1010732-14-5
中文名稱
Maritoclax
英文名稱
Maritoclax
CAS
1010732-14-5
分子式
C22H12Cl4N2O4
分子量
510.15
MOL 文件
1010732-14-5.mol
1010732-14-5 結(jié)構(gòu)式
基本信息
中文別名
MCL-1抑制劑(MARINOPYRROLE A) 英文別名
MaritoclaxMarinopyrrole A
Methanone, 1,1'-[(1R)-4,4',5,5'-tetrachloro[1,3'-bi-1H-pyrrole]-2,2'-diyl]bis[1-(2-hydroxyphenyl)-
應(yīng)用領(lǐng)域
用途一
Maritoclax, also known as Marinopyrrole A , is a small molecule Mcl-1 inhibitor, which induces Mcl-1 proteasomal degradation without transcriptional downregulation. Maritoclax killed AML cell lines and primary cells with elevated Mcl-1 levels through selective Mcl-1 downregulation, and synergized with ABT-737 to overcome Mcl-1-mediated ABT-737 resistance. Maritoclax was more effective than daunorubicin at inducing leukemic cell death when co-cultured with HS-5 bone marrow stroma cells, while being less toxic than daunorubicin against HS-5 stroma cells, primary mouse bone marrow cells, and hematopoietic progenitor cells. Moreover, maritoclax administration at 20 mg/kg/d intraperitoneally caused significant U937 tumor shrinkage, as well as 36% tumors remission rate in athymic nude mice, without apparent toxicity to healthy tissue or circulating blood cells. In summary, our studies suggest that maritoclax belongs to a novel class of Mcl-1 inhibitors that has the potential to be developed for the treatment of AML. ( Cancer Biol Ther. 2014 Aug;15(8):1077-86. )