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Olaparib (AZD2281)
(SynonymsKU-0059436
)Add to Favor
M.Wt: 434.46
Formula: C24H23FN4O3
Solubility: DMSO
Purity: >99%
Storage: at -20℃ 2 years
CAS No.: 763113-22-0
Price and Availability of Olaparib (AZD2281):
Applications & Customer's Feedback of Olaparib (AZD2281):
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Olaparib was supplied by Selleck. Data were provided by Dr David Schürmann from University of Basel.
Primary human lung fibroblast cells (MRC-5) were pre-treated with the indicated concentration of the PARP inhibitor AZD2281 for two hours. Oxidative DNA damage was induced by 500 µM H2O2 for 10 min and cellular PARP activity was measured by immuno-staining of poly(ADP)-ribose (PAR) (right panels). The in vivo effect of PARP inhibition was compared to cells without DNA damage induction and inhibitor (control) and H2O2-treated cells without inhibitor. Average nuclear PAR staining intensities of more than 50 cells were statistically analysed by Kruskal-Wallis and the post-hoc Dunn’s Multiple Comparison tests (left panel). Asterisks indicate highly significant (p<1%) differences to H2O2-treated cells without PARP inhibitor. Thick horizontal bars mark medians and error bars the interquartile range.
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Olaparib was supplied by Selleck. Data were provided by Dr Xiangbing Meng of University of Iowa.
Effect of AZD 2281 on the viability of endometrial cancer cell line Hec50 and Ishikawa and ovarian cancer cell line SKOV3,Caov3 and PA-1 was detected by WST-1 method after 3 days treatment.
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AZD2281 was purchased from Selleck. Data from JBC 286;12157–12165.
MSH3-deficient cells are sensitive to olaparib, aPARPinhibitor, and the combination with oxaliplatin. A, clonogenic survival of HCT11635, G5 without doxycycline (DOX), and G5 cells with doxycycline, which were treated with 2M of oxaliplatin, 2M of olaparib, and the combination of these two drugs. B, clonogenic survival of HT29 cells, which were treated with 1 M oxaliplatin, 2 M olaparib, and the combination of these two drugs.
MSH3 Mediates Sensitization of Colorectal Cancer Cells to Cisplatin, Oxaliplatin, and a Poly(ADP-ribose) Polymerase Inhibitor. ------ Masanobu Takahashi,Minoru Koi et al. JBC 2011 April;286:12157-12165
Double-Strand Break Repair-Independent Role for BRCA2 in Blocking Stalled Replication Fork Degradation by MRE11. ------ Katharina Schlacher,Nicole Christ et al Cell 2011.May;145:529-42
The USP1/UAF1 Complex Promotes Double-Strand Break Repair through Homologous Recombination. ------ Junko Murai, Kailin Yang et al Mol Cell Biol 2011.June;31:2462-9
Nanoparticle-mediated measurement of target-drug binding in cancer cells. ------ Ullal AV, Reiner T et al. ACS Nano. 2011 Nov;5:9216-24.
Rad51 and BRCA2 - New Molecular Targets for Sensitizing Glioma Cells to Alkylating Anticancer Drugs. ------ Steve Quiros, Wynand Paul Roos,et al Plos One 2011;6:e27183
"we tried the product in one of our studies and it performed well. " ------ Stefano Ferrari, IMCR - University of Zurich
Biological Activity of Olaparib (AZD2281):
Olaparib (AZD2281) is a potent PARP inhibitor with IC50 of 5 and 1 nM for PARP-1and PARP-2, respectively. Poly(adenosine diphosphate-ribose) polymerase (PARP) is anenzyme that is involved in a specific kind of DNA repair called base-excision repair. The PARP inhibition can be directly cytotoxic to tumour cells and augments the anti-tumour effects of DNA-damaging agents. Olaparib (AZD2281) at 400 mg twice daily is well tolerated and highly active. The toxicity that was seen in BRCA1/BRCA2 carriers was similar to the previously reported toxicity in noncarriers. Animals bearing SW620 xenografted tumors were treated with Olaparib (AZD2281) (10 mg/kg, po) in combination with TMZ (50 mg/kg, po) once daily for 5 consecutive days, after which the tumors were left to grow out. A considerable inhibition of tumor volumes as compared with that of the TMZ alone group was observed for the TMZ plus Olaparib (AZD2281) combination (mean values given as relative tumor volumes (RTV). [1][2][3]
References on Olaparib (AZD2281):
[1] Khan OA et al. Br J Cancer. 2011 Mar 1;104(5):750-5.
[2] Samol J et al. Invest New Drugs. 2011 May 18.
[3] Menear KA et al. J Med Chem. 2008 Oct 23;51(20):6581-91.
MSDS
Batch S106001: H-NMR COA
Batch S106006: H-NMR HPLC COA
Batch S106007: H-NMR HPLC COA
Batch S106009: H-NMR COA
Batch S106010: H-NMR H-NMR(CDCl3) HPLC COA
PARPWe give free samples and rewards to people who would like to provide us useful scientific data(western blot, etc.) See Details
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