1. Cell Cycle/DNA Damage
    Epigenetics
    Autophagy
  2. PARP
    Autophagy

Olaparib (Synonyms: AZD2281; KU0059436)

Cat. No.: HY-10162 Purity: 99.71%
Data Sheet SDS Handling Instructions

Olaparib is a potent PARP inhibitor with IC50 of 5 and 1 nM for PARP-1 and PARP-2, respectively.

For research use only. We do not sell to patients.
Olaparib Chemical Structure

Olaparib Chemical Structure

CAS No. : 763113-22-0

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Customer Review

    Olaparib purchased from MCE. Usage Cited in: Cancer Chemother Pharmacol. 2017 Jul 29.

    PARP1 inhibition is lethal to MPM cells. Colony formation assays of clonal cell survival with continuous Niraparib or Olaparib, both at 3 uM. a H2452 BPA1-mutant MPM cells exposed to Niraparib. b HMeso01A BAP1-mutant MPM cells exposed to Niraparib. cHMeso01A BAP1-mutant MPM cells exposed to Olaparib. d CRL-2081 BAP1 wild-type MPM cells exposed to Olaparib. e CRL-2081 BAP1 wild-type MPM cells exposed to Niraparib. f Dose response of H2452 BPA1-mutant MPM cells exposed to varying concentrations of
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Olaparib is a potent PARP inhibitor with IC50 of 5 and 1 nM for PARP-1 and PARP-2, respectively.

    IC50 & Target

    IC50: 5/1 nM (PARP-1/2)[1]

    In Vitro

    Olaparib (AZD2281) is a single digit nanomolar inhibitor of both PARP-1 and PARP-2 that shows standalone activity against BRCA1-deficient breast cancer cell lines. Olaparib is applied to SW620 cell lysates, and identified the IC50 for PARP-1 inhibition to be around 6 nM and the total ablation of PARP-1 activity to be at concentrations of 30−100 nM[1].

    In Vivo

    Animals bearing SW620 xenografted tumors are treated with Olaparib (10 mg/kg, p.o.) in combination with Temozolomide (TMZ) (50 mg/kg, p.o.) once daily for 5 consecutive days, after which the tumors are left to grow out[1]. Olaparib increases vascular perfusion in Calu-6 tumors established in a DWC model. Administration of olaparib(50 mg/kg, p.o.) as a single agent (top panel) or in combination with radiation (bottom panel) results in an increase in fluorescence intensity in the Calu-6 tumors[2].

