2713618-08-5
Chemical Structure
Seldegamadlin
Synonym(s): KT-253
- CAS No.: 2713618-08-5
- Formula:C48H52Cl2FN7O6
- Molecular Weight:912.87
InChIKey: CQFHGOWYJXQICA-ZTNLUFLKSA-N
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
Biological Activity: Seldegamadlin (KT-253) is a cereblon-recruiting PROTAC degrader of MDM2, with a DC50 of 0.4 nM. Seldegamadlin catalyzes the ubiquitination and proteasomal degradation of MDM2, disrupts the MDM2/p53 autoregulatory feedback loop, induces apoptosis, caspase activation and p53 target gene expression, and inhibits the growth of wild-type p53 hematologic tumor cells and solid tumor cells. Seldegamadlin is applicable for the research of acute myeloid leukemia, acute lymphoblastic leukemia, diffuse large B-cell lymphoma and wild-type p53 solid tumors[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
Seldegamadlin | 98.53% | Seldegamadlin (KT-253) is a cereblon-recruiting PROTAC degrader of MDM2, with a DC50 of 0.4 nM. Seldegamadlin catalyzes the ubiquitination and proteasomal degradation of MDM2, disrupts the MDM2/p53 autoregulatory feedback loop, induces apoptosis, caspase activation and p53 target gene expression, and inhibits the growth of wild-type p53 hematologic tumor cells and solid tumor cells. Seldegamadlin is applicable for the research of acute myeloid leukemia, acute lymphoblastic leukemia, diffuse large B-cell lymphoma and wild-type p53 solid tumors. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
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. Molecular cancer therapeutics. 2025 Apr 02;24(4):497-510. [Content Brief]
- [2]. Ji N, et al. Mdm2 degraders and uses thereof. WO2021188948A1. WIPO. 2021-09-23.
