KT-253 is a p53 stabilizer and a PROTAC degrader of MDM2 (DC50=0.4 nM). KT-253 inhibits the proliferation of RS4;11 cancer cells (IC50 is 0.3 nM), arrests the cell cycle at the G2/M phase, and induces apoptosis. KT-253 exhibits antitumor activity in mouse models. (Pink: ligand for target protein MDM2 ligand 4; Black: linker; Blue: ligand for E3 ligase cereblon)

Physicochemical Properties

Molecular Formula	C48H52CL2FN7O6
Molecular Weight	912.87
CAS #	2713618-08-5
SMILES	ClC1C=CC2=C(C=1)NC([C@@]12[C@@H](C2C=CC=C(C=2F)Cl)[C@H](C(NC2CCC(C(N3CCC(C4=CC=C5C(=C4)N(C)C(N5C4C(NC(CC4)=O)=O)=O)CC3)=O)CC2)=O)NC21CCCCC2)=O
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

References

[1]. 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.

Solubility Data

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	1.0954 mL	5.4772 mL	10.9545 mL
	5 mM	0.2191 mL	1.0954 mL	2.1909 mL
	10 mM	0.1095 mL	0.5477 mL	1.0954 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.