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Olaparib (AZD2281)

Olaparib (AZD2281)

Item no.	S1060-10
Manufacturer	Selleckchem
CASRN	763113-22-0
Amount	10 mg
Quantity options	10 mg 100 mg 1 g 10 g 10 mM/1 mL 25 mg 500 mg 5 g
Category	Oncology Inhibitors & Compound Libraries Small Molecules By Organ Lung Cancer Bladder Cancer Colorectal Cancer Breast Cancer Testicular & Prostate Cancer Uterine, Ovarian & Cervical Cancer
Type	Inhibitors
Specific against	other
Smiles	C1CC1C(=O)N2CCN(CC2)C(=O)C3=C(C=CC(=C3)CC4=NNC(=O)C5=CC=CC=C54)F
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	Ku-0059436
Similar products	Olaparib
Available
Manufacturer - Targets	PARP2, PARP1
Storage Conditions	2 years -80 in solvent
Molecular Weight	434, 46
Administration	Administered via i.p. injection at 10 uL/g of body weight
Animal Models	Brca1-/-, p53-/- mammary tumors are generated in K14cre, Brca1F/F, p53F/F mice.
Cell lines	Breast cancer cell lines including SW620 colon, A2780 ovarian, HCC1937, Hs578T, MDA-MB-231, MDA-MB-436, and T47D
Clinical Trials	Combining with cediranib, Olaparib is currently in Phase I/II study for treatment of recurrent papillary-serous ovarian, fallopian tube or peritoneal cancer or treatment of recurrent triple-negative breast cancer.
Concentrations	1-300 nM
Dosages	50 mg/kg
Formulation	50 mg/mL stocks in DMSO with 10% 2-hydroxyl-propyl-beta-cyclodextrine/PBS
IC50	5 nM, 5 nM, 5 nM, 5 nM, 5 nM, 5 nM
In vitro	Olaparib would act against BRCA1 or BRCA2 mutations. Olaparib is not sensitive to tankyrase-1 (IC50 >1 uM). Olaparib could ablate the PARP-1 activity at concentrations of 30-100 nM in SW620 cells. Olaparib is hypersensitive to BRCA1-deficient cell lines (MDA-MB-463 and HCC1937), compared with BRCA1- and BRCA2-proficient cell lines (Hs578T, MDA-MB-231, and T47D). [1] Olaparib is strongly sensitive to KB2P cells due to suppression of base excision repair by PARP inhibition, which may result in the conversion of single-strand breaks to double-strand breaks during DNA replication, thus activating BRCA2-dependent recombination pathways. [2]
In vivo	Combining with temozolomide, Olaparib (10 mg/kg, p.o.) significantly suppresses tumor growth in SW620 xenografts. [1] Olaparib shows great response to Brca1-/-, p53-/- mammary tumors (50 mg/kg i.p. per day), while no responses to HR-deficient Ecad-/-, p53-/- mammary tumors. Olaparib even does not show dose-limiting toxicity in tumor-bearing mice. [3] Olaparib has been used to treat with BRCA mutated tumors, such as ovarian, breast and prostate cancers. Moreover, Olaparib shows selectively inhibition to ATM (Ataxia Telangiectasia Mutated)-deficient tumor cells, which indicates to be a potential agent for treating ATM mutant lymphoid tumors. [4]
Incubation Time	7-14 days
Kinase Assay	FlashPlate assay (96-well screening assay), To columns 1 through 10, 1 uL of Olaparib (in DMSO) is added, and 1 uL DMSO only is added to the positive (POS) and negative (NEG) control wells (columns 11 and 12, respectively) of a pretreated FlashPlate. PARP-1 is diluted 1:40 in buffer (buffer B: 10% glycerol (v/v), 25 mM HEPES, 12.5 mM MgCl2, 50 mM KCl, 1 mM DTT, 0.01% NP-40 (v/v), pH 7.6) and 40 uL added to all 96 wells (final PARP-1 concentration in the assay is ca.1 ng/uL). The plate is sealed and shaken at RT for 15 min. Following this, 10 uL of positive reaction mix (0.2 ng/uL of double-stranded oligonucleotide [M3/M4] DNA per well, 5 uM of NAD+ final assay concentration, and 0.075 uCi 3H-NAD+ per well) is added to the appropriate wells (columns 1-11). The negative reaction mix, lacking the DNA oligonucleotide, is added to column 12 (with the mean negative control value used as the background). The plate is resealed and shaken for a further 60 min at RT to allow the reaction to continue. Then, 50 uL of ice-cold acetic acid (30%) is added to each well to stop the reaction, and the plate is sealed and shaken for a further 60 min at RT. Tritiated signal bound to the FlashPlate is then determined in counts per minute (CPM) using the TopCount plate reader.
Method	The cytotoxicity of Olaparib is measured by clonogenic assay. Olaparib is dissolved in DMSO and diluted by culture media before use. The cells are seeded in six well plates and left to attach overnight. Then Olaparib is added at various concentrations and the cells are incubated for 7-14 days. After that the surviving colonies are counted for calculating the IC50.
Solubility (25C)	DMSO 87 mg/mL, Water <1 mg/mL, Ethanol <1 mg/mL
Information	Olaparib (AZD2281, KU0059436) is a selective inhibitor of PARP1/2 with IC50 of 5 nM/1 nM in cell-free assays, 300-times less effective against tankyrase-1. Olaparib induces significant autophagy that is associated with mitophagy in cells with BRCA mutations.
Chemical Name	4-(3-(1-(cyclopropanecarbonyl)piperazine-4-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one
Features	Olaparib is one of the first PARP inhibitors.

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