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Submit ReviewTH 5427 hydrochloride
Description: Potent NUDT5 inhibitor
Chemical Name: 7-[[5-(3,4-Dichlorophenyl)-1,3,4-oxadiazol-2-yl]methyl]-1,3-dimethyl-8-(piperazine-1-yl)-1H-purine-2,6-dione hydrochloride
Purity: ≥98% (HPLC)
Biological Activity for TH 5427 hydrochloride
TH 5427 hydrochloride is a potent nudix hydrolase 5 (NUDT5) inhibitor (IC50 = 29 nM). Displays >650-fold selectivity for NUDT5 over MTH1. Inhibits ATP synthesis, chromatin remodeling, gene expression and proliferation in progestin-treated breast cancer cells in vitro.
Licensing Information
Sold under license from Thomas Helleday's Foundation for Medical Research and Oxcia AB.
Compound Libraries for TH 5427 hydrochloride
TH 5427 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for TH 5427 hydrochloride
| M. Wt | 527.79 |
| Formula | C20H20Cl2N8O3.HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 2253744-57-7 |
| PubChem ID | 137919865 |
| Smiles | O=C1N(C)C(C(N(CC2=NN=C(C3=CC(Cl)=C(Cl)C=C3)O2)C(N4CCNCC4)=N5)=C5N1C)=O.Cl |
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 TH 5427 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 5.28 | 10 | |
| DMSO | 10.56 | 20 |
Preparing Stock Solutions for TH 5427 hydrochloride
The following data is based on the product molecular weight 527.79. 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 |
|---|---|---|---|
| 0.2 mM | 9.47 mL | 47.37 mL | 94.73 mL |
| 1 mM | 1.89 mL | 9.47 mL | 18.95 mL |
| 2 mM | 0.95 mL | 4.74 mL | 9.47 mL |
| 10 mM | 0.19 mL | 0.95 mL | 1.89 mL |
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Product Datasheets for TH 5427 hydrochloride
References for TH 5427 hydrochloride
References are publications that support the biological activity of the product.
Page et al (2018) Targeted NUDT5 inhibitors block hormone signaling in breast cancer cells. Nat.Commun. 9 250 PMID: 29343827
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