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Chemical Structure| 379231-04-6 Chemical Structure| 379231-04-6

Structure of Saracatinib
CAS No.: 379231-04-6

Chemical Structure| 379231-04-6

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Saracatinib (AZD0530) is a potent Src family inhibitor with IC50 values ranging from 2.7 to 11 nM for c-Src, Lck, c-YES, Lyn, Fyn, Fgr, and Blk, showing high selectivity over other tyrosine kinases.

Synonyms: AZD0530

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Product Details of Saracatinib

CAS No. :379231-04-6
Formula : C27H32ClN5O5
M.W : 542.03
SMILES Code : CN1CCN(CC1)CCOC2=CC(OC3CCOCC3)=C4C(N=CN=C4NC5=C(C=CC6=C5OCO6)Cl)=C2
Synonyms :
AZD0530
MDL No. :MFCD09832698
InChI Key :OUKYUETWWIPKQR-UHFFFAOYSA-N
Pubchem ID :10302451

Safety of Saracatinib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Saracatinib

RTK

Isoform Comparison

Biological Activity

Target
  • EGFR/ErbB1

    EGFR (L861Q), IC50:4 nM

    EGFR, IC50:5 nM

  • Fyn

    Fyn, IC50:10 nM

  • Src

    c-Src, IC50:2.7 nM

  • Lck

    LCK, IC50:<4 nM

  • Lyn

    Lyn, IC50:5 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
DS fibroblasts 2 μM 24 h lowering pY682APP-βCTF levels and rescuing v-ATPase deficits Sci Adv. 2023 Jul 28;9(30):eadg1925.
SK-Hep-1 cells 1 mM 6 h Inhibits YAP-induced tumor cell migration Cell Death Dis. 2021 Dec 3;12(12):1126.
PLC5 cells 20 µM 24 h To investigate the effect of Saracatinib on STAT3 phosphorylation in PLC5 cells, results showed that Saracatinib decreased STAT3 phosphorylation. J Transl Med. 2021 Apr 1;19(1):138.
PLC/PRF/5 cells 1 mM 6 h To test the inhibitory effect of Saracatinib on YAP-induced HCC cell migration Cell Death Dis. 2021 Dec 3;12(12):1126.
CRC cell lines 0.0625–2 µM 72 h To evaluate the antiproliferative effects of Saracatinib on CRC cell lines, LS180, H508, and LS174T cell lines were sensitive to Saracatinib with an IC50 of 0.5 µM. Clin Cancer Res. 2010 Aug 15;16(16):4165-77.
SW620, SW480, H508, LS174T 1 µM 48 h To evaluate the effects of Saracatinib on the cell cycle, H508 and LS174T cell lines showed G1 cell cycle arrest after 48 h. Clin Cancer Res. 2010 Aug 15;16(16):4165-77.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Operant conditioning-induced habitual responding for ethanol Intraperitoneal injection 5 mg/kg Single administration, 2h or 30 min prior to testing To evaluate the effects of saracatinib on habitual ethanol-seeking and consumption in mice. Results showed that saracatinib did not significantly alter habitual ethanol-seeking or consumption at either the 2-h or 30-min pretreatment time points. Front Psychiatry. 2021 Aug 31;12:709559
Mice Ts2 mouse model Oral 5 mg/kg Twice daily for 4 weeks Decreasing pY682APP-βCTF levels and restoring v-ATPase function Sci Adv. 2023 Jul 28;9(30):eadg1925.
Mice A549 xenograft model Oral 50 mg/kg Once daily for two weeks To evaluate the effect of Saracatinib in combination with Tazemetostat and MK-2206 on tumor growth, the results showed that the combination significantly reduced tumor weight Nat Commun. 2021 Dec 3;12(1):6941.
Nude mice CRC cell line xenograft model Oral gavage 50 mg/kg Daily for 28 days To evaluate the antitumor effects of Saracatinib in a CRC xenograft model, LS180 and LS174T cell lines were sensitive to Saracatinib with significant tumor growth reduction. Clin Cancer Res. 2010 Aug 15;16(16):4165-77.

