商品介绍

Product Introduction

Bioactivity

名称	BETd-260
描述	BETd-260, a PROTAC linked by a Cereblon ligand and a BET ligand, has an inhibitory effect on BRD4 protein in leukemic cell lines.
体外活性	BETd-260 (ZBC260; Compound 23) 促进了BRD2、BRD3和BRD4蛋白的降解。对于RS4;11白血病细胞,测得的IC50为51 pM。在MOLM-13细胞中,BETd-260的IC50为2.2 nM。3-10 nM的BETd-260能够诱导RS4;11和MOLM-13细胞凋亡。此外,BETd-260抑制了抗凋亡基因Mcl-1、Bcl-2、c-Myc和XIAP的转录和翻译,并增加了肝癌细胞中促凋亡基因Bad的转录和翻译[1]。
体内活性	BETd-260(5 mg/kg,静脉注射）能在超过24小时内降解RS4;11异种移植小鼠模型中的BRD2、BRD3和BRD4蛋白,同时伴有PARP和caspase-3的显著切割以及c-Myc蛋白的强烈下调[1]。通过每隔一天、每周三次、连续三周以5 mg/kg剂量静脉注射BETd-260,可以在携带RS4;11异种移植瘤的小鼠中迅速引起肿瘤退化,最大退化率超过90%,且在小鼠中未观察到体重减轻或其他毒性迹象。
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
溶解度	DMSO : 22.5 mg/mL (28.2 mM), Sonication is recommended. H2O : Insoluble, insoluble
关键字	ZBC-260 \| ZBC260 \| PROTAC \| EpigeneticReaderDomain \| Epigenetic Reader Domain \| BRD4 \| BETd-260
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