Synonyms: compound 23 [PMID: 38316747]
Compound class:
Synthetic organic
Comment: This is a PROTAC degrader that targets the Son-of-sevenless homologue 1 (SOS1) protein [1] as a mechanism to disrupt RAS activation in cancers, particularly for potential to improve the antitumour response to KRASG12C inhibitors. PROTAC 23 engages SOS1 via a target-specific warhead (BI3406) that is linked to a ligand that engages the VHL E3 ubiquitin ligase.
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Bioactivity Comments |
DC50 for SOS1 degradation is ~50 nM in a range of cancer cell lines with wild-type and mutant KRAS [1]. |