    Clinical Trial
    NCT Number Sponsor Condition Start Date Phase
    NCT00678132 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Neoplasms April 24, 2008 Phase 1
    NCT00782574 AstraZeneca Advanced Solid Tumors November 12, 2008 Phase 1
    NCT00572364 AstraZeneca Advanced Solid Malignancies November 2007 Phase 1
    NCT00710268 AstraZeneca Neoplasm Metastasis June 2008 Phase 1
    NCT00679783 AstraZeneca|British Columbia Cancer Agency Ovarian Carcinoma|Breast Cancer July 2008 Phase 2
    NCT00707707 AstraZeneca Breast Cancer|Triple Negative Breast Cancer|Metastatic Breast Cancer September 15, 2008 Phase 1
    NCT00753545 AstraZeneca Ovarian Cancer August 2008 Phase 2
    NCT00819221 AstraZeneca Solid Tumors January 5, 2009 Phase 1
    NCT00633269 AstraZeneca|KuDOS Pharmaceuticals Limited Neoplasm Metastasis April 2008 Phase 1
    NCT00777582 AstraZeneca Solid Tumors October 27, 2008 Phase 1
    NCT00516373 AstraZeneca Ovarian Neoplasms|BRCA1 Protein|BRCA2 Protein July 4, 2005 Phase 1
    NCT00494234 AstraZeneca|KuDOS Pharmaceuticals Limited Breast Neoplasms June 15, 2007 Phase 2
    NCT00628251 AstraZeneca Ovarian Neoplasms July 30, 2008 Phase 2
    NCT00494442 AstraZeneca|KuDOS Pharmaceuticals Limited Ovarian Neoplasm June 11, 2007 Phase 2
    NCT02576444 Joseph Paul Eder|Dana-Farber Cancer Institute|Vanderbilt-Ingram Cancer Center|Yale University Cancer November 2015 Phase 2
    NCT00516802 AstraZeneca|KuDOS Pharmaceuticals Limited Melanoma Neoplasms January 2007 Phase 1
    NCT00516438 AstraZeneca|KuDOS Pharmaceuticals Limited Malignant Solid Tumors July 2007 Phase 1
    NCT00515866 AstraZeneca Pancreatic Neoplasms August 2007 Phase 1
    NCT00516724 AstraZeneca Triple Negative Metastatic Breast Cancer|Advanced Ovarian Cancer|Carboplatin|Paclitaxel June 29, 2007 Phase 1
    NCT00678132 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Neoplasms April 24, 2008 Phase 1
    NCT00782574 AstraZeneca Advanced Solid Tumors November 12, 2008 Phase 1
    NCT00572364 AstraZeneca Advanced Solid Malignancies November 2007 Phase 1
    NCT00710268 AstraZeneca Neoplasm Metastasis June 2008 Phase 1
    NCT00679783 AstraZeneca|British Columbia Cancer Agency Ovarian Carcinoma|Breast Cancer July 2008 Phase 2
    NCT00707707 AstraZeneca Breast Cancer|Triple Negative Breast Cancer|Metastatic Breast Cancer September 15, 2008 Phase 1
    NCT00753545 AstraZeneca Ovarian Cancer August 2008 Phase 2
    NCT00819221 AstraZeneca Solid Tumors January 5, 2009 Phase 1
    NCT00633269 AstraZeneca|KuDOS Pharmaceuticals Limited Neoplasm Metastasis April 2008 Phase 1
    NCT00777582 AstraZeneca Solid Tumors October 27, 2008 Phase 1
    NCT00516373 AstraZeneca Ovarian Neoplasms|BRCA1 Protein|BRCA2 Protein July 4, 2005 Phase 1
    NCT00494234 AstraZeneca|KuDOS Pharmaceuticals Limited Breast Neoplasms June 15, 2007 Phase 2
    NCT00628251 AstraZeneca Ovarian Neoplasms July 30, 2008 Phase 2
    NCT00494442 AstraZeneca|KuDOS Pharmaceuticals Limited Ovarian Neoplasm June 11, 2007 Phase 2
    NCT02576444 Joseph Paul Eder|Dana-Farber Cancer Institute|Vanderbilt-Ingram Cancer Center|Yale University Cancer November 2015 Phase 2
    NCT00516802 AstraZeneca|KuDOS Pharmaceuticals Limited Melanoma Neoplasms January 2007 Phase 1
    NCT00516438 AstraZeneca|KuDOS Pharmaceuticals Limited Malignant Solid Tumors July 2007 Phase 1
    NCT00515866 AstraZeneca Pancreatic Neoplasms August 2007 Phase 1
    NCT00516724 AstraZeneca Triple Negative Metastatic Breast Cancer|Advanced Ovarian Cancer|Carboplatin|Paclitaxel June 29, 2007 Phase 1
    NCT01562210 The Netherlands Cancer Institute|AstraZeneca NSCLC April 2012 Phase 1
    NCT02677038 M.D. Anderson Cancer Center|AstraZeneca Pancreatic Cancer November 2016 Phase 2
    NCT01682772 Institute of Cancer Research, United Kingdom|Royal Marsden NHS Foundation Trust Adenocarcinoma of the Prostate July 2012 Phase 2
    NCT02533765 Istituto Scientifico Romagnolo per lo Studio e la cura dei Tumori Neoplasms, Germ Cell and Embryonal May 2015 Phase 2
    NCT02338622 Royal Marsden NHS Foundation Trust|Institute of Cancer Research, United Kingdom|AstraZeneca Advanced Cancer March 2014 Phase 1
    NCT03047135 Sidney Kimmel Comprehensive Cancer Center Prostate March 1, 2017 Phase 2
