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SB-1317 is a multi-kinase inhibitor.1 It inhibits Cdk1, -2, -3, -5, and -9 (IC50s = 3-9 nM), as well as JAK family kinases (IC50s = 14-59 nM), wild-type and mutant FLT3s (IC50s = 19-27 nM), and Src family kinases (IC50s = 11-15 nM). SB-1317 inhibits proliferation in a panel of 12 liquid and six solid tumor cell lines (mean IC50 = 0.19 µM). It induces cell cycle arrest at the G1 phase and apoptosis in MV4-11 acute myeloid leukemia (AML) cells. SB-1317 (10, 20, and 40 mg/kg) reduces tumor volume and increases survival in an MV4-11 mouse xenograft model.
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1. TG02, a novel oral multi-