Structure of Binimetinib
CAS No.: 606143-89-9
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
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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Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
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 |
GHS Pictogram: |
![]() |
Signal Word: | Warning |
Hazard Statements: | H302-H315-H319-H335 |
Precautionary Statements: | P261-P305+P351+P338 |
Target |
|
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 << |
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 |
Tags: Binimetinib | MEK162 | ARRY-162 | ARRY-438162 | MEK 162 | MEK-162 | ARRY162 | ARRY 162 | ARRY-162 | ARRY438162 | ARRY 438162 | ARRY-438162 | MEK | Mitogen-activated protein kinase kinase | MAPKK | ERK signaling | 606143-89-9
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H229 | Pressurized container: may burst if heated |
H230 | May react explosively even in the absence of air |
H231 | May react explosively even in the absence of air at elevated pressure and/or temperature |
H240 | Heating may cause an explosion |
H241 | Heating may cause a fire or explosion |
H242 | Heating may cause a fire |
H250 | Catches fire spontaneously if exposed to air |
H251 | Self-heating; may catch fire |
H252 | Self-heating in large quantities; may catch fire |
H260 | In contact with water releases flammable gases which may ignite spontaneously |
H261 | In contact with water releases flammable gas |
H270 | May cause or intensify fire; oxidizer |
H271 | May cause fire or explosion; strong oxidizer |
H272 | May intensify fire; oxidizer |
H280 | Contains gas under pressure; may explode if heated |
H281 | Contains refrigerated gas; may cause cryogenic burns or injury |
H290 | May be corrosive to metals |
Health hazards | |
Code | Phrase |
H300 | Fatal if swallowed |
H301 | Toxic if swallowed |
H302 | Harmful if swallowed |
H303 | May be harmful if swallowed |
H304 | May be fatal if swallowed and enters airways |
H305 | May be harmful if swallowed and enters airways |
H310 | Fatal in contact with skin |
H311 | Toxic in contact with skin |
H312 | Harmful in contact with skin |
H313 | May be harmful in contact with skin |
H314 | Causes severe skin burns and eye damage |
H315 | Causes skin irritation |
H316 | Causes mild skin irritation |
H317 | May cause an allergic skin reaction |
H318 | Causes serious eye damage |
H319 | Causes serious eye irritation |
H320 | Causes eye irritation |
H330 | Fatal if inhaled |
H331 | Toxic if inhaled |
H332 | Harmful if inhaled |
H333 | May be harmful if inhaled |
H334 | May cause allergy or asthma symptoms or breathing difficulties if inhaled |
H335 | May cause respiratory irritation |
H336 | May cause drowsiness or dizziness |
H340 | May cause genetic defects |
H341 | Suspected of causing genetic defects |
H350 | May cause cancer |
H351 | Suspected of causing cancer |
H360 | May damage fertility or the unborn child |
H361 | Suspected of damaging fertility or the unborn child |
H361d | Suspected of damaging the unborn child |
H362 | May cause harm to breast-fed children |
H370 | Causes damage to organs |
H371 | May cause damage to organs |
H372 | Causes damage to organs through prolonged or repeated exposure |
H373 | May cause damage to organs through prolonged or repeated exposure |
Environmental hazards | |
Code | Phrase |
H400 | Very toxic to aquatic life |
H401 | Toxic to aquatic life |
H402 | Harmful to aquatic life |
H410 | Very toxic to aquatic life with long-lasting effects |
H411 | Toxic to aquatic life with long-lasting effects |
H412 | Harmful to aquatic life with long-lasting effects |
H413 | May cause long-lasting harmful effects to aquatic life |
H420 | Harms public health and the environment by destroying ozone in the upper atmosphere |
Sorry,this product has been discontinued.
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