    NCT01813474 AstraZeneca Cancer|Advanced Solid Malignancies March 2013 Phase 1
    NCT02227082 The Netherlands Cancer Institute Locally Advanced Malignant Neoplasm|Inflammatory Breast Carcinoma|Triple-Negative Invasive Breast Carcinoma October 2013 Phase 1
    NCT02229656 The Netherlands Cancer Institute|AstraZeneca Laryngeal Cancer Stage II|Laryngeal Cancer Stage III|Carcinoma, Squamous Cell|Head and Neck Neoplasms February 2014 Phase 1
    NCT01583543 Massachusetts General Hospital Ewing's Sarcoma May 2012 Phase 2
    NCT01623349 Dana-Farber Cancer Institute|Novartis|AstraZeneca Ovarian Cancer|Breast Cancer September 2012 Phase 1
    NCT02032823 AstraZeneca|Breast International Group|Frontier Science & Technology Research Foundation, Inc.|NRG Oncology|Myriad Genetic Laboratories, Inc.|Br.E.A.S.T. -Data Center & Operational Office Institut Jules Bordet Breast Cancer April 22, 2014 Phase 3
    NCT03109080 Institut Curie|AstraZeneca Breast Neoplasms, Triple-Negative|Breast Neoplasm Malignant Female|Radiotherapy Side Effect June 8, 2017 Phase 1
    NCT02476968 AstraZeneca BRCA or HRR+ Mutated Ovarian Cancer Patients September 28, 2015 Phase 4
    NCT03205761 Spanish Breast Cancer Research Group|AstraZeneca Advanced Breast Cancer July 2017 Phase 2
    NCT02681562 Istituti Ospitalieri di Cremona Breast Cancer|Triple Negative Breast Cancer January 2016 Phase 2
    NCT02787642 Institut Bergonié|National Cancer Institute, France Soft-tissue Sarcoma June 2016 Phase 1
    NCT02398058 Italian Sarcoma Group|PharmaMar|AstraZeneca|Istituto Di Ricerche Farmacologiche Mario Negri Soft Tissue Sarcoma|Bone Tumor October 2014 Phase 1
    NCT01758731 University of Colorado, Denver Squamous Cell Carcinoma of the Head and Neck October 22, 2012 Phase 1
    NCT02855697 Anna Thomason|The Christie NHS Foundation Trust Ovarian Cancer November 2016 Early Phase 1
    NCT03106987 AstraZeneca|European Network of Gynaecological Oncology Trial Groups (ENGOT) Epithelial Ovarian Cancer June 8, 2017 Phase 3
    NCT01929603 AstraZeneca Solid Tumours December 2013 Phase 1
    NCT02446704 Massachusetts General Hospital|AstraZeneca Small Cell Lung Cancer September 2015 Phase 1|Phase 2
    NCT03162627 M.D. Anderson Cancer Center|AstraZeneca Malignant Neoplasm of Breast|Malignant Neoplasms of Digestive Organs|Malignant Neoplasms of Female Genital Organs|Malignant Neoplasms of Male Genital Organs|Malignant Neoplasms of Thyroid and Other Endocrine Glands July 2017 Phase 1
    NCT02511795 AstraZeneca Ovarian, Breast, and Second-Line Small Cell Lung Cancer August 6, 2015 Phase 1
    NCT02506816 MedSIR|AstraZeneca|Experior Endometrial Carcinoma February 2016 Early Phase 1
    NCT03057145 Khanh Do|Eli Lilly and Company|AstraZeneca|Dana-Farber Cancer Institute Solid Tumor March 10, 2017 Phase 1
    NCT02208375 M.D. Anderson Cancer Center|AstraZeneca|National Cancer Institute (NCI) Breast Cancer|Malignant Female Reproductive System Neoplasm November 2014 Phase 1|Phase 2
    NCT02734004 AstraZeneca|Quintiles, Inc. Ovarian|Breast|SCLC|Gastric Cancers March 17, 2016 Phase 1|Phase 2
    NCT02889900 AstraZeneca|Myriad Genetic Laboratories, Inc. Recurrent Platinum Resistant Ovarian Cancer January 17, 2017 Phase 2
    NCT02489006 University Health Network, Toronto Ovarian Cancer|Fallopian Tube Cancer|Neoadjuvant Treatment|Debulking Surgical Procedures July 15, 2016 Phase 2
    NCT03009682 Samsung Medical Center Small Cell Lung Cancer August 2016 Phase 2
    NCT01851265 AstraZeneca Solid Tumours July 4, 2013 Phase 1
    NCT03167619 Kimberly Blackwell|AstraZeneca|Duke University Triple Negative Breast Cancer October 2017 Phase 2
    NCT02882308 Hellenic Cooperative Oncology Group|AstraZeneca Squamous Cell Carcinoma of the Head and Neck October 2016 Phase 2
    NCT03161132 Grupo Español de Investigación en Cáncer de Ovario|AstraZeneca Advanced Ovarian Cancer June 2017 Phase 2
    NCT01844986 AstraZeneca|Gynecologic Oncology Group (GOG)|Myriad Genetic Laboratories, Inc. Newly Diagnosed|Advanced Ovarian Cancer|FIGO Stage III-IV|BRCA Mutation|Complete Response|Partial Response|First Line Platinum Chemotherapy August 26, 2013 Phase 3
    NCT02184195 AstraZeneca|Myriad Genetic Laboratories, Inc. Germline BRCA1/2 Mutations and|Metastatic Adenocarcinoma of the Pancreas December 16, 2014 Phase 3
