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Submit ReviewAZ 13824374
说明： Potent and selective ATAD2 bromodomain inhibitor
化学名： (1R,2R,5S)-11-(8-((1-(2-Fluoro-2-methylpropyl)piperidin-4-yl)amino)-3-methyl-[1,2,4]triazolo[4,3-b]pyridazine-6-carbonyl)-2-isopropyl-2,3,5,6-tetrahydro-1,5-epiminobenzo[d]azocin-4(1H)-one
纯度： ≥98% (HPLC)
生物活性 for AZ 13824374
AZ 13824374 is a potent and selective inhibitor of ATPase family AAA domain-containing protein 2 (ATAD2) bromodomain (pIC50 values are 6.2 and 8.2 in NanoBRET assay and FRET assay, respectively). It is >100-fold selective over a range of epigenetic targets from ROMOscan panel (DiscoveRx Corp.). AZ 13824374 shows cellular target engagement (cellular inhibition pIC50 = 6.9) and antiproliferative activity in a range of breast cancer cell lines.
许可信息
Sold with the permission of AstraZeneca UK Ltd.
技术数据 for AZ 13824374
| 分子量 | 562.69 |
| 公式 | C30H39FN8O2 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 3040082-19-4 |
| PubChem ID | 162422438 |
| InChI Key | NGXAMXNWIHBLBN-JIMJEQGWSA-N |
| Smiles | CC(C)[C@H]1NC([C@@H]2CC3=C([C@H]1N2C(C4=NN5C(C)=NN=C5C(NC6CCN(CC6)CC(F)(C)C)=C4)=O)C=CC=C3)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for AZ 13824374
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 56.27 | 100 | |
| ethanol | 56.27 | 100 |
制备储备液 for AZ 13824374
以下数据基于产品分子量 562.69。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.78 mL | 8.89 mL | 17.77 mL |
| 5 mM | 0.36 mL | 1.78 mL | 3.55 mL |
| 10 mM | 0.18 mL | 0.89 mL | 1.78 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.36 mL |
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产品说明书 for AZ 13824374
参考文献 for AZ 13824374
参考文献是支持产品生物活性的出版物。
Winter-Holt et al (2022) Discovery of a potent and selective ATAD2 bromodomain inhibitor with antiproliferative activity in breast cancer models. J.Med.Chem. 65 3306 PMID: 35133824
If you know of a relevant reference for AZ 13824374, please let us know.
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关键词: AZ 13824374, AZ 13824374 supplier, AZ13824374, potent, selective, inhibitors, inhibits, ATAD2, bromodomain, antiproliferative, AAA, domain-containing, protein, 2, Bromodomains, 7757, Tocris Bioscience
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
Stem Cell Research Product Guide
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Epigenetics Scientific Review
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.
Epigenetics in Cancer Poster
This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.
Rheumatoid Arthritis Poster
Rheumatoid arthritis (RA) is a chronic destructive inflammatory autoimmune disease that results from a breakdown in immune tolerance, for reasons that are as yet unknown. This poster summarizes the pathology of RA and the inflammatory processes involved, as well as describing some of the epigenetic modifications associated with the disease and the potential for targeting these changes in the discovery of new treatments.