CF53是一种高效、选择性、可口服的BET抑制剂，对BRD4BD1的Ki值为<1nM，Kd值为2.2nM，IC50值为2nM；CF53对BRD2，BRD3，BRD4和BRDTBET蛋白的BD1和BD2两个结构域都有高亲和性，对其选择性远高于非含溴结构域BET蛋白。CF53在体外和体内都具有显著的抗肿瘤活性[1]货号:ajcx12864
CAS:1808160-52-2
分子式:C24H25N7O2
分子量：443.5
溶解度:DMSO : 110 mg/mL (248.03 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a Ki of<1 nM, Kd of 2.2 nM and an IC50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo[1].

CF53 (Compound 28) binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, Kds are 1.1 nM (BRD2 BD1), 0.6 nM (BRD2 BD2), 0.52 nM (BRD3 BD1), 0.49 nM (BRD3 BD2), 0.8 nM (BRD4 BD2), 2 nM (BRDT BD1), 2.1 nM (BRDT BD2), 47 nM (CREBBP), 570 nM (CECR2), 110 nM (EP300), respectively[1].CF53 exhibits IC50s of 7, 85 nM against MOLM-13 acute leukemia and MDA-MB-231 breast cancer cell lines, respectively[1].

CF53 (25, 50 mg/kg, p.o.) exhibits potent anti-tumor activity both in MDA-MB-231 xenograft tumor model and in RS4;11 model in mice[1].

[1]. Zhao Y, et al. Structure-Based Discovery of CF53 as a Potent and Orally Bioavailable Bromodomain and Extra-Terminal (BET) Bromodomain Inhibitor. J Med Chem. 2018 Jul 26;61(14):6110-6120.