    NCT02340611 University Health Network, Toronto|AstraZeneca Ovarian Cancer June 2015 Phase 2
    NCT03212274 National Cancer Institute (NCI) Advanced Malignant Solid Neoplasm|Glioblastoma|Grade II Glioma|IDH1 Gene Mutation|IDH2 Gene Mutation|Recurrent Cholangiocarcinoma|Recurrent Glioma|Recurrent Malignant Solid Neoplasm|WHO Grade III Glioma March 30, 2018 Phase 2
    NCT01460888 The Christie NHS Foundation Trust|Cancer Research UK|AstraZeneca Carcinoma of the Oesophagus July 2013 Phase 1
    NCT02000622 AstraZeneca|Myriad Genetic Laboratories, Inc. Breast Cancer Metastatic|BRCA 1 Gene Mutation|BRCA 2 Gene Mutation March 27, 2014 Phase 3
    NCT02686008 Yale University Squamous Cell Carcinoma of the Head and Neck December 2016 Phase 1
    NCT01921140 AstraZeneca Solid Tumours September 24, 2013 Phase 1
    NCT01661868 Dana-Farber Cancer Institute Ovarian Cancer|Peritoneal Cancer|Fallopian Tube Cancer August 2012 Phase 2
    NCT01900028 AstraZeneca Solid Tumours October 2013 Phase 1
    NCT02769962 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Solid Tumors|Small Cell Lung Carcinoma|Carcinoma, Non-Small-Cell Lung|Lung Neoplasms May 3, 2016 Phase 1|Phase 2
    NCT02755844 Hospices Civils de Lyon Recurrent Endometrial Cancer April 2016 Phase 1|Phase 2
    NCT01116648 National Cancer Institute (NCI) Deleterious BRCA1 Gene Mutation|Deleterious BRCA2 Gene Mutation|Estrogen Receptor Negative|HER2/Neu Negative|Ovarian Endometrioid Adenocarcinoma|Ovarian Serous Adenocarcinoma|Ovarian Serous Surface Papillary Adenocarcinoma|Progesterone Receptor Negative|Recurrent Breast Carcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma|Triple-Negative Breast Carcinoma March 25, 2010 Phase 1|Phase 2
    NCT01972217 AstraZeneca Metastatic Castration-resistant Prostate Cancer April 1, 2014 Phase 2
    NCT01237067 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Cervical Cancer|Ovarian Cancer|Breast Cancer|Primary Peritoneal Cancer|Fallopian Tube Cancer|Endometrial Cancer October 26, 2010 Phase 1
    NCT02282020 AstraZeneca|Myriad Genetic Laboratories, Inc. Relapsed Ovarian Cancer, BRCA Mutation, Platinum Sensitivity February 6, 2015 Phase 3
    NCT02822157 Universitaire Ziekenhuizen Leuven|AstraZeneca Ovarian Epithelial Cancer August 2016 Phase 2
    NCT02324998 Cambridge University Hospitals NHS Foundation Trust|AstraZeneca Prostate Cancer December 2016 Phase 1
    NCT02418624 The Netherlands Cancer Institute Breast Cancer|Ovarian Cancer|Advanced Cancer May 2015 Phase 1
    NCT02485990 Sidney Kimmel Comprehensive Cancer Center|AstraZeneca|MedImmune LLC Primary Peritoneal Carcinoma December 2015 Phase 1|Phase 2
    NCT01874353 AstraZeneca|European Network of Gynaecological Oncology Trial Groups (ENGOT)|Myriad Genetic Laboratories, Inc. Platinum Sensitive|BRCA Mutated|Relapsed Ovarian Cancer|Following Complete or Partial Response to Platinum Based Chemotherapy September 3, 2013 Phase 3
    NCT02893917 National Cancer Institute (NCI) Castration Levels of Testosterone|Castration-Resistant Prostate Carcinoma|Metastatic Prostate Carcinoma|Prostate Adenocarcinoma With Focal Neuroendocrine Differentiation|Prostate Carcinoma Metastatic in the Bone|Prostate Small Cell Carcinoma|PSA Progression|Stage IV Prostate Adenocarcinoma December 23, 2016 Phase 2
    NCT01788332 Lisette Nixon|AstraZeneca|Velindre NHS Trust Non-small Cell Lung Cancer January 2014 Phase 2
    NCT01078662 AstraZeneca Ovarian|Breast|Prostate|Pancreatic|Advanced Tumours February 21, 2010 Phase 2
    NCT01894243 AstraZeneca Solid Tumours March 13, 2014 Phase 1
    NCT02681237 University Health Network, Toronto|AstraZeneca Ovarian Cancer April 29, 2016
    NCT03012321 Northwestern University|AstraZeneca|National Cancer Institute (NCI) Prostate Cancer Metastatic Castration-Resistant|Abnormal DNA Repair|Metastatic Prostate Carcinoma|Stage IV Prostate Cancer January 2017 Phase 2
    NCT01650376 Swedish Medical Center|AstraZeneca Stage III Ovarian Cancer|Stage IV Ovarian Cancer|Uterine Cancer August 2012 Phase 1|Phase 2
    NCT01894256 AstraZeneca Solid Tumours November 2013 Phase 1
    NCT02392676 AstraZeneca|Myriad Genetic Laboratories, Inc. Platinum Sensitive Relapsed Ovarian Cancer July 2016 Phase 3
