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

基本信息物理化學(xué)性質(zhì) 應(yīng)用領(lǐng)域常見(jiàn)問(wèn)題列表

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(xué)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.

常見(jiàn)問(wèn)題列表

概述

XP-524 是一種有效的 BET 和 EP300 抑制劑。XP-524 在體內(nèi)顯示出強(qiáng)大的殺腫瘤活性。 XP-524 可防止 KRAS 誘導(dǎo)的體內(nèi)腫瘤轉(zhuǎn)化，并延長(zhǎng)兩種侵襲性 PDAC 轉(zhuǎn)基因小鼠模型的存活時(shí)間。XP-524 還增強(qiáng)了自身肽的表達(dá)和將腫瘤細(xì)胞向細(xì)胞毒性 T 淋巴細(xì)胞的募集。XP-524 具有研究胰腺導(dǎo)管腺癌（PDAC）的潛力。