SOS1-IN-20 (Compound 12f) is an orally active inhibitor of SOS1, exhibiting an IC50 of 5.11 nM against KRASG12C::SOS1. It prevents KRAS activation and its downstream signaling by disrupting the KRAS-SOS1 interaction. In PC-9 cells, it shows an IC50 of 253 nM for p-ERK, while its IC50 for the hERG channel is 16.71 µM. SOS1-IN-20 also inhibits tumor cell proliferation, displaying antitumor activity.
Target-Kategorie:
Ras|||Raf|||Potassium Channel
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