AZ 13824374

Name: AZ 13824374
Brand: Tocris Bioscience
SKU: 7757

Tocris Bioscience, part of Bio-Techne | Catalog # 7757

COA / SDS

Potent and selective ATAD2 bromodomain inhibitor

Key Product Details

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)
Molecular Weight:	562.69

View Full Technical Details for AZ 13824374

Technical Data
Citations

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)
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 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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References for AZ 13824374

References are publications that support the biological activity of the product.

Winter-Holt Discovery of a potent and selective ATAD2 bromodomain inhibitor with antiproliferative activity in breast cancer models. J.Med.Chem. 2022 PMID: 35133824