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Chemical Structure| 606143-89-9 Chemical Structure| 606143-89-9

Structure of Binimetinib
CAS No.: 606143-89-9

Chemical Structure| 606143-89-9

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Binimetinib (MEK162) is an oral and selective inhibitor of MEK1/2, with an IC50 of 12 nM.

Synonyms: MEK162; ARRY-162; ARRY-438162

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Product Details of Binimetinib

CAS No. :606143-89-9
Formula : C17H15BrF2N4O3
M.W : 441.23
SMILES Code : O=C(C1=C(NC2=CC=C(Br)C=C2F)C(F)=C3N=CN(C)C3=C1)NOCCO
Synonyms :
MEK162; ARRY-162; ARRY-438162
MDL No. :MFCD22124525
InChI Key :ACWZRVQXLIRSDF-UHFFFAOYSA-N
Pubchem ID :10288191

Safety of Binimetinib

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

Related Pathways of Binimetinib

MAPK

Isoform Comparison

Biological Activity

Target
  • MEK

    MEK, IC50:12 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Neonatal rat cardiomyocytes (NRCM) 10 µM 1 h Binimetinib inhibited ERK1/2 activation, prevented cardiomyocyte hypertrophy but also increased cell death. PMC7138859
A375 cells 0.1 nM to 10 nM 5 days To evaluate the inhibitory effect of Binimetinib on A375 cells, results showed that Binimetinib has an inhibitory effect on A375 cells. PMC9890140
PC-9 cells 1 μM 7 or 14 days To study the inhibitory effect of Binimetinib on PC-9 cells, 57 resistant ORFs were identified, revealing the central role of the MAP kinase pathway in resistance to EGFR inhibitors. PMC6981068
A549 cells 1 µM Investigate the effect of Binimetinib on the migration of KRAS-mutant cells, showing that Binimetinib reversibly inhibits cell migration. PMC11408588
A431 cells 1 µM Study the effect of Binimetinib on filopodia formation in A431 cells upon EGF stimulation, showing that Binimetinib significantly reduces filopodia formation. PMC11408588
m82 (Brn2-hom) and m82-BRN2 mouse melanoma cells 10^-3 to 100 μM 9 days To evaluate the effect of Binimetinib on colony formation in mouse melanoma cells and determine the IC50. Results showed that Brn2-het/hom cells are more sensitive to Binimetinib than WT cells. PMC8211827
SKOV3 10 µM 1 h MAP3K8 inhibition by KI significantly reduced the total number of cells in the two ovarian cancer cell lines tested. PMC4633961
IGROV-1 10 µM 1 h MAP3K8 inhibition by KI significantly reduced the total number of cells in the two ovarian cancer cell lines tested. PMC4633961

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice KitV558Δ;T669I/+ mice Oral 10 mg/kg Twice daily for 7 days To evaluate the effect of Binimetinib on imatinib-resistant KitV558Δ;T669I/+ mouse tumors, results showed that both PI3K and MAPK signaling pathways were inhibited, and tumor cell proliferation was reduced. PMC5635919
mice SK-N-AS xenograft model oral 3 mg/kg or 30 mg/kg twice daily, monitored continuously Binimetinib significantly inhibited SK-N-AS tumor growth and increased survival PMC4775079