    NCT01513174 Spanish Lung Cancer Group Non Small Cell Lung Cancer August 2011 Phase 1|Phase 2
    NCT02898207 National Cancer Institute (NCI) Estrogen Receptor Negative|HER2/Neu Negative|High Grade Fallopian Tube Serous Adenocarcinoma|High Grade Ovarian Serous Adenocarcinoma|Metastatic Malignant Solid Neoplasm|Primary Peritoneal High Grade Serous Adenocarcinoma|Progesterone Receptor Negative|Recurrent Breast Carcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma|Triple-Negative Breast Carcinoma|Unresectable Solid Neoplasm May 19, 2017 Phase 1
    NCT02684318 Poveda, Andrés, M.D.|AstraZeneca|PharmaMar Advanced Cancer|Ovarian Cancer|Endometrial Cancer|Breast Cancer July 2015 Phase 1|Phase 2
    NCT03127215 National Center for Tumor Diseases, Heidelberg|AstraZeneca|PharmaMar Cancers With DNA Repair-Deficiency August 1, 2017 Phase 2
    NCT02899728 National Cancer Institute (NCI) Small Cell Lung Carcinoma April 7, 2017 Phase 2
    NCT02345265 National Cancer Institute (NCI) Deleterious BRCA1 Gene Mutation|Deleterious BRCA2 Gene Mutation|Fallopian Tube Endometrioid Adenocarcinoma|Fallopian Tube Serous Adenocarcinoma|High Grade Ovarian Serous Adenocarcinoma|Ovarian Endometrioid Tumor|Primary Peritoneal Serous Adenocarcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma December 4, 2015 Phase 2
    NCT02987543 AstraZeneca Metastatic Castration-resistant Prostate Cancer February 6, 2017 Phase 3
    NCT02983799 AstraZeneca Relapsed Ovarian Cancer, BRCA Mutation, Platinum Sensitivity December 22, 2016 Phase 2
    NCT02571725 New Mexico Cancer Care Alliance Ovarian Cancer|Fallopian Tube Cancer|Peritoneal Neoplasms February 2016 Phase 1|Phase 2
    NCT02308072 University College, London|Cancer Research UK|AstraZeneca Head and Neck Cancer September 2015 Phase 1
    NCT02679963 Gustave Roussy, Cancer Campus, Grand Paris Non Small Cell Lung Cancer January 2016 Phase 2
    NCT03212742 Centre Francois Baclesse|National Cancer Institute, France Malignant Gliomas|Radiotherapy|PARP Inhibitor September 1, 2017 Phase 1|Phase 2
    NCT01924533 AstraZeneca Gastric Cancer September 2013 Phase 3
    NCT03079687 AstraZeneca|Parexel Ovarian Cancer
    NCT02477644 ARCAGY/ GINECO GROUP|Arbeitsgemeinschaft Gynaekologishe Onkologie Germany|Arbeitsgemeinschaft Gynaekologische Onkologie Austria|Grupo Español de Investigación en Cáncer de Ovario|Belgian Gynaecological Oncology Group|Multicenter Italian Trials in Ovarian cancer and gynecologic malignancies (MITO)|Mario Negri Gynecologic Oncology|Nordic Society for Gynaecologic Oncology|Gynecologic Oncology Trial & Investigation Consortium Ovarian Cancer May 2015 Phase 3
    NCT03008278 National Cancer Institute (NCI) Gastroesophageal Junction Adenocarcinoma|Metastatic Malignant Neoplasm in the Lymph Nodes|Recurrent Gastric Carcinoma|Stage IV Gastric Cancer AJCC v7 September 15, 2017 Phase 1|Phase 2
    NCT02953457 Roswell Park Cancer Institute|National Cancer Institute (NCI) BRCA1 Gene Mutation|BRCA2 Gene Mutation|Ovarian Serous Adenocarcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma June 29, 2017 Phase 1|Phase 2
    NCT03150576 Cambridge University Hospitals NHS Foundation Trust|AstraZeneca|Cancer Research UK Breast Cancer May 2016 Phase 2|Phase 3
    NCT00912743 AstraZeneca Colorectal Cancer May 2009 Phase 2
    NCT01296763 Sidney Kimmel Comprehensive Cancer Center|National Cancer Institute (NCI) Pancreatic Cancer January 2011 Phase 1
    NCT02430311 AstraZeneca Advanced Solid Tumours June 10, 2015 Phase 1
    NCT01063517 AstraZeneca Gastric Cancer February 2, 2010 Phase 2
    NCT03117933 University of Oxford|AstraZeneca Ovarian Cancer March 9, 2017 Phase 2
    NCT02498613 National Cancer Institute (NCI)|AstraZeneca BRCA1 wt Allele|BRCA2 wt Allele|Estrogen Receptor Negative|HER2/Neu Negative|Metastatic Pancreatic Adenocarcinoma|Pancreatic Adenocarcinoma|Progesterone Receptor Negative|Recurrent Breast Carcinoma|Recurrent Non-Small Cell Lung Carcinoma|Recurrent Pancreatic Carcinoma|Recurrent Small Cell Lung Carcinoma|Stage III Breast Cancer|Stage III Non-Small Cell Lung Cancer AJCC v7|Stage III Pancreatic Cancer AJCC v6 and v7|Stage III Small Cell Lung Carcinoma AJCC v7|Stage IIIA Breast Cancer|Stage IIIA Non April 26, 2016 Phase 2
