SB-1317

多激酶抑制剂；抑制各种CDK（IC50s=3-9nM）以及JAK家族激酶（IC50s=14-59nM）、野生型和突变型FLT3（IC50s=19-27nM）和Src家族激酶（IC50s=11-15nM）；抑制12种液体和6种实体肿瘤细胞系的增殖（平均IC50=0.19µM）；诱导MV4-11AML细胞在G1期细胞周期停滞和凋亡；在10、20和40mg/kg的剂量下，减少肿瘤体积并增加MV4-11小鼠异种移植模型中的存活率。A multi-kinase inhibitor; inhibits various CDKs (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); inhibits proliferation in a panel of 12 liquid and six solid tumor cell lines (mean IC50 = 0.19 µM); induces cell cycle arrest at the G1 phase and apoptosis in MV4-11 AML cells; reduces tumor volume and increases survival in an MV4-11 mouse xenograft model at 10, 20, and 40 mg/kg.