Olaparib, PARP1 inhibitor (TBI2154)

Description

Product Details

Formal Name: 4-(3-(4-(Cyclopropanecarbonyl)piperazine-1-carbonyl)-4-fluorobenzyl)phthalazine-1(2H)-one

Alternate Names: AZD-2281; KU-59436

Molecular Formula: C₂₄H₂₃FN₄O₃

Formula Weight: 434.47

CAS Number: 763113-22-0

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to 33 mg/ml) or in Ethanol (up to 1.7 mg/ml)

Storage: -20°C

Stability: ≥ 2 years.

Applications

PARP1 inhibitor

Functions

A highly potent and selective PARP-inhibitor with IC₅₀ values of 5 nM and 1 nM for PARP-1 and PARP-2, respectively. In a genetically engineered mouse model for BRCA1-associated breast cancer olaparib inhibited tumor growth and improved survival with no signs of toxicity. Synergizes with many other anticancer agents. Shows efficacy in colorectal cancers. Prevents house dust mite allergen-induced asthma in a mouse model.

Application Procedures

First dissolved in DMSO (up to 33 mg/ml) or in Ethanol (up to 1.7 mg/ml), then diluted to aqueous buffer. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.