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编 号:F734174
分子式:C17H12F3N3O2
分子量:347.29
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PROTAC BCR-ABL1 ligand 1, compound GMB-475, is the ligand of PROTAC that allosterically targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel-Lindau, resulting in ubiquitination and subsequent degradation of BCR-ABL1.

体外研究:
GMB-475 (0-10 μM) exhibits cell proferation with IC50 values of 1.11,1.98,0.37 μM for BCR-ABL1 WT, T315I, G250E cells, respectively.GMB-475 (0-30 μM) induces the degradation of BCR-ABL1 and c-ABL1 with concomitant inhibition of downstream signaling via the STAT5 pathway, in a dose- and time-dependent fashion in the context of both K562 and Ba/F3 cells.
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