SR-5037 is an orally active CDK12 (IC50 = 31 nM)/CDK13 inhibitor and CycK (DC50 = 30 nM,Dmax > 98%) molecular glue degrader. SR-5037 inhibits the enzymatic activity of CDK12/CycK and CDK13/CycK complexes. SR-5037 promotes the recruitment of DDB1 to the CDK12/CycK complex, thereby triggering proteasome-mediated CycK degradation. SR-5037 degrades active CycK in mouse models of triple-negative breast cancer. SR-5037 can be used in the research of cancers such as triple-negative breast cancer[1].
Molekulargewicht:
535.34
CAS Nummer:
[2387704-74-5]
Formel:
C21H18Cl2F2N10O
Target-Kategorie:
CDK,Molecular Glues
Anwendungsbeschreibung:
MCE Product type: Reference compound
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