PROTAC ALK degrader-3

PROTAC ALK degrader-3 (Compound 4B) (72 h) potently inhibits the proliferation of Karpas 299 cells, with an IC₅₀ value of 3.11 nM^[1].
PROTAC ALK degrader-3 (20-1000 nM; 3-48 h) induces concentration-dependent degradation of NPM-ALK in Karpas 299 cells, with a DC₅₀ of 119.33 nM and a D_max of 97.1%^[1].
PROTAC ALK degrader-3 (20-200 nM; 3-48 h) induces degradation of NPM-ALK, inhibition of p-ALK, and over 80% inhibition of p-STAT3 without altering total STAT3 levels in Karpas 299 cells^[1].
PROTAC ALK degrader-3 (200 nM; 2 h pretreatment followed by 24 h co-treatment) induces degradation of NPM-ALK in Karpas 299 cells via the ubiquitin-proteasome system, and this process depends on the binding of CRBN E3 ligase to ALK^[1].
PROTAC ALK degrader-3 (72 h) inhibits the proliferation of Ba/F3-EML4-ALK wild-type and mutant cell lines (C1156Y, L1196M, G1202R, G1202R-L1196M) with IC₅₀ values ranging from 27.25 nM to 215.2 nM, and shows no activity against parental Ba/F3 cells^[1].
PROTAC ALK degrader-3 (20-500 nM; 48 h) induces 52% degradation of EML4-ALK^G1202R[1].