AZD 2461

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. It was developed to overcome the resistance encountered with olaparib (Cay-10621) that is presumed to be mediated in part by P-glycoprotein-mediated drug efflux. 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. Furthermore, it can induce a loss of p53 binding protein 1 expression in mice with KB1P tumors at 100 mg/kg.Formal Name: 4-[[4-fluoro-3-[(4-methoxy-1-piperidinyl)carbonyl]phenyl]methyl]-1(2H)-phthalazinone. CAS Number: 1174043-16-3. Molecular Formula: C22H22FN3O3. Formula Weight: 395.4. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 3 mg/mL, DMSO: 2 mg/mL, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/mL, Ethanol: 0.5 mg/mL. lambdamax: 277 nm. SMILES: O=C1C2=CC=CC=C2C(CC3=CC(C(N4CCC(OC)CC4)=O)=C(F)C=C3)=NN1. InChi Code: InChI=1S/C22H22FN3O3/c1-29-15-8-10-26(11-9-15)22(28)18-12-14(6-7-19(18)23)13-20-16-4-2-3-5-17(16)21(27)25-24-20/h2-7,12,15H,8-11,13H2,1H3,(H,25,27). InChi Key: HYNBNUYQTQIHJK-UHFFFAOYSA-N.