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2344825-52-9

中文名稱 化合物 XP-524
英文名稱 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 結(jié)構(gòu)式 2344825-52-9 結(jié)構(gòu)式

基本信息

中文別名
化合物 XP-524
英文別名
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]-

物理化學性質(zhì)

密度1.36±0.1 g/cm3(Predicted)
酸度系數(shù)(pKa)9.13±0.30(Predicted)
形態(tài)Solid
顏色Light yellow to light brown

應(yīng)用領(lǐng)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.
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