SIAIS100 TFA is a potent BCR-ABL PROTAC degrader with an DC50 value of 2.7 nM. SIAIS100 TFA can be used to research chronic myeloid leukemia (CML).
SIAIS100 exhibits anti-proliferative activity against K562 cells with an IC50 value of 12 nM[1].SIAIS100 degrades BCR-ABL with degradation ratio of 81.78% and 91.20% at 5 nM and 100 nM, respectively[1].SIAIS100 (100 nM; 8 h) significantly decreases BCR-ABL in K562 cells[1].SIAIS100 (100 nM; 6 h) induced sustained and robust BCR-ABL degradation and maintained a durable cellular response after drug removal[1].SIAIS100 (1-1000 nM) significantly degrade mutation G250E/T315I dose-dependently accompanied by the inhibition of BCR-ABL signaling assessed by the level of p-BCR-ABL in 32D cells[1].
References:
[1]. Liu H, et al. Discovery and characterization of novel potent BCR-ABL degraders by conjugating allosteric inhibitor. Eur J Med Chem. 2022 Dec 15;244:114810.