    NCT03063710 AstraZeneca PSR Ovarian Cancer With a BRCA Mutation
    NCT01858168 Massachusetts General Hospital Ewing Sarcoma July 2013 Phase 1
    NCT02484404 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Lung Cancer|Breast Cancer|Ovarian Cancer|Colorectal Cancer|Prostate Cancer|Triple Negative Breast Cancer June 4, 2015 Phase 1|Phase 2
    NCT02974621 National Cancer Institute (NCI) Recurrent Glioblastoma September 15, 2017 Phase 2
    NCT02093351 AstraZeneca Solid Tumours September 1, 2014 Phase 1
    NCT02121990 Memorial Sloan Kettering Cancer Center|AstraZeneca|Genentech, Inc. Ovarian Cancer|Primary Peritoneal Cancer|Fallopian Tube Cancer April 21, 2014 Phase 1
    NCT01491139 University College, London|AstraZeneca Carcinoma, Squamous Cell Phase 1
    NCT02446600 National Cancer Institute (NCI)|AstraZeneca Deleterious BRCA1 Gene Mutation|Deleterious BRCA2 Gene Mutation|Endometrial Undifferentiated Carcinoma|Fallopian Tube Clear Cell Adenocarcinoma|Fallopian Tube Transitional Cell Carcinoma|Ovarian Clear Cell Adenocarcinoma|Ovarian Endometrioid Tumor|Ovarian Seromucinous Carcinoma|Ovarian Serous Tumor|Ovarian Transitional Cell Carcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma|Undifferentiated Fallopian Tube Carcinoma|Undifferentiated Ova February 4, 2016 Phase 3
    NCT02561832 AstraZeneca Breast Cancer November 2015 Phase 1
    NCT01390571 Cancer Research UK Brain and Central Nervous System Tumors July 2011 Phase 1
    NCT01081951 AstraZeneca Ovarian Cancer February 4, 2010 Phase 2
    NCT00535353 NCIC Clinical Trials Group|Canadian Cancer Trials Group Colorectal Cancer August 2007 Phase 1
    NCT02502266 National Cancer Institute (NCI) Deleterious BRCA1 Gene Mutation|Deleterious BRCA2 Gene Mutation|Fallopian Tube Clear Cell Adenocarcinoma|Fallopian Tube Endometrioid Adenocarcinoma|Fallopian Tube Serous Adenocarcinoma|Fallopian Tube Transitional Cell Carcinoma|Ovarian Clear Cell Adenocarcinoma|Ovarian Endometrioid Adenocarcinoma|Ovarian Seromucinous Carcinoma|Ovarian Serous Adenocarcinoma|Ovarian Transitional Cell Carcinoma|Primary Peritoneal Serous Adenocarcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|R February 5, 2016 Phase 2|Phase 3
    NCT02511223 Sheba Medical Center Pancreatic Cancer September 2015 Phase 2
    NCT02588105 AstraZeneca|INC Research Advanced Solid Tumours November 10, 2015 Phase 1
    NCT03022409 AstraZeneca Head and Neck Squamous Cell Carcinoma March 2017 Phase 1
    NCT02810743 The Netherlands Cancer Institute Breast Cancer August 2016 Phase 3
    NCT02861573 Merck Sharp & Dohme Corp. Metastatic Castration-Resistant Prostate Cancer November 17, 2016 Phase 1
    NCT03085147 Memorial Sloan Kettering Cancer Center Oral Squamous Cell Carcinoma (OSCC) March 15, 2017 Phase 1|Phase 2
    NCT02264678 AstraZeneca Adv Solid Malig - H&N SCC, ATM Pro / Def NSCLC, Gastric & Breast Cancer October 21, 2014 Phase 1|Phase 2
    NCT02546661 AstraZeneca Muscle Invasive Bladder Cancer October 3, 2016 Phase 1
    NCT02419495 M.D. Anderson Cancer Center|Karyopharm Therapeutics Inc Advanced Cancers June 26, 2015 Phase 1
    NCT02925234 The Netherlands Cancer Institute|Amgen|AstraZeneca|Bayer|Bristol-Myers Squibb|Novartis|Roche Pharma AG Cancer|Tumors|Neoplasm|Neoplasia August 2016 Phase 2
    NCT02299999 UNICANCER|Fondation ARC|AstraZeneca Metastatic Breast Cancer April 7, 2014 Phase 2
    NCT02693535 American Society of Clinical Oncology|AstraZeneca|Bayer|Bristol-Myers Squibb|Eli Lilly and Company|Genentech, Inc.|Merck Sharp & Dohme Corp.|Pfizer Lymphoma, Non-Hodgkin|Multiple Myeloma|Advanced Solid Tumors March 2016 Phase 2
    NCT02813135 Gustave Roussy, Cancer Campus, Grand Paris|National Cancer Institute, France Children, Adolescents and Young Adults With Refractory or Recurrent Malignancies June 2016 Phase 1|Phase 2
    NCT02624973 Haukeland University Hospital|Helse Vest|Pfizer|AstraZeneca Breast Cancer April 2016 Phase 2
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    References
    Preparing Stock Solutions
    Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
    1 mM 2.3017 mL 11.5085 mL 23.0171 mL
    5 mM 0.4603 mL 2.3017 mL 4.6034 mL
    10 mM 0.2302 mL 1.1509 mL 2.3017 mL
    Kinase Assay
    [1]

