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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
Technical Data for AZD 2461
|Storage||Store at -20°C|
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|
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|
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
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Citations for AZD 2461
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Literature in this Area
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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.