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Chemical Structure| 1374640-70-6 Chemical Structure| 1374640-70-6

Structure of Rociletinib
CAS No.: 1374640-70-6

Chemical Structure| 1374640-70-6

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Rociletinib (CO-1686) is an orally delivered kinase inhibitor that specifically targets mutant forms of EGFR, including T790M, with Ki values of 21.5 nM for EGFRL858R/T790M and 303.3 nM for EGFRWT.

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Product Details of Rociletinib

CAS No. :1374640-70-6
Formula : C27H28F3N7O3
M.W : 555.55
SMILES Code : C=CC(NC1=CC=CC(NC2=NC(NC3=CC=C(N4CCN(C(C)=O)CC4)C=C3OC)=NC=C2C(F)(F)F)=C1)=O
MDL No. :MFCD26793864
InChI Key :HUFOZJXAKZVRNJ-UHFFFAOYSA-N
Pubchem ID :57335384

Safety of Rociletinib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Rociletinib

RTK
JAK-STAT

Isoform Comparison

Biological Activity

Description
Rociletinib (CO-1686) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively[1].
Target
  • EGFR/ErbB1

    EGFR (wt), Ki:303.3 nM

    EGFR (L858R/T790M), Ki:21.5 nM

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02147990 Non-small Cell Lung Cancer PHASE2 TERMINATED 2019-08-27 UCLA Medical Center, Alhambra,... More >> California, 91801, United States|Comprehensive Blood and Cancer Center, Bakersfield, California, 93309, United States|Saint Jude Heritage Healthcare, Fullerton, California, 92835, United States|University of California San Diego Moores Cancer Center, La Jolla, California, 92093, United States|Northridge Hospital Medical Center, Northridge, California, 91328, United States|Cancer Care Associates, Redondo Beach, California, 90277, United States|University of California Davis Medical Center, Sacramento, California, 95817, United States|University of California San Francisco, San Francisco, California, 94115, United States|Coastal Integrative Cancer Care, San Luis Obispo, California, 93401, United States|Saint Mary's Regional Cancer Center, Grand Junction, Colorado, 81501-6132, United States|Rocky Mountain Cancer Centers, LLP, Lone Tree, Colorado, 80218, United States|Yale University School of Medicine, New Haven, Connecticut, 32135, United States|Advanced Medical Specialties, Miami, Florida, 33176, United States|Cleveland Clinic Florida, Weston, Florida, 33331, United States|Northwestern University Feinberg School of Medicine, Chicago, Illinois, 60611, United States|University of Illinois Chicago, Chicago, Illinois, 60612, United States|Illinois Cancer Specialists, Niles, Illinois, 60714, United States|Beth Israel Comprehensive Cancer Center, Boston, Massachusetts, 02215, United States|Lahey Hospital and Medical Center, Burlington, Massachusetts, 01805, United States|Minnesota Oncology Hematology, P.A, Minneapolis, Minnesota, 55404, United States|Mayo Clinic - Rochester, Rochester, Minnesota, 55905, United States|Washington University School of Medicine, Saint Louis, Missouri, 63110, United States|Montefiore Medical Center, Bronx, New York, 10461, United States|New York Oncology Hematology, PC, Latham, New York, 12110-2188, United States|University of Rochester, Rochester, New York, 14642, United States|University Hospitals of Cleveland, Cleveland, Ohio, 44106, United States|Cleveland Clinic, Cleveland, Ohio, 44195, United States|Fox Chase Cancer Center, Philadelphia, Pennsylvania, 19111, United States|Tennessee Oncology, PLLC, Nashville, Tennessee, 37203, United States|Texas Oncology P.A., Amarillo, Texas, 79106, United States|USO - Texas Oncology P.A., Arlington, Texas, 76014, United States|Texas Oncology-Austin Central, Austin, Texas, 78705, United States|Texas Oncology-Beaumont, Beaumont, Texas, 77702, United States|Texas Oncology P.A., Bedford, Texas, 76022, United States|Texas Oncology P.A., Dallas, Texas, 75246, United States|Texas Oncology P.A., Flower Mound, Texas, 75028, United States|The Methodist Hospital, Houston, Texas, 77030, United States|Texas Oncology - Plano East, Plano, Texas, 75075-7787, United States|Virginia Cancer Specialists, Fairfax, Virginia, 22031, United States|Northwest Cancer Specialists, P.C., Vancouver, Washington, 98686, United States|Yakima Valley Memorial Hospital, North Star Lodge, Yakima, Washington, 98902, United States|Icon Cancer Centre, South Brisbane, New South Wales, 4101, Australia|Royal North Shore Hospital, Sydney, New South Wales, 2065, Australia|Westmead Hospital, Westmead, New