AZD5153 6-Hydroxy-2-naphthoic acid|1869912-40-2|-陌孚医药/Medlife

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AZD5153 6-Hydroxy-2-naphthoic acid

目录号: PL13482 纯度: ≥99%

CAS No. :1869912-40-2

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中文名称	AZD5153 6-Hydroxy-2-naphthoic acid
中文别名	AZD5153结晶体(API形式);BET/BRD4溴结构域抑制剂(AZD5153 6-HYDROXY-2-NAPHTHOIC ACID);AZD51536-羟基-2-萘甲酸;化合物AZD5153 6-HYDROXY-2-NAPHTHOIC ACID
英文名称	AZD5153 6-Hydroxy-2-naphthoic acid
英文别名	AZD5153 (6-Hydroxy-2-naphthoic acid);AZD 5153 6-Hydroxy-2-naphthoic acid;AZD-5153 6-Hydroxy-2-naphthoic acid;AZD5153 6-Hydroxy-2-naphthoic acid;78VBM99SEV;(R)-4-(2-(4-(1-(3-methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-4-yl)phenoxy)ethyl)-1,3-dimethylpiperazin-2-one 6-hydroxy-2-naphthoate;BCP20066;s8344;2-Naphthalenecarboxylic acid, 6-h;AZD5153;AZD5153 (API form);1869912-39-9 FREE BASE;AZD5153 (API form)(1869912-39-9 free base);AZD515;AZD 5153 6-HYDROXY-2-NAPHTHOIC ACID; AZD-5153 6-HYDROXY-2-NAPHTHOIC ACID;AZD-5153 HNT salt
Cas No.	1869912-40-2
分子式	C₃₆H₄₁N₇O₆
分子量	667.75
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

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溴结构域抑制剂; 干扰BRD4的IC₅₀值为1.7nM。

生物活性

AZD5153 6-Hydroxy-2-naphthoic acid is the 6-Hydroxy-2-naphthoic acid of AZD5153. AZD5153 is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor; disrupts BRD4 with an IC 50 of 1.7 nM.

性状

Solid

IC50 & Target[1][2]

IC50: 1.7 nM (BRD4)

体外研究(In Vitro)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Rhyasen GW, et al. AZD5153: A Novel Bivalent BET Bromodomain Inhibitor Highly Active against Hematologic Malignancies. Mol Cancer Ther. 2016 Nov;15(11):2563-2574.

溶解度数据	In Vitro: DMSO : ≥ 34 mg/mL (50.92 mM)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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