MBQ-167

一种Rac和Cdc42的双重抑制剂（IC50值分别为103nM和78nM）；在250nM浓度下，减少Rac和Cdc42的GTP结合和GTP酶活性，并限制MDA-MB-231细胞的迁移和乳腺球形成；在250nM浓度下，单独或与拉帕替尼联合使用时，降低对拉帕替尼耐药的SK-BR-3和MDA-MB-435细胞的细胞活性并诱导凋亡；在200µM浓度下，降低酿酒酵母（S.cerevisiae）的生长速率、轴向出芽和Cdc42活性；在MDA-MB-435小鼠异种移植模型中，以每周三次、每次1或10mg/kg的剂量腹腔注射，可减少肿瘤生长。A dual inhibitor of Rac and Cdc42 (IC50s = 103 and 78 nM, respectively); reduces Rac and Cdc42 GTP-binding and GTPase activity and limits migration and mammosphere formation in MDA-MB-231 cells at 250 nM; reduces cell viability and induces apoptosis at 250 nM in lapatinib-resistant SK-BR-3 and MDA-MB-435 cells alone or with lapatinib; reduces growth rates, axial budding, and Cdc42 activity in S. cerevisiae at 200 µM; reduces tumor growth in an MDA-MB-435 mouse xenograft model at 1 or 10 mg/kg three times per week, i.p.分子式C22H18N4分子量338.4CCN1C2=CC=CC=C2C3=CC(N4N=NC=C4C5=CC=CC=C5)=CC=C31