BAY-2402234

DHODH抑制剂(IC50=1.2nM)；诱导MOLM-13和HELAML细胞中的CD11b上调（EC50s分别为3.16和0.96nM）；抑制九种白血病细胞系的增殖(IC50s=0.08-8.2nM)；诱导细胞周期停滞在G2/M期并诱导TF-1细胞凋亡；以1.25、2.5和5mg/kg的剂量减小MV4-11小鼠异种移植模型中的肿瘤体积；提高AMLPDX小鼠模型中的存活率。A DHODH inhibitor (IC50 = 1.2 nM); induces CD11b upregulation in MOLM-13 and HEL AML cells (EC50s = 3.16 and 0.96 nM, respectively); inhibits the proliferation of nine leukemia cell lines (IC50s = 0.08-8.2 nM); induces cell cycle arrest at the G2/M phase and apoptosis in TF-1 cells; reduces tumor volume in an MV4-11 mouse xenograft model at 1.25, 2.5, and 5 mg/kg; increases survival in PDX mouse models of AML.分子式C21H18ClF5N4O4分子量520.8O=C1N(C2=CC(O[C@@H](C)C(F)(F)F)=C(C=C2F)C(NC3=C(C=CC=C3F)Cl)=O)N=C(CO)N1CC