产品描述:
A1874 is a proteolysis-targeting chimera (PROTAC) that contains (+)-JQ1 (Item No. 11187), an inhibitor of bromodomain and extra terminal domain (BET) bromodomains, conjugated to RG7388 (Item No. 21532), an inhibitor of the MDM2-p53 interaction.{69840} It induces the degradation of bromodomain-containing protein 4 (BRD4), decreases the levels of c-Myc, and increases the levels of p53 and p21 in HCT116 colorectal cancer cells when used at a concentration of 10 µM. A1874 (1 µM) reduces the proliferation of wild-type p53-expressing HCT116 and A375 melanoma cells but not p53 mutant-expressing NCI H2030 lung and HT-29 colon cancer cells. It decreases cell viability and induces cell cycle arrest at the G1 phase in, and reduces colony formation by, pCAN1 colon cancer cells when used at a concentration of 500 nM.{69841} In vivo, A1874 (20 mg/kg per day) decreases tumor volume, weight, and growth in a pCAN1 mouse xenograft model.