Setidegrasib is a PROTAC-mediated KRAS degrader (DC50: 37 nM). Setidegrasib induces the formation of a ternary complex between KRAS G12D and the VHL E3 ubiquitin ligase, thereby facilitating the ubiquitination and proteasomal degradation of the oncogenic protein. Setidegrasib inhibits the levels of p-ERK, p-AKT, and p-S6 in AsPC-1 cells. Setidegrasib demonstrates antitumor activity in various mouse xenograft models of cancer. Setidegrasib can be used to study solid tumors with KRAS(G12D) mutations.
Molekulargewicht:
1117.3
Reinheit:
99.49%
CAS Nummer:
[2821793-99-9]
Formel:
C60H65FN12O7S
Target-Kategorie:
PROTACs|||Kras|||Ras
T74663
T74663
* Mehrwertsteuer und Versandkosten nicht enthalten. Irrtümer und Preisänderungen vorbehalten