    This assay determined the ability of Olaparib to inhibit PARP-1 enzyme activity. PARP-2 activity inhibition is measured by using a variation of the PARP-1 assay in which PARP-2 protein (recombinant) is bound down by a PARP-2 specific antibody in a 96-well white-walled plate. PARP-2 activity is measured following 3H-NAD+ DNA additions. After washing, scintillant is added to measure 3H-incorporated ribosylations. For tankyrase-1, an AlphaScreen assay is developed in which HIS-tagged recombinant TANK-1 protein is incubated with biotinylated NAD+ in a 384-well ProxiPlate assay. Alpha beads are added to bind the HIS and biotin tags to create a proximity signal, whereas the inhibition of TANK-1 activity is directly proportional to the loss of this signal. All experiments are repeated at least three times[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [1]

    Olaparib is dissolved in DMSO and stored, and then diluted with appropriate media before use[1].

    The PF50 value is the potentiation factor, which is calculated as the ratio of the IC50 of the control growth with alkylating agent methylmethane sulfonate (MMS) divided by the IC50 of the MMS combined with the PARP inhibitor. HeLa B cells are used, and Olaparib is tested at a fixed 200 nM concentration for screening with MMS. For the testing of Olaparib on the SW620 colorectal cell line, the concentrations that are used are 1, 3, 10, 100 and 300 nM. Cell growth is assessed by the use of the sulforhodamine B (SRB) assay[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2]

