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Submit ReviewAZ 13824374
Description: Potent and selective ATAD2 bromodomain inhibitor
Chemical Name: (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
Purity: ≥98% (HPLC)
Biological Activity 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.
Licensing Information
Sold with the permission of AstraZeneca UK Ltd.
Technical Data for AZ 13824374
| M. Wt | 562.69 |
| Formula | C30H39FN8O2 |
| Storage | Store at -20°C |
| Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for AZ 13824374
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 56.27 | 100 | |
| ethanol | 56.27 | 100 |
Preparing Stock Solutions for AZ 13824374
The following data is based on the product molecular weight 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.
| Concentration / Solvent Volume / Mass | 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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Product Datasheets for AZ 13824374
References for AZ 13824374
References are publications that support the biological activity of the product.
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
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Keywords: AZ 13824374, AZ 13824374 supplier, AZ13824374, potent, selective, inhibitors, inhibits, ATAD2, bromodomain, antiproliferative, AAA, domain-containing, protein, 2, Bromodomains, 7757, Tocris Bioscience
Citations for AZ 13824374
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Literature in this Area
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