Olaparib | PARP1 inhibitor

CAS:
763113-22-0
Catalog Number:
10-2154
Activity:
PARP1 inhibitor
Chemical Name:
4-(3-(4-(Cyclopropanecarbonyl)piperazine-1-carbonyl)-4-fluorobenzyl)phthalazine-1(2H)-one
Alternate Names:
AZD-2281; KU-59436
Molecular Weight:
434.47
Molecular Formula:
C24H23FN4O3
Solubility:
Soluble in DMSO (up to 33 mg/ml) or in Ethanol (up to 1.7 mg/ml)
Physical Properties:
Off-white solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.
Shipping Code:
RT

Available Options

Size :PriceQuantity 
5 mg$45.00
25 mg$130.00

Olaparib (763113-22-0) is a highly potent and selective PARP-inhibitor with IC50 values of 5 nM and 1 nM for PARP-1 and PARP-2, respectively.1  In a genetically engineered mouse model for BRCA1-associated breast cancer olaparib inhibited tumor growth and improved survival with no signs of toxicity.2 Synergizes with many other anticancer agents.3 Olaparib shows efficacy in colorectal cancers.4 Prevents house dust mite allergen-induced asthma in a mouse model.5

References/Citations:

1) Menear et al. (2008), 4-[3-(4-Cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: a novel bioavailable inhibitor of poly(ADP-ribose)polymerase-1;  J. Med. Chem., 51 6581
2) Rottenberg et al. (2008), High sensitivity of BRCA1-deficient mammary tumors to the PARP inhibitor AZD2281 alone and in combination with platinum drugs; Proc. Natl. Acad. Sci. USA, 105 17079
3) Avila-Arroyo et al. (2015), Synergistic effect of Trabectedin and Olaparib combination regimen in breast cancer cell lines; J. Breast Cancer, 18 329
4) Xu et al. (2015), Combined olaparib and oxaliplatin inhibits tumor proliferation and induces G2/M arrest and γ-H2AX foci formation in colorectal cancer; Onco. Targets Ther., 8 3047
5) Ghonim et al. (2015), PARP is activated in human asthma and its inhibition by olaparib blocks house dust mite-induced disease in mice; Clin. Sci.(Lond), 129 951

CAS:
763113-22-0
Catalog Number:
10-2154
Activity:
PARP1 inhibitor
Chemical Name:
4-(3-(4-(Cyclopropanecarbonyl)piperazine-1-carbonyl)-4-fluorobenzyl)phthalazine-1(2H)-one
Alternate Names:
AZD-2281; KU-59436
Molecular Weight:
434.47
Molecular Formula:
C24H23FN4O3
Solubility:
Soluble in DMSO (up to 33 mg/ml) or in Ethanol (up to 1.7 mg/ml)
Physical Properties:
Off-white solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

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