2344825-52-9
中文名称
化合物 XP-524
英文名称
Ethanesulfonamide, N-[6-(6,7-dihydro-1-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridin-3-yl)-1-(1,1-di-2-pyridinylethyl)-1H-indol-4-yl]-
CAS
2344825-52-9
分子式
C30H28N6O3S
分子量
552.65
MOL 文件
2344825-52-9.mol
2344825-52-9 结构式
基本信息
中文别名
化合物 XP-524 英文别名
Ethanesulfonamide, N-[6-(6,7-dihydro-1-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridin-3-yl)-1-(1,1-di-2-pyridinylethyl)-1H-indol-4-yl]-应用领域
用途一
XL-223 is a potent BET inhibitor effective in endocrine-resistant ER+ breast cancer with acquired resistance to fulvestrant and palbociclib. XL-223 was more potent in MCF-7:CFR cells than six BET inhibitors in clinical trials. Transcriptomic analysis differentiated XL-223 from the benchmark BETi, JQ-1, showing downregulation of oncogenes and upregulation of tumor suppressors and apoptosis. The therapeutic approach was validated by oral administration of XL-223 in orthotopic xenografts of endocrine-resistant breast cancer in monotherapy and in combination with fulvestrant. Importantly, at an equivalent dose in rats, thrombocytopenia was mitigated.