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01144481 - Completed - Canada, Ontario ... More >> University Health Network Toronto, Ontario, Canada, M5G 2C4 Less <<
NCT00265876 Pancreatic Cancer Phase 1 Phase 2 Completed - Canada, British Columbia ... More >> BCCA - Vancouver Cancer Centre Vancouver, British Columbia, Canada, V5Z 4E6 Canada, Ontario Ottawa Health Research Institute - General Division Ottawa, Ontario, Canada, K1H 8L6 Algoma District Cancer Program Sault Ste. Marie, Ontario, Canada, P6B 0A8 Univ. Health Network-Princess Margaret Hospital Toronto, Ontario, Canada, M5G 2M9 Less <<
NCT01000896 Cancer Non Sm... More >>all Cell Lung Cancer Epithelial Ovarian Cancer Less << Phase 1 Withdrawn(AstraZeneca has disc... More >>ontinued the development of AZD0530. No new AstraZeneca-sponsored clinical studies will be initiated..) Less << March 2011 Japan ... More >> Research Site Matsuyama, Ehime, Japan Research Site Fukuoka, Japan Less <<
NCT00853983 Healthy Phase 1 Completed - United Kingdom ... More >> Research Site Alderley Park, Cheshire, United Kingdom Less <<
NCT00496028 Neoplasms Phase 1 Completed - France ... More >> Research Site Paris, France Research Site Pierre Benite Cedex, France Netherlands Research Site Amsterdam, Netherlands Research Site Groningen, Netherlands Norway Research Site Oslo, Norway United Kingdom Research Site Glasgow, United Kingdom Research Site Sutton, United Kingdom Less <<
NCT00475956 Neoplasms Phase 1 Completed - Germany ... More >> Research Site Freiburg, Baden-Wurttemberg, Germany Research Site Essen, Ruhr, Germany Research Site Herne, Ruhr, Germany Less <<
NCT00735917 Adenocarcinoma of the Pancreas... More >> Recurrent Pancreatic Cancer Stage IV Pancreatic Cancer Less << Phase 2 Completed - United States, Arizona ... More >> Mayo Clinic in Arizona Scottsdale, Arizona, United States, 85259 United States, Colorado University of Colorado at Denver Aurora, Colorado, United States, 80045 United States, Florida Mayo Clinic in Florida Jacksonville, Florida, United States, 32224-9980 United States, Michigan Wayne State University/Karmanos Cancer Institute Detroit, Michigan, United States, 48201 United States, Minnesota Mayo Clinic Rochester, Minnesota, United States, 55905 United States, Missouri Washington University School of Medicine Saint Louis, Missouri, United States, 63110 United States, Wisconsin University of Wisconsin Hospital and Clinics Madison, Wisconsin, United States, 53792 Australia, Western Australia Sir Charles Gairdner Hospital Nedlands, Western Australia, Australia, 6009 Singapore National University Hospital Singapore, Singapore, 119074 Less <<
NCT00610714 - Completed - -
NCT01216176 Breast Cancer Phase 1 Phase 2 Completed - United States, California ... More >> Stanford University Palo Alto, California, United States, 94304 United States, Florida University of Miami Miami, Florida, United States, 33136 Less <<
NCT00610714 Ovarian Neoplasms ... More >> Ovarian Cancer Less << Phase 2 Completed - -
NCT00771979 Healthy Phase 1 Completed - United Kingdom ... More >> Research Site Alderley Park, United Kingdom Less <<
NCT00558272 Breast Cancer ... More >> Prostate Cancer Bone Neoplasms Less << Phase 2 Completed - -
NCT00735917 - Completed - -
NCT00558272 - Completed - -
NCT01196741 - Completed - -
NCT00704366 Solid Tumor PHASE1 COMPLETED 2025-05-11 Research Site, Takatsuk, Osaka... More >>, Japan|Research Site, Sunto-gun, Shizuoka, Japan Less <<
