SAR of optimal linker lengths and species in FGFR degraders designed based on BGJ398. Similar to BR-cpd7, Compounds 1-11 were prepared from building block 1 in 3 steps. Including reductive amination of building block 1 with corresponding acetones or aldehydes, deprotection and condensation. HEK293T cells transfected with HiBiT-FGFR1 were treated with FGFR degraders for 36 h. FGFR1 protein level was quantified with Nano-Glo HiBiT (n=3 replicates).
No takes yet. Share an insight, caveat, or question.
Kong et al. (2024) studied this question.
Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context: