CF53,1808160-52-2

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CF53

CAS No. : 1808160-52-2

MCE 国际站：CF53

产品活性：CF53 是一种高效、选择性、可口服的 BET 抑制剂，对 BRD4 BD1 的 K_i 值为 <1 nM，K_d 值为 2.2 nM，IC₅₀ 值为 2 nM；CF53 对 BRD2，BRD3，BRD4 和 BRDT BET 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。

研究领域：Epigenetics

作用靶点：Epigenetic Reader Domain  |  Histone Acetyltransferase

In Vitro: CF53 (Compound 28) binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, K_ds 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.
CF53 exhibits IC₅₀s of 7, 85 nM against MOLM-13 acute leukemia and MDA-MB-231 breast cancer cell lines, respectively.

In Vivo: 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.

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