NCT00752206 Osteosarcoma Phase 2 Completed - United States, Alabama ... More >> University of Alabama Birmingham, Alabama, United States, 35233 United States, California Children's Hospital Los Angeles Los Angeles, California, United States, 90027 USC/Norris Comprehensive Cancer Center and Hospital Los Angeles, California, United States, 90089 UCLA/Mattel's Children's Hospital Los Angeles, California, United States, 90095 Stanford University Palo Alto, California, United States, 94304 UCSF San Francisco, California, United States, 94143 Sarcoma Oncology Center Santa Monica, California, United States, 90403 United States, Florida University of Florida Gainesville, Florida, United States, 32610 University of Miami Miami, Florida, United States United States, Indiana Indiana University Indianapolis, Indiana, United States, 46202 United States, Iowa University of Iowa Hospitals and Clinics Iowa City, Iowa, United States, 52242 United States, Maryland Johns Hopkins Sidney Kimmel Comprehensive Cancer Center Baltimore, Maryland, United States, 21231 National Cancer Institute Bethesda, Maryland, United States, 20892 United States, Massachusetts Dana-Farber Cancer Institute Boston, Massachusetts, United States, 02115 United States, Michigan University of Michigan Ann Arbor, Michigan, United States, 48106 United States, Ohio Cincinnati Children's Hospital Medical Center Cincinnati, Ohio, United States, 45229 United States, Tennessee St. Jude Children's Research Hospital Memphis, Tennessee, United States, 38105 United States, Washington Seattle Cancer Care Alliance/University of Washington Medical Center Seattle, Washington, United States, 98109 Less <<
NCT01196741 Ovarian Cancer ... More >> Fallopian Tube Cancer Primary Peritoneal Cancer Less << Phase 2 Phase 3 Completed - United Kingdom ... More >> Addenbrooke's Hospital Cambridge, Cambridgeshire, United Kingdom, BC2 0QQ St Bartholomew's Hospital London, Greater London, United Kingdom, EC1A 7BE University College London Hospital London, Greater London, United Kingdom, NW1 2PG Guy's Hospital London, Greater London, United Kingdom, SE1 9RT The Royal Mardsen Hospital London, Greater London, United Kingdom, SW3 6JJ The Christie NHS Foundation Trust Manchester, Greater Manchester, United Kingdom, M20 4BX Mount Vernon Hospital Rickmansworth, Middlesex, United Kingdom, HA6 2RN The Churchill Hospital Oxford, Oxfordshire, United Kingdom, OX3 7LJ Queen's Hospital Burton upon Trent, Staffordshire, United Kingdom, DE13 0RB Royal Marsden Hospital Sutton, Surrey, United Kingdom, SM2 5PT St James's University Hospital Leeds, Yorkshire, United Kingdom, LS9 7TF Beatson West of Scotland Cancer Centre Glasgow, United Kingdom, G12 0YN Less <<
NCT02167256 Alzheimer's Disease Phase 2 Completed - -
NCT00659360 Adult Fibrosarcoma ... More >> Adult Leiomyosarcoma Adult Liposarcoma Adult Malignant Fibrous Histiocytoma Adult Rhabdomyosarcoma Dermatofibrosarcoma Protuberans Endometrial Stromal Sarcoma Recurrent Adult Soft Tissue Sarcoma Recurrent Uterine Sarcoma Stage III Adult Soft Tissue Sarcoma Stage III Uterine Sarcoma Stage IV Adult Soft Tissue Sarcoma Stage IV Uterine Sarcoma Uterine Carcinosarcoma Uterine Leiomyosarcoma Less << Phase 2 Completed - United States, Pennsylvania ... More >> Fox Chase Cancer Center Rockledge, Pennsylvania, United States, 19046 Canada, Alberta Cross Cancer Institute Edmonton, Alberta, Canada, T6G 1Z2 Canada, Ontario University Health Network-Princess Margaret Hospital Toronto, Ontario, Canada, M5G 2M9 Canada, Quebec Montreal General Hospital Montreal, Quebec, Canada, H3G 1A4 Less <<
