Seldegamadlin

Seldegamadlin (KT-253) is a selective p53 stabilizer and a MDM2 PROTAC degrader (DC50 = 0.4 nM) . Seldegamadlin 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. Seldegamadlin upregulates p53 activity and overcomes the p53-MDM2 feedback loop. Seldegamadlin can be used for the study of hematologic and solid tumors, such as acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL) . (Pink: ligand for target protein MDM2 ligand 4 (HY-170452) ; Black: linker (HY-W001478) ; Blue: ligand for E3 ligase cereblon (HY-163927) ) [1][2][3][4].

Product Specifications

CAS Number

[2713618-08-5]

Product Name Alternative

KT-253

UNSPSC

12352005

Target

Apoptosis; MDM-2/p53; PROTACs

Related Pathways

Apoptosis; PROTAC

Applications

Cancer-programmed cell death

Field of Research

Cancer

Purity

98.53

Solubility

DMSO : 95 mg/mL (ultrasonic)

Smiles

ClC1=CC2=C([C@]3(C4(CCCCC4)N[C@@H](C(N[C@H]5CC[C@H](C(N6CCC(C7=CC=C8C(N(C)C(N8C9CCC(NC9=O)=O)=O)=C7)CC6)=O)CC5)=O)[C@@H]3C%10=C(F)C(Cl)=CC=C%10)C(N2)=O)C=C1

Molecular Formula

C48H52Cl2FN7O6

Molecular Weight

912.87

References & Citations

[1]Yogesh Chutake, KT-253, a highly potent and selective heterobifunctional MDM2 degrader for the treatment of wildtype p53 tumors with superior potency and differentiated biological activity compared to small molecule inhibitors (SMI) . |[2]Min Lu, et al. KT-253, a Highly Potent and Selective MDM2 Protein Degrader, Eliminates Malignant Myelofibrosis Stem/Progenitor Cells. Blood. Volume 144, Supplement 1, 5 November 2024, Page 3588.|[3]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. 2025;24 (4) :497-510.|[4]Nancy Dumont, et al. Predictive Markers of Response to the MDM2 Degrader KT-253.