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01885195 Solid Tumor and Hematologic Ma... More >>lignancies Less << PHASE2 COMPLETED 2017-04-11 University of South Alabama / ... More >>Mitchell Cancer Institute Univ South Alabama, Mobile, Alabama, 36688, United States|Alaska Oncology and Hematology AOH (2), Anchorage, Alaska, 99508, United States|Arizona Oncology Associates AZ Oncology Assoc., Phoenix, Arizona, United States|Arizona Oncology Associates HOPE Division, Phoenix, Arizona, United States|Arizona Oncology Associates PC- NAHOA, Sedona, Arizona, 86336, United States|Highlands Oncology Group Highlands Oncology Group (22), Fayetteville, Arkansas, 72703, United States|PCR Oncology, Pismo Beach, California, 93449, United States|University of California Davis Cancer Center UC Davis Cancer (3), Sacramento, California, 95817, United States|Rocky Mountain Cancer Centers USOR, Boulder, Colorado, 80304, United States|Yale University School of Medicine Yale Cancer Center, New Haven, Connecticut, 06511, United States|Whittingham Cancer Center Norwalk Hospital, Norwalk, Connecticut, 06856, United States|Eastern Connecticut Hematology & Oncology Associates Dept. of ECHO, Norwich, Connecticut, 06360, United States|Hematology Oncology PC Stamford Hospital, Stamford, Connecticut, 06902, United States|Florida Cancer Specialists Florida Cancer Specialists (31, Fort Myers, Florida, 33901, United States|Memorial Cancer Institute Memorial Healthcare System, Hollywood, Florida, 33021, United States|Cancer Specialists of North Florida, Jacksonville, Florida, 32256, United States|Mt. Sinai Comprehensive Cancer Center, Miami Beach, Florida, 33140, United States|Ocala Oncology Center Dept. of Ocala Oncology Center, Ocala, Florida, 34474, United States|Cancer Centers of Florida PA Cancer Centers of FL-Orlando-4, Ocoee, Florida, United States|University Cancer & Blood Center, LLC, Athens, Georgia, 30607, United States|Lurie Children's Hospital of Chicago Developmental Therapeutics, Chicago, Illinois, 60611, United States|Oncology Specialists, SC Onc Specialists, Park Ridge, Illinois, 60068-0736, United States|Illinois Cancer Care IL. Cancer Care, Peoria, Illinois, 61615-7828, United States|Indiana University Indiana Univ. - Purdue Univ., Indianapolis, Indiana, 46202, United States|University of Iowa Hospitals & Clinics Regulatory Contact 2, Iowa City, Iowa, 52242, United States|Maryland Oncology Hematology, P.A. Oncology Hematology, Rockville, Maryland, 20850, United States|Cancer and Hematology Centers of West Michigan Dept. of Oncology, Grand Rapids, Michigan, 49546, United States|Metro MN CCOP - Coon Rapids, Coon Rapids, Minnesota, 55433, United States|Research Medical Center Research Med Center (2), Kansas City, Missouri, 64132, United States|Washington University School of Medicine Washington University (16), Saint Louis, Missouri, 63110, United States|Glacier View Research Institute - Cancer Oncology Dept, Kalispell, Montana, 59901, United States|Comprehensive Cancer Centers of Nevada CCC of Nevada (21), Las Vegas, Nevada, 89109, United States|Cancer Institute of New Jersey CINJ, New Brunswick, New Jersey, 08901, United States|New Mexico Cancer Care Alliance Oncology Dept, Albuquerque, New Mexico, 87106, United States|New York Oncology Hematology, P.C. NYOH Latham, Troy, New York, 12180, United States|University of North Carolina Chapel Hill Physician Office Building, Chapel Hill, North Carolina, 27514, United States|Duke University Medical Center Seeley G. Mudd Bldg., Durham, North Carolina, 27710, United States|Sanford Research/USD-Fargo Sanford Hematology Oncology, Fargo, North Dakota, 58122, United States|Cleveland Clinic Foundation Cleveland Clinic (19), Cleveland, Ohio, 44195, United States|Ohio State University Medical Center Comprehensive Cancer Center, Columbus, Ohio, 43221, United States|St. Charles Cancer Center, Bend, Oregon, 97701, United States|Willamette Valley Clinical Studies Cancer Institute & Res. Ctr., Eugene, Oregon, 97404, United States|Northwest Cancer Specialists Vancouver Cancer Center, Portland, Oregon, 97210, United States|Oregon Health & Science University Oregon Health & Science U (56), Portland, Oregon, 97239, United States|St. Luke's Hospital and Health Network St Luke's (2), Bethlehem, Pennsylvania, United States|West Penn Allegheny Oncology Network, Natrona Heights, Pennsylvania, 15065, United States|Abington Hematology Oncology Associates, Inc Abington Hem Onc Assoc (5), Willow Grove, Pennsylvania, 