NCT00397878 - Terminated - -
NCT02262026 Alcoholism Phase 1 Recruiting April 28, 2019 United States, Connecticut ... More >> Hartford Hospital Recruiting Hartford, Connecticut, United States, 06102 Contact: Godfrey Pearlson, MD    203-737-3416    godfrey.pearlson@hhchealth.org Less <<
NCT00513071 Hormone-resistant Prostate Can... More >>cer Recurrent Prostate Cancer Less << Phase 2 Completed - United States, California ... More >> City of Hope Duarte, California, United States, 91010 Less <<
NCT00513071 - Completed - -
NCT00397878 Adenocarcinoma of the Colon ... More >> Adenocarcinoma of the Rectum Recurrent Colon Cancer Recurrent Rectal Cancer Stage IV Colon Cancer Stage IV Rectal Cancer Less << Phase 2 Terminated - United States, Texas ... More >> M D Anderson Cancer Center Houston, Texas, United States, 77030 Less <<
NCT00513435 - Completed - -
NCT00659360 - Completed - -
NCT00718809 Invasive Thymoma and Thymic Ca... More >>rcinoma Recurrent Thymoma and Thymic Carcinoma Stage III Thymoma Stage IVA Thymoma Stage IVB Thymoma Less << Phase 2 Terminated - United States, California ... More >> Stanford University Hospitals and Clinics Stanford, California, United States, 94305 United States, Indiana Indiana University Medical Center Indianapolis, Indiana, United States, 46202 Less <<
NCT00513435 Metastatic Squamous Neck Cance... More >>r With Occult Primary Squamous Cell Carcinoma Recurrent Metastatic Squamous Neck Cancer With Occult Primary Recurrent Squamous Cell Carcinoma of the Hypopharynx Recurrent Squamous Cell Carcinoma of the Larynx Recurrent Squamous Cell Carcinoma of the Lip and Oral Cavity Recurrent Squamous Cell Carcinoma of the Nasopharynx Recurrent Squamous Cell Carcinoma of the Oropharynx Recurrent Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity Recurrent Verrucous Carcinoma of the Larynx Recurrent Verrucous Carcinoma of the Oral Cavity Stage III Squamous Cell Carcinoma of the Hypopharynx Stage III Squamous Cell Carcinoma of the Larynx Stage III Squamous Cell Carcinoma of the Lip and Oral Cavity Stage III Squamous Cell Carcinoma of the Nasopharynx Stage III Squamous Cell Carcinoma of the Oropharynx Stage III Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity Stage III Verrucous Carcinoma of the Larynx Stage III Verrucous Carcinoma of the Oral Cavity Stage IV Squamous Cell Carcinoma of the Hypopharynx Stage IV Squamous Cell Carcinoma of the Nasopharynx Stage IVA Squamous Cell Carcinoma of the Larynx Stage IVA Squamous Cell Carcinoma of the Lip and Oral Cavity Stage IVA Squamous Cell Carcinoma of the Oropharynx Stage IVA Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity Stage IVA Verrucous Carcinoma of the Larynx Stage IVA Verrucous Carcinoma of the Oral Cavity Stage IVB Squamous Cell Carcinoma of the Larynx Stage IVB Squamous Cell Carcinoma of the Lip and Oral Cavity Stage IVB Squamous Cell Carcinoma of the Oropharynx Stage IVB Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity Stage IVB Verrucous Carcinoma of the Larynx Stage IVB Verrucous Carcinoma of the Oral Cavity Stage IVC Squamous Cell Carcinoma of the Larynx Stage IVC Squamous Cell Carcinoma of the Lip and Oral Cavity Stage IVC Squamous Cell Carcinoma of the Oropharynx Stage IVC Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity Stage IVC Verrucous Carcinoma of the Larynx Stage IVC Verrucous Carcinoma of the Oral Cavity Tongue Cancer Less << Phase 2 Completed - United States, New York ... More >> Memorial Sloan Kettering Cancer Center New York, New York, United States, 10065 Less <<
