AZD5153 6-Hydroxy-2-naphthoic acid,1869912-40-2

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YZ剂描述：

产品名称：AZD5153 6-Hydroxy-2-naphthoic acid

产品别名：AZD-5153 HNT salt；AZD5153

英文别名：AZD-5153 HNT salt;AZD5153

靶点：Epigenetic Reader Domain

CAS：1869912-40-2

纯度：98%

外观：见爱必信官网

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

AZD5153 6-Hydroxy-2-naphthoic acid是AZD5153的6-羟基-2-萘甲酸盐形式。AZD5153是一种有效选择性，有口服活性的BET/BRD4溴结构域YZ剂; 干扰BRD4的IC50值为1.7nM。

溶解性：DMSO : 93 mg/mL (139.3 mM)
Ethanol : 26 mg/mL (38.9 mM)

体外研究：

AZD5153 demonstrates a remarkable enhancement in potency for the displacement of full-length BRD4 relative to BD1, with IC50 values of 5.0 nM and 1.6 μM, respectively. AZD5153 potently disrupts BRD4 foci in U2OS cells with an IC50 value of 1.7 nM. AZD5153 efficiently down-regulates MYC protein levels across the cell line panel irrespective of their sensitivity to AZD5153.

体内研究：Administration of AZD5153 leads to tumor stasis or regression in multiple xenograft models of acute myeloid leukemia, multiple myeloma, and diffuse large B-cell lymphoma. AZD5153 treatment markedly impacts transcriptional programs of MYC, E2F, and mTOR.

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