AZD 2461

Key Product Details

Product Description

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.

Product Specifications for AZD 2461

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 3 publications citing the usage of this product.

• Jaspers Loss of 53BP1 causes PARP inhibitor resistance in Brca1-mutated mouse mammary tumors. Cancer Discov. 2013 PMID: 23103855
• Oplustil O'Connor 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. 2016 PMID: 27550455

Product Documents for AZD 2461