NCT00559507 - Completed - -
NCT00718809 - Terminated - -
NCT01267266 - Terminated(Per protocol, study... More >> was terminated due to low rate of randomized patients.) Less << - -
NCT00559507 Estrogen Receptor-negative Bre... More >>ast Cancer Male Breast Cancer Progesterone Receptor-negative Breast Cancer Recurrent Breast Cancer Stage IIIB Breast Cancer Stage IIIC Breast Cancer Stage IV Breast Cancer Less << Phase 2 Completed - United States, New York ... More >> Memorial Sloan Kettering Cancer Center New York, New York, United States, 10065 Less <<
NCT00528645 Extensive Stage Small Cell Lun... More >>g Cancer Lung Metastases Malignant Pleural Effusion Recurrent Small Cell Lung Cancer Less << Phase 2 Completed - United States, Minnesota ... More >> North Central Cancer Treatment Group Rochester, Minnesota, United States, 55905 Less <<
NCT00638937 Recurrent Non-small Cell Lung ... More >>Cancer Stage IIIB Non-small Cell Lung Cancer Stage IV Non-small Cell Lung Cancer Less << Phase 2 Completed - Canada, Ontario ... More >> Juravinski Cancer Centre at Hamilton Health Sciences Hamilton, Ontario, Canada, L8V 5C2 The Ottawa Hospital Cancer Centre (Ottawa Health Research Institute) Civic Campus Ottawa, Ontario, Canada, K1Y 4E9 University Health Network-Princess Margaret Hospital Toronto, Ontario, Canada, M5G 2M9 Canada, Quebec McGill University Department of Oncology Montreal, Quebec, Canada, H2W 1S6 Less <<
NCT00528645 - Completed - -
NCT00607594 - Completed - -
NCT00607594 Adenocarcinoma of the Gastroes... More >>ophageal Junction Adenocarcinoma of the Stomach Recurrent Gastric Cancer Stage III Gastric Cancer Stage III Esophageal Cancer Stage IV Esophageal Cancer Stage IV Gastric Cancer Less << Phase 2 Completed - United States, Georgia ... More >> Hamilton Medical Center Dalton, Georgia, United States, 30720 Canada, Alberta Cross Cancer Institute Edmonton, Alberta, Canada, T6G 1Z2 Canada, Ontario Juravinski Cancer Centre at Hamilton Health Sciences Hamilton, Ontario, Canada, L8V 5C2 University Health Network-Princess Margaret Hospital Toronto, Ontario, Canada, M5G 2M9 Canada, Quebec McGill University Department of Oncology Montreal, Quebec, Canada, H2W 1S6 Less <<
NCT02955186 Alcohol Drinking Phase 2 Recruiting June 2021 United States, Connecticut ... More >> CMHC, Substance Abuse Center Recruiting New Haven, Connecticut, United States, 06519 Contact: Dana A Cavallo, Ph.D.    203-974-7607    dana.cavallo@yale.edu    Principal Investigator: Suchitra Krishnan-Sarin, Ph.D. Less <<
NCT00638937 - Completed - -
NCT02085603 Cancer Phase 2 Completed - United Kingdom ... More >> Sheffield Teaching Hospitals NHS Trust Sheffield, South Yorkshire, United Kingdom, S10 1SN Less <<
NCT01267266 Hormone-resistant Prostate Can... More >>cer Recurrent Prostate Cancer Stage IV Prostate Cancer Less << Phase 2 Terminated(Per protocol, study... More >> was terminated due to low rate of randomized patients.) Less << - United States, Illinois ... More >> University of Chicago Chicago, Illinois, United States, 60637 Decatur Memorial Hospital Decatur, Illinois, United States, 62526 NorthShore University HealthSystem-Evanston Hospital Evanston, Illinois, United States, 60201 Ingalls Memorial Hospital Harvey, Illinois, United States, 60426 Loyola University Medical Center Maywood, Illinois, United States, 60153 Illinois CancerCare-Peoria Peoria, Illinois, United States, 61615 Central Illinois Hematology Oncology Center Springfield, Illinois, United States, 60702 Southern Illinois University