AG-636

一种二氢乳清酸脱氢酶（DHODH）抑制剂（IC50=17nM）；在1µM浓度下，可使六种细胞系中尿苷琥珀酸和二氢乳清酸（DHO）的水平升高；在100mg/kg剂量下，可诱导OCI-Ly19弥漫大B细胞淋巴瘤（DLBCL）小鼠异种移植模型中肿瘤完全停滞，并在Z-138小鼠异种移植模型中诱导肿瘤完全消退；在Z-138和JeKo-1淋巴瘤小鼠异种移植模型中，可增加DHO水平并降低嘧啶水平。A DHODH inhibitor (IC50 = 17 nM); increases levels of ureidosuccinic acid and DHO in a panel of six cell lines at 1 µM; induces complete tumor stasis in an OCI-Ly19 DLBCL mouse xenograft model and complete tumor regression in a Z-138 mouse xenograft model at 100 mg/kg; increases DHO levels and reduces pyrimidine levels in Z-138 and JeKo-1 lymphoma mouse xenograft models.分子式C21H17N3O2分子量343.4O=C(C1=CC(C2=CC=C(C3=C(C)C=CC=C3)C=C2)=CC4=C1N(C)N=N4)O