SIAIS056 is a BCR-ABL PROTAC degrader that effectively targets and degrades BCR-ABL fusion proteins, displaying a potent DC50 value of 0.18 nM. It inhibits the BCR-ABL signaling pathway in a time-dependent manner, leading to reduced phosphorylation of BCR-ABL as well as downstream effectors like STAT5 and CRKL in K562 cells. Additionally, SIAIS056 demonstrates the ability to degrade various BCR-ABL resistance mutations and exhibits significant anti-proliferative effects, resulting in marked tumor regression in K562 xenograft models. This compound is valuable for research in leukemia.
SIAIS056 is a BCR-ABL PROTAC degrader that effectively targets and degrades BCR-ABL fusion proteins, displaying a potent DC50 value of 0.18 nM. It inhibits the BCR-ABL signaling pathway in a time-dependent manner, leading to reduced phosphorylation of BCR-ABL as well as downstream effectors like STAT5 and CRKL in K562 cells. Additionally, SIAIS056 demonstrates the ability to degrade various BCR-ABL resistance mutations and exhibits significant anti-proliferative effects, resulting in marked tumor regression in K562 xenograft models. This compound is valuable for research in leukemia.
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