SIAIS100 

SIAIS100 is a potent BCR-ABL PROTAC degrader with an DC₅₀ value of 2.7 nM. SIAIS100 can be used to research chronic myeloid leukemia (CML)^[1].

DC₅₀: 2.7 nM ^[1]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

890.44

C₄₄H₅₀ClF₂N₉O₅S

O=C1CCC(C(N1)=O)N2CC3=C(C2=O)C=CC=C3SCCCCCCN4CCN(CC4)C5CCN(CC5)C6=NC=C(C=C6C7=CC=NN7)C(NC8=CC=C(C=C8)OC(F)(Cl)F)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]