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.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 395.43. Batch specific molecular weights may vary from batch to batch due to solvent 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 are publications that support the products' biological activity.
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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