ABBV-744|2138861-99-9|-陌孚医药/Medlife

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ABBV-744

目录号: PL12275 纯度: ≥99%

CAS No. :2138861-99-9

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中文名称	ABBV-744
中文别名	ABBV-744
英文名称	ABBV-744
英文别名	ABBV-744;ABBV744;9MX546E2SF;ABBV 744;N-ethyl-4-(2-(4-fluoro-2,6-dimethylphenoxy)-5-(2-hydroxypropan-2-yl)phenyl)-6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridine-2-carboxamide;N-ethyl-4-[2-(4-fluoro-2,6-dimethylphenoxy)-5-(2-hydroxypropan-2-yl)phenyl]-6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridine-2-carboxamide;HWV;N-Ethyl-4-(2-(4-fluoro-2,6-dimethylphenoxy)-5-(2-hydroxypropan-2-yl)phenyl)-6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo(2,3-C)pyridine-2-carboxamide;C
Cas No.	2138861-99-9
分子式	C₂₈H₃₀FN₃O₄
分子量	491.55
包装储存	4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

产品详情

ABBV-744 是一种首创，具有口服活性和选择性的 BET 家族蛋白 BDII 结构域 (BDII domain)，对 BRD2、BRD3、BRD4 和 BRDT 的 IC₅₀ 值为 4~18 nM。ABBV-744 主要由 CYP3A4 代谢，具有类似药物的特性，可用于研究其抗肿瘤功效和耐受性。

生物活性

ABBV-744 is a first-in-class, orally active and selective inhibitor of the BDII domain of BET family proteins with IC 50 values ranging from 4 to 18 nM for BRD2, BRD3, BRD4 and BRDT. ABBV-744 is primarily metabolized by CYP3A4 with drug-like properties enable the investigation of its antitumor efficacy and tolerability.

性状

Solid

IC50 & Target[1][2]

BRD2 (BD2) 8 nM (IC50) BRD3 (BD2) 13 nM (I

体外研究(In Vitro)

ABBV-744 (90 nM; 0~24 h; LNCaP cells) downregulates the expression of KLK2 and MYC genes.
ABBV-744 (90 nM; 0~72 h; LNCaP cells) induces cell cycle arrest in G1 followed by senescence. has not independently confirmed the accuracy of these methods. They are for reference only.Western Blot Analysis

体内研究(In Vivo)

ABBV-744 (4.7 mg/kg; oral gavage; 28 days) causes a delay in tumor growth and displays equivalent or better antitumor activity compared with ABBV-075.
ABBV-744 (30 mg/kg; 14 days) is able to produce significant antitumor activity. ABBV-744 (30 mg/kg) triggers a reduction in platelets of only 20 %. 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, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

ClinicalTrial

参考文献

[1]. Faivre EJ, et al. Selective inhibition of the BD2 bromodomain of BET proteins in prostate cancer. Nature. 2020;578(7794):306-310.

溶解度数据	In Vitro: DMSO : 100 mg/mL (203.44 mM; Need ultrasonic)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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