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.
Molecular Weight:
1117.3
Purity:
99.49%
CAS Number:
[2821793-99-9]
Formula:
C60H65FN12O7S
Target:
PROTACs|||Kras|||Ras
T74663
T74663
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