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BBT594 is an inhibitor of Bcr-AblT315I (IC50 = 44 nM), a form of the Bcr-Abl fusion protein containing a tyrosine-to-isoleucine substitution at position 315.1 It decreases proliferation in mouse Ba/F3 hematopoietic cells expressing Bcr-AblT315I (GI50 = 117 nM). BBT594 (1 or 5 µM) also inhibits phosphorylation of Jak2 and Stat5 in Ba/F3 cells.2
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1. Rational design of T3151 BCR-
2. Modulation of activation-