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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).
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Ying Kong
Xinyue Zhao
Zhaofu Wang
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Kong et al. (Thu,) studied this question.
www.synapsesocial.com/papers/68e5e0e0b6db643587574c20 — DOI: https://doi.org/10.1158/1535-7163.26423434.v1
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