Synonyms: compound 13ba [PMID: 38007910] | LWY-713
Compound class:
Synthetic organic
Comment: LWY713 is a FLT3 PROTAC degrader [1]. It combines a gilteritinib warhead to bind FLT3 with a lenalidomide-based cereblon E3 ubiquitin ligase bait ligand. It effectively induces FLT3 proteasomal degradation, inhibits FLT3 signalling and reduces proliferation in appropriate cellular assays. LWY713 is active in MV4-11 (FLT3-activated cells) xenograft models.
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Bioactivity Comments |
DC50 is 0.64 nM, achieving ~95% FLT3 degradation by 20 hours [1]. |
Selectivity at catalytic receptors | ||||||||||||||||||||||||||||||||||
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