19090, United States|Chattanooga Oncology and Hematology Assoicates, PC Chattanooga Oncology, Chattanooga, Tennessee, 37404, United States|The West Clinic Dept. of the West Clinic, Memphis, Tennessee, 38120, United States|Sarah Cannon Research Institute Sarah Cannon Research Inst (51, Nashville, Tennessee, 37203, United States|Texas Oncology Presbyterian Hospital (3), Dallas, Texas, 75246, United States|Texas Oncology Texas Oncology - Denton, Dallas, Texas, 75246, United States|Texas Oncology Austin Midtown, Dallas, Texas, 75251, United States|Texas Oncology Texas Oncology - Midland, Dallas, Texas, 75251, United States|Sammons Cancer Center - Texas Oncology Sammons Cancer Center (10), Dallas, Texas, 78246, United States|Oncology Consultants Oncology Group, Houston, Texas, 77024, United States|MD Anderson Cancer Center/University of Texas MD Anderson Cancer Center (3), Houston, Texas, 77030, United States|Cancer Care Centers of South Texas / HOAST CCC of So. TX-San Antonio (3), San Antonio, Texas, 78229, United States|Tyler Cancer Center Dept.ofTylerCancerCtr. (2), Tyler, Texas, 75702, United States|Deke Slayton Cancer Center Deke Slayton Cancer Center (2), Webster, Texas, 77598, United States|Intermountain Medical Center Intermountain Healthcare, Murray, Utah, 84157, United States|Virginia Cancer Specialists, PC Virginia Cancer Specialists, Fairfax, Virginia, 22031, United States|Medical Oncology & Hematology Associates of Northern VA Med Onc Hem Northern VA, Reston, Virginia, 20190, United States|Kadlec Clinic Hematology and Oncology Kadlec Clinic Hematology & Onc, Kennewick, Washington, 99336, United States|Providence Regional Cancer System, Lacey, Washington, 98503, United States|MultiCare Health System Institute for Research & Innovation MultiCare, Tacoma, Washington, 98405, United States|Northwest Medical Specialties NW Medical Specialties, Tacoma, Washington, 98405, United States|Medical College of Wisconsin Cancer Center, Milwaukee, Wisconsin, 53226, United States Less <<
NCT03231306 Neurofibromatosis Type 1|Plexi... More >>form Neurofibroma Less << PHASE2 COMPLETED 2024-04-17 University of Alabama at Birmi... More >>ngham, Birmingham, Alabama, 35294, United States|Children's Hospital of Los Angeles, Los Angeles, California, 90027, United States|University of California at Los Angeles, Los Angeles, California, 90095, United States|UCSF Benioff Children's Hospital Oakland, Oakland, California, 94609, United States|University of California, San Diego - Rady Children's Hospital, San Diego, California, 92123, United States|University of California, San Francisco, San Francisco, California, 94153, United States|Children's National Medical Center, Washington DC, District of Columbia, 20010, United States|Lurie Children's Hospital of Chicago, Chicago, Illinois, 60611, United States|University of Chicago, Chicago, Illinois, 60637, United States|Indiana University, Indianapolis, Indiana, 46202, United States|Johns Hopkins University, Baltimore, Maryland, 21287, United States|National Institute of Health - National Cancer Institute, Bethesda, Maryland, 20892, United States|Boston Children's Hospital / Dana Farber Cancer Institute / Massachusetts General Hospital, Boston, Massachusetts, 02115, United States|Washington University School of Medicine, St. Louis, Missouri, 63110, United States|New York University Medical Center, New York, New York, 10016, United States|Cinncinnati Children's Hospital Medical Center, Cincinnati, Ohio, 45229, United States|Nationwide Children's Hospital, Columbus, Ohio, 43205, United States|Ohio State University, Columbus, Ohio, 43210, United States|Oregon Health and Science University Hospital, Portland, Oregon, 97239, United States|Children's Hospital of Philadelphia, Philadelphia, Pennsylvania, 19096, United States|University of Utah, Salt Lake City, Utah, 84132, United States|University of Washington - Seattle Children's Hospital, Seattle, Washington, 98105, United States Less <<
