Identification | Back Directory | [Name]
SIAIS178 | [CAS]
2376047-73-1 | [Synonyms]
SIAIS178 | [Molecular Formula]
C50H62ClN11O6S2 | [MDL Number]
MFCD32689531 | [Molecular Weight]
1012.68 |
Hazard Information | Back Directory | [Description]
SIAIS178 is a potent BCR-ABL Degrader. SIAIS178 induces proper interaction between BCR-ABL and VHL ligase leading to effective degradation of BCR-ABL protein, achieves significant growth inhibition of BCR-ABL+ leukemic cells in vitro, and induces substantial tumor regression against K562 xenograft tumors in vivo. In addition, SIAIS178 also degrades several clinically relevant resistance-conferring mutations. Our data indicate that SIAIS178 as efficacious BCR-ABL degrader warrants extensive further investigation for the treatment of BCR-ABL+ leukemia. |
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