Shelf life (days): 1460.0
Formulation: A crystalline solid
Formal Name: 4-[[4-fluoro-3-[(4-methoxy-1-piperidinyl)carbonyl]phenyl]methyl]-1(2H)-phthalazinone
Purity: ≥95%
Formula Markup: C22H22FN3O3
Formula Weight: 395.4
CAS Number: 1174043-16-3
Notes: The poly(ADP-ribose) polymerases (PARPs) form a family of enzymes with roles in DNA repair and apoptosis, particularly in response to reactive oxygen and nitrogen species. AZD 2461 is a PARP inhibitor (IC50 = 5 nM) with low affinity for the P-glycoprotein drug efflux transporter.{31078} It was developed to overcome the resistance encountered with olaparib (Item No. 10621) that is presumed to be mediated in part by P-glycoprotein-mediated drug efflux.{31078} When tested on the olaparib-resistant KB1P tumor T6-28, which has an 80-fold increased Mdr1b expression, AZD 2461 did not affect P-glycoprotein.{31078} Furthermore, it can induce a loss of p53 binding protein 1 expression in mice with KB1P tumors at 100 mg/kg.{31078}
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