NCT02285439 Low-Grade Gliomas|Malignant Ne... More >>oplasms, Brain|Soft Tissue Neoplasms Less << PHASE1|PHASE2 ACTIVE_NOT_RECRUITING 2023-11-30 Children's Hospital of Alabama... More >>, Birmingham, Alabama, 35233, United States|Children's Hospital Los Angeles, Los Angeles, California, 90027, United States|Children's Hospital of Colorado, Aurora, Colorado, 80045, United States|Children's National Heath Systems, Washington, District of Columbia, 20010, United States|Nicklaus Children's Hospital, Miami, Florida, 33155, United States|Children's Healthcare of Atlanta, Atlanta, Georgia, 30322, United States|Johns Hopkins University, Baltimore, Maryland, 21287, United States|Dana Farber Cancer Institute, Boston, Massachusetts, 02215, United States|Children's Hospitals and Clinics of Minnesota-Minneapolis, Minneapolis, Minnesota, 55404, United States|Washington University School of Medicine, Saint Louis, Missouri, 63110, United States|New York University, New York, New York, 10016, United States|Oregon Health and Science University, Portland, Oregon, 97239, United States|University of Texas Southwestern Medical, Dallas, Texas, 75390, United States|Texas Children's Hospital, Houston, Texas, 77030, United States|Seattle Children's Hospital, Seattle, Washington, 98145, United States Less <<
NCT01320085 BRAF or NRAS Mutant Metastatic... More >> Melanoma Less << PHASE2 COMPLETED 2023-02-06 Highlands Oncology Group, Faye... More >>tteville, Arkansas, 72703-4005, United States|H. Lee Moffitt Cancer Center & Research Institute, Inc., Tampa, Florida, 33612, United States|OHSU Knight Cancer Institute, Portland, Oregon, 97201, United States|OHSU Center for Health and Healing, Portland, Oregon, 97239, United States|Oregon Health and Science University, Portland, Oregon, 97239, United States|Cancer Care Associates Medical Oncology, Allentown, Pennsylvania, 18104, United States|St. Luke's Cancer Center - Allentown Campus, Allentown, Pennsylvania, 18104, United States|Cancer Care Associates Medical Oncology, Bethlehem, Pennsylvania, 18015, United States|St. Luke's University Health Network, Bethlehem, Pennsylvania, 18015, United States|St. Luke's Hospital - Quakertown Campus, Quakertown, Pennsylvania, 18951, United States|LMU Klinikum der Universit?t, Muenchen, Bayern, 80337, Germany|LMU Klinikum der Universit?t München, München, Bayern, 80337, Germany|Universit?tsklinikum Essen, Essen, Nordrhein-westfalen, 45122, Germany|Universitatsklinikum Schleswig-Holstein, Kiel, Schleswig-holstein, 24105, Germany|Universitatsklinikum Schleswig-Holstein, Kiel, Schleswig-holstein, D-24105, Germany|Universitatsklinikum Schleswig-Holstein, Luebeck, Schleswig-holstein, 23562, Germany|SRH Wald-Klinikum Gera GmbH, Gera, Thüringen, 07548, Germany|LMU Klinikum der Universit?t München, Munich, 80337, Germany|Istituto nazionale Per la Ricerca sul Cancro, Genova, 16132, Italy|Istituto Nazionale per lo studio e la cura dei tumori Fondazione Giovanni Pascale, Napoli, 80131, Italy|Radboud University Nijmegen Medical Centre, Nijmegen, Gelderland, 6525 GA, Netherlands|Maastricht University Medical Center, Maastricht, Limburg, 6229 HX, Netherlands|Het Nederlands Kanker Instituut Antoni Van Leeuwenhoek Ziekenhuis, Amsterdam, Noord-holland, 1066 CX, Netherlands|Slotervaartziekenhuis, Amsterdam, Noord-holland, 1066 EC, Netherlands|Universit?tsspital Zürich, Zürich (de), 08091, Switzerland Less <<
NCT05510895 Colorectal Cancer|Colon Cancer... More >>|BRAF V600E|BRAF V600 Mutation|Localized Cancer Less << PHASE2 RECRUITING 2025-01-31 H?matologisch-Onkologische Pra... More >>xis Eppendorf, Hamburg, 20249, Germany Less <<
NCT01556568 Cardiomegaly PHASE2 WITHDRAWN - Pfizer Investigative Site, Bos... More >>ton, Massachusetts, 02115, United States|Pfizer Investigative Site, London, W1G 8PH, United Kingdom Less <<
NCT04439344 Advanced Lymphoma|Advanced Mal... More >>ignant Solid Neoplasm|Hematopoietic and Lymphoid Cell Neoplasm|Refractory Lymphoma|Refractory Malignant Solid Neoplasm|Refractory Multiple Myeloma Less << PHASE2 ACTIVE_NOT_RECRUITING 2025-03-05 ECOG-ACRIN Cancer Research Gro... More >>up, Philadelphia, Pennsylvania, 19103, United States Less <<
NCT02050815 Hepatic Impairment PHASE1 TERMINATED 2016-08-26 DaVita Clinical Research-Denve... More >>r, Lakewood, Colorado, 80228, United States|Clinical Pharmacology of Miami (CPMI), Miami, Florida, 33014, United States|Orlando Clinical Research Center, Orlando, Florida, 32809, United States|DaVita Clinical Research, Minneapolis, Minnesota, 55404, United States|Kansas City Research Institute, LLC, Kansas City, Missouri, 64131, United States Less <<
NCT01469130 Advanced Solid Tumor PHASE1 COMPLETED 2018-02-01 Pfizer Investigative Site, Nag... More >>oya-city, Aichi, 466-8560, Japan|Pfizer Investigative Site, Yufu, Oita, 879-5593, Japan Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.27mL

0.45mL

0.23mL

11.33mL

2.27mL

1.13mL

22.66mL

4.53mL

2.27mL

References

 

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