SD) IC 50 and IC 75 values of the different compounds in the indicated cell line treated for 48 h ( n = 3). NR: not reached. c ) Graphic representation of the selectivity of each compound using the ratio of IC 50 for AGS (p53 WT) and NUGC3 (p53 Y220C) cells indicated in b and Fig S3b . d ) Representative wells of a clonogenic assay performed with NUGC3 cells treated or not (NT) for 48 h with oxaliplatin (IC 25 , 12 µM) and/or AG3 (IC 50 , 18 µM) ( n = 3). e ) Quantification of clonogenic assays performed as described in d , with the number of colonies obtained for non-treated cells set at 100%. ( n = 3). f ) MTT assays for <t>BxPC3</t> cells treated with increasing concentrations of AG3 for 48 h. g ) MTT assays for HCT116 and SW480 cells treated with increasing concentrations of RK349 and AG3 for 48 h.
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Evaluation of the cytotoxicity of compounds AG1, AG2, AG3, and RK349 . a ) MTT assays for AGS and NUGC3 cells treated with increasing concentrations of AG2 (top) and AG3 (bottom) for 48 h ( n = 3). b ) Mean (-/+ SD) IC 50 and IC 75 values of the different compounds in the indicated cell line treated for 48 h ( n = 3). NR: not reached. c ) Graphic representation of the selectivity of each compound using the ratio of IC 50 for AGS (p53 WT) and NUGC3 (p53 Y220C) cells indicated in b and Fig S3b . d ) Representative wells of a clonogenic assay performed with NUGC3 cells treated or not (NT) for 48 h with oxaliplatin (IC 25 , 12 µM) and/or AG3 (IC 50 , 18 µM) ( n = 3). e ) Quantification of clonogenic assays performed as described in d , with the number of colonies obtained for non-treated cells set at 100%. ( n = 3). f ) MTT assays for BxPC3 cells treated with increasing concentrations of AG3 for 48 h. g ) MTT assays for HCT116 and SW480 cells treated with increasing concentrations of RK349 and AG3 for 48 h.

Journal: Journal of Enzyme Inhibition and Medicinal Chemistry

Article Title: In vitro screening of compounds for targeting gastric cancer with Y220C p53 mutation: a molecule combining zinc chelation and a Michael acceptor drives CDKN1 and BBC3 expression to restore a p53-dependent cytotoxicity

doi: 10.1080/14756366.2026.2638836

Figure Lengend Snippet: Evaluation of the cytotoxicity of compounds AG1, AG2, AG3, and RK349 . a ) MTT assays for AGS and NUGC3 cells treated with increasing concentrations of AG2 (top) and AG3 (bottom) for 48 h ( n = 3). b ) Mean (-/+ SD) IC 50 and IC 75 values of the different compounds in the indicated cell line treated for 48 h ( n = 3). NR: not reached. c ) Graphic representation of the selectivity of each compound using the ratio of IC 50 for AGS (p53 WT) and NUGC3 (p53 Y220C) cells indicated in b and Fig S3b . d ) Representative wells of a clonogenic assay performed with NUGC3 cells treated or not (NT) for 48 h with oxaliplatin (IC 25 , 12 µM) and/or AG3 (IC 50 , 18 µM) ( n = 3). e ) Quantification of clonogenic assays performed as described in d , with the number of colonies obtained for non-treated cells set at 100%. ( n = 3). f ) MTT assays for BxPC3 cells treated with increasing concentrations of AG3 for 48 h. g ) MTT assays for HCT116 and SW480 cells treated with increasing concentrations of RK349 and AG3 for 48 h.

Article Snippet: BxPC3 cells (ATCC©, CRL1687) are from pancreatic cancer expressing Y220C mutant p53.

Techniques: Clonogenic Assay