PTC-596

BMI1抑制剂；抑制MOLM-13 AML和Rec-1 MCL癌细胞的增殖（IC50分别为22.4和136nM）；诱导相同细胞中的BMI1降解和凋亡；减少微管聚合并诱导MM.1S多发性骨髓瘤细胞在G2/M期细胞周期停滞；减少Rec-1细胞中的侧群细胞数量（IC50=138nM）；以5mg/kg口服剂量增加MOLM-13小鼠异种移植模型中的存活率。A BMI1 inhibitor; inhibits proliferation of MOLM-13 AML and Rec-1 MCL cancer cells (IC50s = 22.4 and 136 nM, respectively); induces BMI1 degradation in, and apoptosis of, the same cells; reduces microtubule polymerization and induces cell cycle arrest at the G2/M phase in MM.1S multiple myeloma cells; decreases the number of side population cells in Rec-1 cells (IC50 = 138 nM); increases survival in a MOLM-13 mouse xenograft model at 5 mg/kg, p.o.分子式C19H13F5N6分子量420.3FC1=CC2=C(N=C(C)N2C3=NC(NC4=CC=C(C(F)(F)F)C=C4)=C(F)C(N)=N3)C=C1