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Chemical Structure| 934660-93-2 Chemical Structure| 934660-93-2
Chemical Structure| 934660-93-2

Cobimetinib

CAS No.: 934660-93-2

Cobimetinib (GDC-0973, RG7420) is a potent, selective, oral MEK1 inhibitor with an IC50 of 4.2 nM for MEK1.

Synonyms: XL518; GDC-0973; RG-7420

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Cat. No.: A181766 Purity: 98%

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Product Details of Cobimetinib

CAS No. :934660-93-2
Formula : C21H21F3IN3O2
M.W : 531.31
SMILES Code : O=C(C1=CC=C(F)C(F)=C1NC2=CC=C(I)C=C2F)N3CC([C@H]4NCCCC4)(O)C3
Synonyms :
XL518; GDC-0973; RG-7420
MDL No. :MFCD22124461

Safety of Cobimetinib

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

Related Pathways of Cobimetinib

MAPK

Isoform Comparison

Biological Activity

Target
  • MEK1

    MEK1, IC50:4.2 nM

In Vitro:

Cell Line
Concentration Treated Time Description Reference
MD-MSC 0.3–1 µM 24 hours Cobimetinib reduced pERK levels in MD-MSCs and induced caspase-3 cleavage after 24 hours, indicating it induced apoptosis. PMC6422635
MD-HSC 0.3–1 µM 72 hours Cobimetinib reduced pERK levels in MD-HSCs and induced caspase-3 cleavage after 72 hours, indicating it induced apoptosis. PMC6422635
MCF10A cells 1uM 48 hours MEK inhibition restores MHC I and MHC II expression PMC8492503
B cells 1 nM, 10 nM, 100 nM 24 hours To evaluate the inhibitory effect of Cobimetinib on B cell activation, results showed that Cobimetinib significantly reduced the MFI of CD69. PMC9830178
Monocytes 1 nM, 10 nM, 100 nM 4 hours To evaluate the inhibitory effect of Cobimetinib on TNF-α production by monocytes, results showed that Cobimetinib significantly suppressed TNF-α production. PMC9830178
KP4×1.1 cells 0.9 µM Inhibition of KP4×1.1 cell migration PMC4380185

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description Reference
Mice Allograft model Oral 50 mg/kg/day Twice per day for two weeks Cobimetinib significantly reduced the median tumor weight and decreased pERK, Ki-67, and cyclin D1 levels, indicating its inhibitory effect on tumor growth. PMC6422635
Mice CT26 colorectal cancer model Intraperitoneal injection 1 × 10^11 viral particles Single injection, lasting 15 weeks Cobimetinib treatment significantly reduced tumor burden but did not significantly alter CD8+ T cell infiltration PMC8492503
Mice Pulmonary GVHD model Oral 5 mg/kg once daily for 45 days To evaluate the inhibitory effect of Cobimetinib on pulmonary GVHD in mice, results showed that Cobimetinib significantly improved survival rates and attenuated bronchiolitis and perivascular inflammation. PMC9830178
SCID mice Melanoma xenograft model Subcutaneous injection 5 mg/kg Single dose, 24 hours To investigate the effect of miR-211 on melanoma xenograft model, results showed that miR-211 expression significantly increased tumor growth and weight. PMC9004592

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT05125471 Arteriovenous Malformations (E... More >>xtracranial) Less << PHASE2 RECRUITING 2025-12-26 Arkansas Children's Hospital, ... More >>Little Rock, Arkansas, 72202, United States Less <<
NCT04079179 Langerhan's Cell Histiocytosis... More >>|Juvenile Xanthogranuloma|Erdheim-Chester Disease|Rosai Dorfman Disease|Neuro-Degenerative Disease|Histiocytic Sarcoma|Histiocytic Disorders, Malignant Less << PHASE2 RECRUITING 2025-12-29 Phoenix Children's Hospital, P... More >>hoenix, Arizona, 85016, United States|Arkansas Children's Hospital, Little Rock, Arkansas, 72202, United States|Children's Hospital of Orange County, Orange, California, 92868, United States|Children's National Hospital, Washington, District of Columbia, 20010, United States|John Hopkins University School of Medicine, Baltimore, Maryland, 21287, United States|Dana Farber Cancer Institute, Boston Children's, Boston, Massachusetts, 02215, United States|Memorial Sloan Kettering Cancer Center, New York, New York, 10065, United States|NACHO Consortium, Memphis, Tennessee, 38105, United States|Children's Medical Center- UTSW, Dallas, Texas, 75235, United States|Texas Children's Hospital, Houston, Texas, 77030, United States|University of Wisconsin-American Family Children's Hospital, Madison, Wisconsin, 53792, United States Less <<
NCT01711762 Healthy Volunteer PHASE1 COMPLETED 2025-09-12 Madison, Wisconsin, 53704, Uni... More >>ted States Less <<
NCT02639546 Solid Tumors PHASE1|PHASE2 COMPLETED 2021-07-21 Arkansas Children'S Hospital, ... More >>Little Rock, Arkansas, 72202, United States|Arnold Palmer Hosp-Children, Orlando, Florida, 32806, United States|Dana Farber Cancer Institute, Boston, Massachusetts, 02215, United States|Memorial Sloan Kettering Cancer Center, New York, New York, 10065, United States|University of Texas Health Science Center at San Antonio, San Antonio, Texas, 78229, United States|H?pital de la Timone, Oncologie Pédiatrique, Marseille, 13385, France|Institut Curie, Oncologie Pédiatrique, Paris, 75231, France|Institut Gustave Roussy; Service Pediatrique, Villejuif, 94805, France|Universitaetsklinikum Muenster, Muenster, 48149, Germany|Schneider Children's Medical Center, Petach-Tikva, 49100, Israel|Fondazione IRCCS Istituto Nazionale dei Tumori; Struttura Complessa di Pediatria Oncologica, Milano, Lombardia, 20133, Italy|Hospital Universitari Vall d'Hebron, Barcelona, 08035, Spain|Hospital Infantil Universitario Nino Jesus, Madrid, 28009, Spain|Hospital Universitari i Politecnic La Fe de Valencia, Valencia, 46026, Spain|Alderhey Childrens Trust, Liverpool, L12 2AP, United Kingdom|Great Ormond Street Hospital; Dept. Of Pediatric Oncology, London, WC1N 3JH, United Kingdom|The Royal Victoria Infirmary; Paediatric and Adolescent Oncology Unit, Newcastle Upon Tyne, NE1 4LP, United Kingdom Less <<
NCT02649972 Histiocytic Disorders PHASE2 COMPLETED 2022-12-16 Mayo Clinic, Rochester, Minnes... More >>ota, 55905, United States|Memorial Sloan Kettering Cancer Center, New York, New York, 10065, United States Less <<
NCT04409639 Chronic Myelomonocytic Leukemi... More >>a (CMML) Less << PHASE2 RECRUITING 2026-08-15 Oregon Health and Science Univ... More >>ersity, Portland, Oregon, 97239, United States|Huntsman Cancer Institute at University of Utah, Salt Lake City, Utah, 84112, United States|Fred Hutchinson Cancer Research Center, Seattle, Washington, 98109, United States Less <<
NCT01249131 Healthy Volunteers PHASE1 COMPLETED 2011-01-10 -

Protocol

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Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.88mL

0.38mL

0.19mL

9.41mL

1.88mL

0.94mL

18.82mL

3.76mL

1.88mL

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