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AZD2281 (Olaparib)

Cat. No. M1664
AZD2281 (Olaparib) Structure
Synonym:

Olaparib; KU-0059436

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 35  USD35 In stock
10mg USD 37  USD37 In stock
25mg USD 60  USD60 In stock
50mg USD 90  USD90 In stock
100mg USD 120  USD120 In stock
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Quality Control & Documentation
Biological Activity

AZD 2281 (Olaparib, KU-0059436) is a  novel, potent orally active PARP (poly ADP-ribose polymerase) inhibitorwith IC50 of 5 and 1 nM for PARP-1and PARP-2  respectively. AZD 2281 (Olaparib, KU-0059436) acts as an inhibitor of the enzyme Poly ADP ribose polymerase (PARP) and is one of the first PARP inhibitors.It induces cancer specific synthetic lethality in homologous recombination repair defective cells, including BRCA-deficient tumors. Olaparib is an autophagy and mitophagy activator.

Product Citations
Customer Product Validations & Biological Datas
Source Int J Biol Sci (2018 Oct). Figure 5. Olaparib (Abmole Bioscience, Houston, USA)
Method IP
Cell Lines mice
Concentrations 100 mg/kg
Incubation Time -
Results The overall RTVs (treated vs. non-treated tumors) for mice bearing Brca1-mutant tumor allografts were 60.8% and 62.6% for mice treated with MK-2206 and olaparib, respectively.
Source Int J Biol Sci (2018 Oct). Figure 4. Olaparib (Abmole Bioscience, Houston, USA)
Method IP
Cell Lines mice
Concentrations 100 mg/kg
Incubation Time -
Results In mice co-treated with olaparib and MK-2206, tumor volume was only increased ~1.8-fold at this same time, indicating that these agents exerted a additive effect on tumor growth.
Source Int J Oncol (2015). Figure 4. AZD2281
Method apoptosis assay
Cell Lines HCC‑1428 cells
Concentrations 2 μM
Incubation Time 4 day
Results Inhibition of autophagy by knocking down ATG5 also partially inhibited AZD2281-induced apoptosis, suggesting that autophagy contributes to AZD2281-induced cell death in BRCA mutated breast cancer cells.
Source Int J Oncol (2015). Figure 1. AZD2281
Method Transmission electron microscopy
Cell Lines BRCA1 or BRCA2 mutant breast cancer cell lines
Concentrations 2 μM
Incubation Time 4 day
Results The growth inhibition effect of AZD2281 was significantly higher in the BRCA wild-type cell lines with BRCA1 allelic loss than in the BRCA wild-type cell line without BRCA1 allelic loss.
Protocol (for reference only)
Cell Experiment
Cell lines SW620 colorectal cell line
Preparation method Potentiation of MMS Cytotoxicity by 47 Determined by the Use of Sulforhodamine B Cell Growth Assays. SW620 cells were seeded in 96-well plates and were left to attach overnight. Cells were preincubated with vehicle control (DMSO) or with a single concentration of KU-0059436 (1, 3, 10, 30, 100 or 300 nM) for 1 h before the addition of increasing concentrations of MMS. Cells were incubated in the presence of each drug combination for 4 days before cell growth was quantified by the use of an SRB assay.44 Data were calculated from triplicate wells as the mean percentage of cell growth relative to KU-0059436-only wells, and (SE and IC50 were calculated by the use of XL-FIT 4 software. SW620 cells showed <24% growth inhibition (>76% cell growth) when only KU-0059436 was used at concentrations below 300 nM (data not shown).
Concentrations 1, 3, 10, 100 and 300 nM
Incubation time 4 days
Animal Experiment
Animal models mouse bearing SW620 xenografted tumors
Formulation methylcellulose/PBS
Dosages 10 mg/kg once daily for 5 consecutive days
Administration orally
Chemical Information
Molecular Weight 434.46
Formula C24H23FN4O3
CAS Number 763113-22-0
Solubility (25°C) DMSO 90 mg/mL
DMF 45 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Bajrami et al. EMBO Mol Med. Synthetic lethality of PARP and NAMPT inhibition in triple-negative breast cancer cells.

[2] Itamochi et al. Int J Clin Oncol. Clinical trials and future potential of targeted therapy for ovarian cancer.

[3] Ibrahim et al. Cancer Discov. PI3K inhibition impairs BRCA1/2 expression and sensitizes BRCA proficient triple negative breast cancer to PARP inhibition.

[4] Daemen et al. Breast Cancer Res Treat. Cross-platform pathway-based analysis identifies markers of response to the PARP inhibitor olaparib.

[5] Marchetti et al. Expert Opin Investig Drugs. Olaparib , PARP1 inhibitor in ovarian cancer.

[6] Keith A Menear, et al. J Med Chem . 4-[3-(4-cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: a novel bioavailable inhibitor of poly(ADP-ribose) polymerase-1

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Keywords: AZD2281 (Olaparib), Olaparib; KU-0059436 supplier, PARP, inhibitors, activators


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