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Description: Potent PARP inhibitor
Chemical Name: 8-Hydroxy-2-methyl-4(3H)-quinazolinone
Purity: ≥99% (HPLC)
Biological Activity
Novel, potent inhibitor of poly(ADP-ribose) polymerase (PARP). Ki and IC50 values are 48 and 400 nM respectively.
Technical Data
| M. Wt | 176.17 |
| Formula | C9H8N2O2 |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 90417-38-2 |
| PubChem ID | 63306 |
| InChI Key | YJDAOHJWLUNFLX-UHFFFAOYSA-N |
| Smiles | CC1=NC2=C(O)C=CC=C2C(=O)N1 |
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
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 1eq. NaOH | 17.62 | 100 | |
| DMSO | 17.62 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 176.17. 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 | 5.68 mL | 28.38 mL | 56.76 mL |
| 5 mM | 1.14 mL | 5.68 mL | 11.35 mL |
| 10 mM | 0.57 mL | 2.84 mL | 5.68 mL |
| 50 mM | 0.11 mL | 0.57 mL | 1.14 mL |
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Product Datasheets
References
References are publications that support the biological activity of the product.
Bowman et al (1998) Potentiation of anti-cancer agent cytotoxicity by the potent poly(ADP-ribose) polymerase inhibitors NU1025 and NU1064. Br.J.Cancer. 78 1269 PMID: 9823965
Delaney et al (2000) Potentiation of temozol. and topo. growth inhibition and cytotoxicity by novel poly(adenosine diphosphoribose) polymerase inhibitors in a panel of human tumor cell lines. Clin.Cancer.Res. 6 2860 PMID: 10914735
Griffin et al (1998) Resistance-modifying agents. 5. Synthesis and biological properties of quinazolinone inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase (PARP). J.Med.Chem. 41 5247 PMID: 9857092
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Keywords: NU 1025, NU 1025 supplier, Potent, PARP, inhibitors, inhibits, PolyADP-ribose, Polymerases, NU1025, Poly(ADP-ribose), Polymerase, 1401, Tocris Bioscience
1 Citation for NU 1025
Citations are publications that use Tocris products. Selected citations for NU 1025 include:
Sultana et al (2012) Synthetic lethal targeting of DNA double-strand break repair deficient cells by human apurinic/apyrimidinic endonuclease inhibitors. Int J Cancer 131 2433 PMID: 22377908
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Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.