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Chemical Structure| 1269440-17-6 Chemical Structure| 1269440-17-6

Structure of Encorafenib
CAS No.: 1269440-17-6

Chemical Structure| 1269440-17-6

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Encorafenib is a potent and selective B-RafV600E inhibitor, with no significant activity observed against a panel of 100 kinases (IC50>900nM).

Synonyms: LGX818

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Product Details of Encorafenib

CAS No. :1269440-17-6
Formula : C22H27ClFN7O4S
M.W : 540.01
SMILES Code : O=C(OC)N[C@@H](C)CNC1=NC=CC(C2=CN(C(C)C)N=C2C3=CC(Cl)=CC(NS(=O)(C)=O)=C3F)=N1
Synonyms :
LGX818
MDL No. :MFCD25976758
InChI Key :CMJCXYNUCSMDBY-ZDUSSCGKSA-N
Pubchem ID :50922675

Safety of Encorafenib

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

Related Pathways of Encorafenib

MAPK

Isoform Comparison

Biological Activity

Target
  • B-Raf

In Vitro:

Cell Line
Concentration Treated Time Description References
BRAFV600E colorectal cancer cell lines 100 nM 72 hours To investigate the effect of Encorafenib alone and in combination with a BCL-XL inhibitor (A-1331852) on apoptosis, results showed that the combination significantly enhanced apoptosis. PMC10907349
MDCKII-ABCB1 cells 25.1 µM 60 minutes To evaluate the inhibitory effect of Encorafenib on the ABCB1 transporter, the results showed that Encorafenib could moderately increase the accumulation of daunorubicin in MDCKII-ABCB1 cells. PMC9785850
MDCKII-ABCG2 cells >20 µM 60 minutes To evaluate the inhibitory effect of Encorafenib on the ABCG2 transporter, the results showed that Encorafenib did not significantly affect the efflux of mitoxantrone within the tested concentration range. PMC9785850
MDCKII-ABCC1 cells 8.63 µM 60 minutes To evaluate the inhibitory effect of Encorafenib on the ABCC1 transporter, the results showed that even at low concentrations, Encorafenib could significantly increase the accumulation of daunorubicin in MDCKII-ABCC1 cells. PMC9785850

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NOD Scid gamma mice COLO 201 xenograft model Oral gavage 20 mg/kg bi-daily, for 22 days To investigate the effect of Encorafenib in combination with the BCL-2/BCL-XL inhibitor AZD0466 on tumor growth, results showed that the combination significantly suppressed tumor growth. PMC10907349

