Bioactivity | 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)) |
CAS | 2713618-08-5 |
Formula | C48H52Cl2FN7O6 |
Molar Mass | 912.87 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. |