South Wales, 2145, Australia|Flinders Medical Centre, Bedford Park, South Australia, 5042, Australia|Princess Margaret Hospital, Toronto, Ontario, M5G 2L7, Canada|Centre Hospitalier Regional Universitaire (CHRU) de Besancon - L'Hopital Jean Minjoz, Besan?on, Franche-comte, 25030 cedex, France|H?pital Tenon, Paris, Ile-de-france, 75020, France|Institut Gustave Roussy, Villejuif, Ile-de-France, 94805, France|Institut de Cancérologie de l'Ouest - René Gauducheau, Saint Herblain cedex, PAYS DE LA Loire, France|Centre Hospitalier Lyon Sud, Pierre Bénité cedex, Rhone-alpes, 69495, France|Centre Hospitalier Universitaire C?te de Nacre, Caen, France|Centre Hospitalier Universitaire H?pital Nord, Marseille Cedex 20, 13915, France|Asklepios Fachkliniken München-Gauting, Gauting, Bayern, 82131, Germany|Klinikum Innenstadt LMU, München, Bayern, 80336, Germany|Goethe-Universit?t Frankfurt am Main, Frankfurt am Main, Hessen, 60590, Germany|Pius Hospital Oldenburg, Oldenburg, Niedersachsen, 26121, Germany|Universitaetsklinikum Bonn - Zentrum fuer Innere Medizin - Medizinische Klinik und Poliklink III, Bonn, Nordrhein-westfalen, 53127, Germany|Universit?tsklinikum Essen, Essen, Nordrhein-westfalen, 45122, Germany|Universit?tsklinikum K?ln, K?ln, Nordrhein-westfalen, 50937, Germany|LungenClinic Gro?hansdorf GmbH, Gro?hansdorf, Schleswig-holstein, 22927, Germany|Evangelische Lungenklinik Berlin, Berlin, 13125, Germany|Queen Mary Hospital, Hong Kong, Hong Kong|Chungbuk National University Hospital, Chungju, Chungcheongbuk-do, Korea, Republic of|National Cancer Center, Goyang-si, Gyeonggi-do, Korea, Republic of|Gachon University Gil Medical Center, Incheon, Gyeonggi-do, 405-760, Korea, Republic of|Dong-A University Hospital, Busan, Korea, Republic of|Inha University Hospital, Incheon, 400-711, Korea, Republic of|Samsung Medical Center, Seoul, 135-710, Korea, Republic of|Asan Medical Center, Seoul, Korea, Republic of|Seoul National University Hospital, Seoul, Korea, Republic of|Seoul Saint Mary's Hospital, Seoul, Korea, Republic of|Severance Hospital, Yonsei University Health System, Seoul, Korea, Republic of|Antoni van Leeuwenhoek Hospital, Amsterdam, Noord-holland, 1066 CX, Netherlands|Vrije Universiteit Medisch Centrum, Amsterdam, 1081 HV, Netherlands|Hospital Universitario Virgen del Rocio, Seville, Sevilla, 41013, Spain|Hospital Universitari Germans Trias i Pujol, Badalona, Spain|Hospital Vall d′Hebrón, Barcelona, 08035, Spain|Hospital Universitario Quirón Dexeus, Barcelona, Spain|Hospital Universitario La Paz, Madrid, Spain|Centre Hospitalier Universitaire Vaudoise, Lausanne, Vaud, 1011, Switzerland|Taipei Veterans General Hospital, Taipei, Taipei CITY, 11217, Taiwan|Chang Gung Memorial Hospital Linkou, Taoyuan, Tao-Yuan, 33305, Taiwan|China Medical University Hospital, Taichung, 40447, Taiwan|Taichung Veterans General Hospital, Taichung, 40705, Taiwan|National Taiwan University Hospital, Taipei, 100, Taiwan|Cambridge University Hospitals NHS Foundation Trust, Cambridge, England, CB2 0QQ, United Kingdom|Guy's and Saint Thomas NHS Foundation Trust, London, Greater London, SE1 9RT, United Kingdom|Royal Marsden Hospital, London, Greater London, SW3 6JJ, United Kingdom|Royal Marsden NHS Trust, Sutton, Surrey, SM2 5PT, United Kingdom|University College Hospital, London, NW1 2PQ, United Kingdom Less <<
NCT02547675 Non-small Cell Lung Cancer NO_LONGER_AVAILABLE - Mayo Clinic Arizona, Scottsdal... More >>e, Arizona, 85024, United States|Compassionate Care Research Group, Inc., Fountain Valley, California, 92866, United States|Pacific Cancer Care, Monterey, California, 93940, United States|Sutter Cancer Institute, Sacramento, California, 95816, United States|UCSF Helen Diller Family Comprehensive Cancer Center, San Francisco, California, 94115, United States|Halifax Health - Center for Oncology, Daytona Beach, Florida, 32114, United States|UF Health Center Orlando, Orlando, Florida, 32806, United States|Beth Israel Deaconess Medical Center, Boston, Massachusetts, 02215, United States|Henry Ford Hospital, Detroit, Michigan, 48202, United States|Billings Clinic, Billings, Montana, 59101, United States|Tulsa Cancer Institute, Tulsa, Oklahoma, 74146, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.80mL

0.36mL

0.18mL

9.00mL

1.80mL

0.90mL

18.00mL

3.60mL

1.80mL

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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