CB-103

Notch信号抑制剂；与RBPJ的BTD结构域结合并抑制RBPJ-NICD转录复合物的组装；抑制表达小鼠Notch1、-2、-3或-4的HeLa细胞中配体诱导的Notch信号（IC50s分别为1.5、0.9、1.1和2.9µM）；降低RPMI-8402T-ALL细胞中Notch靶基因HES1、MYC和DTX1的表达；在25mg/kg剂量下，在HCC-1187小鼠异种移植模型中缩小肿瘤体积并增加存活率。An inhibitor of Notch signaling; binds to the BTD domain of RBPJ and inhibits the assembly of the RBPJ-NICD transcription complex; inhibits ligand-induced Notch signaling in HeLa cells expressing mouse Notch1, -2, -3, or -4 (IC50s = 1.5, 0.9, 1.1, and 2.9 µM, respectively); reduces expression of the Notch target genes HES1, MYC, and DTX1 in RPMI-8402 T-ALL cells; reduces tumor volume and increases survival in an HCC-1187 mouse xenograft model at 25 mg/kg.分子式C15H18N2O分子量242.3NC1=CC=C(OC2=CC=C(C(C)(C)C)C=C2)N=C1