Chemical Name: 4-[[4-Fluoro-3-[(4-methoxy-1-piperidinyl)carbonyl]phenyl]methyl]-1(2H)-phthalazinone
Biological ActivityAZD 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.
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.
Complete Your Research
The PARP inhibitor AZD2461 provides insights into the role of PARP3 inhibition for both synthetic lethality and tolerability with chemotherapy in preclinical models.
Oplustil O'Connor et al.
Cancer Res., 2016;76:6084
Loss of 53BP1 causes PARP inhibitor resistance in Brca1-mutated mouse mammary tumors.
Jaspers et al.
Cancer Discov., 2013;3:68
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