Springfield, Illinois, United States, 62702 United States, Indiana Fort Wayne Medical Oncology and Hematology Inc-Parkview Fort Wayne, Indiana, United States, 46845 United States, Maryland University of Maryland Greenebaum Cancer Center Baltimore, Maryland, United States, 21201-1595 United States, Michigan University of Michigan Ann Arbor, Michigan, United States, 48109 United States, Missouri Saint John's Mercy Medical Center Saint Louis, Missouri, United States, 63141 United States, Texas M D Anderson Cancer Center Houston, Texas, United States, 77030 United States, Wisconsin University of Wisconsin Women's Health Center Madison, Wisconsin, United States, 53715 Froedtert and the Medical College of Wisconsin Milwaukee, Wisconsin, United States, 53226 Less <<
NCT00669019 - Completed - -
NCT02732587 Alcohol Drinking PHASE1 COMPLETED 2016-03-23 CMHC, Substance Abuse Center, ... More >>New Haven, Connecticut, 06519, United States Less <<
NCT03661125 Parkinson Disease Psychosis Early Phase 1 Not yet recruiting September 1, 2021 United Kingdom ... More >> Mitul Mehta Not yet recruiting London, Camberwell, United Kingdom, SE5 8AF Contact: Mitul Mehta    +44 (0)2032283053    mitul.mehta@kcl.ac.uk    Contact: Miriam Vignando    07492634351    miriam.vignando@kcl.ac.uk Less <<
NCT00669019 Recurrent Melanoma ... More >> Stage IIA Melanoma Stage IIB Melanoma Stage IIC Melanoma Stage IV Melanoma Less << Phase 2 Completed - United States, Illinois ... More >> University of Chicago Comprehensive Cancer Center Chicago, Illinois, United States, 60637-1470 Less <<
NCT01864655 Alzheimer's Disease Phase 1 Completed - United States, Connecticut ... More >> Yale Alzheimer's Disease Research Unit New Haven, Connecticut, United States, 06510 Less <<
NCT02737202 Pulmonary Lymphangioleiomyomat... More >>osis Less << Phase 2 Recruiting July 30, 2020 United States, California ... More >> Stanford University Recruiting Stanford, California, United States, 94305 Contact: Susan Jacobs, RN MS    650-725-8083    ssjpulm@stanford.edu    Principal Investigator: Stephen Ruoss, MD          United States, Illinois Loyola Medical Center Recruiting Chicago, Illinois, United States, 90153 Contact: Elizabeth Kirwan, RN    708-216-2057    ekirwan@luc.edu    Principal Investigator: Daniel Dilling, MD          United States, Maryland Laboratory of Translational Research NHLBI Recruiting Bethesda, Maryland, United States, 20814 Contact: Mary Haughey, RN    301-496-3632    mhaughey@nhlbi.nih.gov    Principal Investigator: Joel Moss, MD          United States, Ohio University of Cincinnati Recruiting Cincinnati, Ohio, United States, 45267 Contact: Tammy Roads    513-558-2148    roadst@ucmail.uc.edu    Principal Investigator: Frank X McCormack, MD          United States, Texas Baylor College of Medicine - Ben Taub General Hospital Recruiting Houston, Texas, United States, 77030 Contact: Caryn O Pope    713-873-2471    cpope@bcm.edu    Principal Investigator: Nicola A Hanania, MD Less <<
NCT02116712 Pulmonary Lymphangioleiomyomat... More >>osis Less << PHASE1 COMPLETED 2025-07-15 University of Cincinnati, Cinc... More >>innati, Ohio, 45267, United States|Baylor College of Medicine, Houston, Texas, 77030, United States|University of Texas Health Science Center-Houston, Houston, Texas, 77030, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.84mL

0.37mL

0.18mL

9.22mL

1.84mL

0.92mL

18.45mL

3.69mL

1.84mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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