SOS1-IN-17 (Compound 8d) is an orally active inhibitor targeting the SOS1-KRASG12C interaction, with an IC50 of 5.1 nM. It suppresses ERK phosphorylation in DLD-1 cells with an IC50 of 18 nM and demonstrates antiproliferative activity in KRASG12C-mutant Mia-Paca-2 cells, with an IC50 of 0.11 µM. In mouse models, SOS1-IN-17 shows antitumor efficacy against pancreatic cancer.
Molekulargewicht:
541.61
Formel:
C29H34F3N5O2
Target-Kategorie:
Ras|||Raf
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