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Submit ReviewAZD 2461
Description: Potent PARP inhibitor; orally bioavailable
Chemical Name: 4-[[4-Fluoro-3-[(4-methoxy-1-piperidinyl)carbonyl]phenyl]methyl]-1(2H)-phthalazinone
Purity: ≥98% (HPLC)
Biological Activity for AZD 2461
AZD 2461 is a potent PARP inhibitor (IC50 values are 2, 5 and 200 nM for PARP2, PARP1 and PARP3, respectively). Exhibits anticancer effects in BRCA1 mutant, but not wild-type breast cancer cell lines in vitro. Inhibits growth of olaparib-resistant mammary tumors in a mouse model and is a poor substrate for the P-gp transporter. Orally bioavailable.
Compound Libraries for AZD 2461
AZD 2461 is also offered as part of the Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.
Technical Data for AZD 2461
| M. Wt | 395.43 |
| Formula | C22H22FN3O3 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1174043-16-3 |
| PubChem ID | 44199317 |
| InChI Key | HYNBNUYQTQIHJK-UHFFFAOYSA-N |
| Smiles | COC1CCN(C(C2=C(C=CC(CC3=NNC(C4=CC=CC=C34)=O)=C2)F)=O)CC1 |
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 AZD 2461
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 39.54 | 100 | |
| ethanol | 39.54 | 100 |
Preparing Stock Solutions for AZD 2461
The following data is based on the product molecular weight 395.43. 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 | 2.53 mL | 12.64 mL | 25.29 mL |
| 5 mM | 0.51 mL | 2.53 mL | 5.06 mL |
| 10 mM | 0.25 mL | 1.26 mL | 2.53 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.51 mL |
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Product Datasheets for AZD 2461
References for AZD 2461
References are publications that support the biological activity of the product.
Oplustil O'Connor et al (2016) The PARP inhibitor AZD2461 provides insights into the role of PARP3 inhibition for both synthetic lethality and tolerability with chemotherapy in preclinical models. Cancer Res. 76 6084 PMID: 27550455
Jaspers et al (2013) Loss of 53BP1 causes PARP inhibitor resistance in Brca1-mutated mouse mammary tumors. Cancer Discov. 3 68 PMID: 23103855
If you know of a relevant reference for AZD 2461, please let us know.
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Keywords: AZD 2461, AZD 2461 supplier, AZD2461, potent, PARP, inhibitors, inhibits, poly, (ADP-ribose), polymerases, orally, bioavailable, chemotherapeutics, Poly(ADP-ribose), Polymerase, 6060, Tocris Bioscience
Citations for AZD 2461
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