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01436656 Melanoma and Metastatic Colore... More >>ctal Cancer Less << PHASE1 COMPLETED 2022-11-07 H Lee Moffitt Cancer Center an... More >>d Research Institute, Tampa, Florida, 33612, United States|Massachusetts General Hospital, Boston, Massachusetts, 02114, United States|Brigham and Women's Hospital, Boston, Massachusetts, 02115, United States|Beth Israel Deaconess Medical Center, Boston, Massachusetts, 02215, United States|Dana-Farber Cancer Institute, Boston, Massachusetts, 02215, United States|Western Sydney Local Health District, Westmead, New South Wales, 2145, Australia|Westmead Hospital- Redbank Rd, Westmead, New South Wales, 2145, Australia|Peter MacCallum Cancer Centre, East Melbourne, Victoria, 3002, Australia|EDOG - Institut Claudius Regaud - PPDS, Toulouse, Haute-garonne, 31059 Cedex 9, France|Institut Gustave Roussy, Villejuif, ILE DE France - VAL DE Marne (94), 94800, France|Institut Gustave Roussy, Villejuif, VAL DE Marne, 94800, France|Institut Gustave Roussy, Villejuif Cedex, Val-de-marne, 94805, France|Institut Gustave Roussy, Villejuif, Val-de-marne, 94805, France|Institut Gustave Roussy, Villejuif, 94805, France|National Cancer Center Hospital, Chuo-ku, Tokyo, 104-0045, Japan|Oslo Myeloma Center - PPDS, Oslo, 00424, Norway|Hospital Clinic de Barcelona, Badalona, 08036, Spain|Hospital General Vall d'Hebron, Barcelona, 08035, Spain|Hospital Universitario Vall d'Hebron - PPDS, Barcelona, 08035, Spain|Hospital Universitario Vall d'Hebron, Barcelona, 08035, Spain|Hospital Universitario Vall d'Hebron - PPDS, Barcelona, 8035, Spain|Hospital Universitario HM Sanchinarro_CIOCC, Madrid, 28050, Spain|START MADRID_Hospital Universitario HM Sanchinarro - CIOCC, Madrid, 28050, Spain|Kantonsspital Graubünden, Chur, Graubünden (DE), 07000, Switzerland|Universit?t Zürich, Zürich, 8091, Switzerland Less <<
NCT01894672 Melanoma PHASE2 COMPLETED 2016-03-17 Memorial Sloan Kettering Cance... More >>r Center at Basking Ridge, Basking Ridge, New Jersey, United States|Memorial Sloan Kettering Cancer Center at Commack, Commack, New York, 11725, United States|Memorial Sloan Kettering Cancer Center, New York, New York, 10065, United States|Memorial Sloan Kettering Cancer Center at Mercy Medical Center, Rockville Centre, New York, 11570, United States|Memorial Sloan Kettering Cancer Center at Phelps Memorial Hospital Center, Sleepy Hollow, New York, 10591, United States Less <<
NCT02109653 Non-Small Cell Lung Cancer PHASE2 WITHDRAWN 2025-11-17 University of Chicago Medical ... More >>Center SC-2, Chicago, Illinois, 60546, United States Less <<
NCT01981187 Solid Tumor|Hematologic Malign... More >>ancies Less << PHASE2 TERMINATED 2015-10-13 Alabama Oncology St. Vincent's... More >> Birmingham, Birmingham, Alabama, 35211, United States|Highlands Oncology Group Highlands Oncology Group (22), Fayetteville, Arkansas, 72703, United States|Yale University School of Medicine Smilow Cancer Hospital, New Haven, Connecticut, 06520, United States|Whittingham Cancer Center Norwalk Hospital, Norwalk, Connecticut, 06856, United States|Florida Cancer Specialists Florida Cancer Specialists (31, Fort Myers, Florida, 33901, United States|Lurie Children's Hospital of Chicago Developmental Therapeutics, Chicago, Illinois, 60611, United States|Comprehensive Cancer Centers of Nevada CCC of Nevada (1), Las Vegas, Nevada, 89109, United States|Genesis Cancer Services, Zanesville, Ohio, 43701, United States|University of Pennsylvania Presbyterian Medical Center University of Pennsylvania, Philadelphia, Pennsylvania, 19104, United States|Sanford Research Sanford Health, Sioux Falls, South Dakota, 57104, United States|Oncology Consultants Oncology Group, Houston, Texas, 77024, United States|Utah Cancer Specialists Utah Cancer Specialists (11), Salt Lake City, Utah, 84106, United States|Shenandoah Oncology Shenadoah Oncology (2), Winchester, Virginia, 22601, United States Less <<
NCT05003622 BRAF V600E Unresectable or Met... More >>astatic Melanoma|BRAF V600E Metastatic NSCLC|Melanoma Less << PHASE1 COMPLETED 2022-05-06 Sun Yat-sen University Cancer ... More >>Center, Guangzhou, Guangdong, 510060, China Less <<
NCT01820364 Melanoma PHASE2 TERMINATED 2025-03-15 Sarah Cannon Research Institut... More >>e Onc Dept, Nashville, Tennessee, 37203, United States|Novartis Investigative Site, East Melbourne, Victoria, 3002, Australia|Novartis Investigative Site, Edmonton, Alberta, T6G 1Z2, Canada|Novartis Investigative Site, Heidelberg, 69120, Germany|Novartis Investigative Site, Barcelona, Catalunya, 08035, Spain|Novartis Investigative Site, Zuerich, 8091, Switzerland Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.85mL

0.37mL

0.19mL

9.26mL

1.85mL

0.93mL

18.52mL

3.70mL

1.85mL

References

 

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