A PARP inhibitor (IC50 = 5 nM) with low affinity for the P-glycoprotein drug efflux transporter; induces a loss of p53 binding protein 1 expression in mice with KB1P tumors at 100 mg/kg

AZD 2461 – 1 mg

Brand:
Cayman
CAS:
1174043-16-3
Storage:
-20
UN-No:
Non-Hazardous - /

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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Description

A PARP inhibitor (IC50 = 5 nM) with low affinity for the P-glycoprotein drug efflux transporter; induces 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

Synonyms: 

Molecular weight: 395.4

CAS: 1174043-16-3

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|DNA Repair Enzymes||Research Area|Cancer|DNA Damage and Repair|PARP||Research Area|Cancer|Multidrug Resistance

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