| Identification | Back Directory | [Name]
(3'R,4'S,5'R)-6"-chloro-4'-(3-chloro-2-fluorophenyl)-N-((1r,4R)-4-(4-(1-(2,6-dioxopiperidin-3-yl)-3-methyl-2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)piperidine-1-carbonyl)cyclohexyl)-2''-oxodispiro[cyclohexane-1,2'-pyrrolidine-3',3"-indoline]-5'-carboxamide | [CAS]
2713618-08-5 | [Synonyms]
KT-253
(3'R,4'S,5'R)-6"-chloro-4'-(3-chloro-2-fluorophenyl)-N-((1r,4R)-4-(4-(1-(2,6-dioxopiperidin-3-yl)-3-methyl-2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)piperidine-1-carbonyl)cyclohexyl)-2''-oxodispiro[cyclohexane-1,2'-pyrrolidine-3',3"-indoline]-5'-carboxamide | [Molecular Formula]
C48H52Cl2FN7O6 | [MOL File]
2713618-08-5.mol | [Molecular Weight]
912.88 |
| Hazard Information | Back Directory | [Uses]
KT-253 is a p53 stabilizer and a PROTAC degrader for MDM2 (DC50=0.4 nM). KT-253 inhibits the proliferation of cancer cell RS4;11 with an IC50 of 0.3 nM, arrests the cell cycle at G2/M phase, and induces apoptosis. KT-253 exhibits antitumor efficacy in mouse models[1]. (Pink: ligand for target protein MDM2 ligand 4 (HY-170452); Black: linker (HY-W001478); Blue: ligand for E3 ligase cereblon (HY-163927)) | [References]
[1] Chutake YK, et al., KT-253, A Novel MDM2 Degrader and p53 Stabilizer, Has Superior Potency and Efficacy Than MDM2 Small Molecule Inhibitors. Mol Cancer Ther. 2024 Dec 9. DOI:10.1158/1535-7163.MCT-24-0306 |
|
|