    Olaparib is prepared in PBS (containing 10% DMSO and 10% 2-hydroxy-propyl-β-cyclodextrin) (Mice)[2].

    Mice[2]
    Mice bearing 220-250 mm3 tumors are randomized into 4 treatment groups (n=5): A; vehicle control (10% DMSO in PBS/10% 2-hydroxy-propyl-β-cyclodextrin daily for 5 days by oral gavage), B; Olaparib (50 mg/kg daily for 5 days by oral gavage), C; 10 Gy fractionated radiotherapy (2 Gy daily for 5 days), D; Olaparib and 10 Gy (5×2 Gy) fractionated radiotherapy (with olaparib given 30 min prior to each daily 2 Gy dose of radiation). Tumor volume measurements are determined daily until they reached 1000 mm3. The number of days for each individual tumor to quadruple in size from the start of the treatment (relative tumor volume×4; RTV4) is calculated for the individual tumors in each group. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    434.46

    Formula

    C₂₄H₂₃FN₄O₃

    CAS No.

    763113-22-0

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: 29 mg/mL

    in vivo: Olaparib is dissolved in DMSO (31.25 mg/mL) and then diluted with PBS (DMSO: PBS=1:9).
    Olaparib (AZD2281) is dissolved in 200 µL sterilized water)[3].

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    References

    Purity: 99.71%

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    Product Name:
    Olaparib
    Cat. No.:
    HY-10162
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