1. MAPK/ERK Pathway
  2. Raf

LGX818 (Synonyms: Encorafenib; LGX 818; LGX-818)

Cat. No.: HY-15605 Purity: 99.88%
Data Sheet SDS Handling Instructions

LGX818 is an orally available mutated BRafV600E inhibitor (IC50=0.3 nM) with potential antineoplastic activity.

For research use only. We do not sell to patients.
LGX818 Chemical Structure

LGX818 Chemical Structure

CAS No. : 1269440-17-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO $428 In-stock
1 mg $105 In-stock
5 mg $360 In-stock
10 mg $550 In-stock
50 mg   Get quote  
100 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References


LGX818 is an orally available mutated BRafV600E inhibitor (IC50=0.3 nM) with potential antineoplastic activity.

IC50 & Target

IC50: 0.3 nM (BRafV600E)

In Vitro

LGX818 is a potent drug that can prevents diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of B-Raf[1]. LGX818 (10 nM) suppresses the ERK/MAPK pathway and displays marked inhibition of pERK in A375, G361 and SK-MEL-24 cells. 10 nM LGX818 treatment for 12 days potently inhibits colony formation in A375, G361 and SK-MEL-24 cells, but not in RPMI7951 and C8161 cells. LGX818 treatment induces a steady increase in the β-catenin level in G361 cells over time[2].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT02834364 University of Heidelberg Medical Center|Array BioPharma|German Cancer Research Center|Coordinating Centre for Clinical Trials Heidelberg|University Hospital Heidelberg Relapsed or Refractory Multiple Myeloma|Patients With BRAFV600 E or BRAFV600K Mutation June 2016 Phase 2
NCT02928224 Array BioPharma|Merck KGaA|Pierre Fabre Medicament BRAF V600E-mutant Metastatic Colorectal Cancer August 2016 Phase 3
NCT02902042 Prof. Dr. med. Dirk Schadendorf|University Hospital, Essen Malignant Melanoma December 2016 Phase 1|Phase 2
NCT01981187 Array BioPharma Solid Tumor|Hematologic Malignancies January 2014 Phase 2
NCT01820364 Array BioPharma Melanoma November 2013 Phase 2
NCT02109653 Array BioPharma Non-Small Cell Lung Cancer June 2015 Phase 2
NCT01894672 Memorial Sloan Kettering Cancer Center|Array BioPharma Melanoma July 2013 Phase 2
NCT02263898 Jonsson Comprehensive Cancer Center|National Cancer Institute (NCI) Recurrent Melanoma|Stage IV Melanoma January 2015 Phase 2
NCT02278133 Array BioPharma Metastatic Colorectal Cancer December 2014 Phase 1|Phase 2
NCT01777776 Array BioPharma Locally Advanced Metastatic BRAF Mutant Melanoma July 2013 Phase 1|Phase 2
NCT01436656 Array BioPharma Melanoma and Metastatic Colorectal Cancer September 2011 Phase 1
NCT01719380 Array BioPharma Colorectal Cancer November 2012 Phase 1|Phase 2
NCT01909453 Array BioPharma Melanoma September 2013 Phase 3
NCT01543698 Array BioPharma Solid Tumors Harboring a BRAF V600 Mutation May 2012 Phase 1|Phase 2
NCT02159066 Array BioPharma Melanoma July 2014 Phase 2
NCT02631447 Fondazione Melanoma Onlus|Clinical Research Technology S.r.l. Metastatic Melanoma November 2016 Phase 2
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Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 1.8518 mL 9.2591 mL 18.5182 mL
5 mM 0.3704 mL 1.8518 mL 3.7036 mL
10 mM 0.1852 mL 0.9259 mL 1.8518 mL
Kinase Assay

The Raf kinase activity reaction is started by the addition of 10 μL per well of 2×ATP diluted in assay buffer. After 3 hours (bRaf(V600E)) or 1 hour (c-Raf), the reactions are stopped with the addition of 10 μL of stop reagent (60 mM EDTA). Phosphorylated product is measured using a rabbit anti-p-MEK antibody and the Alpha Screen IgG (ProteinA) detection Kit, by the addition of 30 μL to the well of a mixture of the antibody (1:2000 dilution) and detection beads (1:2000 dilution of both beads) in bead buffer (50 mM Tris, pH 7.5, 0.01% Tween20). The additions are carried out under dark conditions to protect the detection beads from light. A lid is placed on top of the plate and incubated for 1 hour at room temperature, then the luminescence is read on a PerkinElmer Envision instrument. The concentration of each compound for 50% inhibition (IC50) is calculated by non-linear regression using XL Fit data analysis software

Cell Assay

LGX818 is dissolved in DMSO.

A375 is a melanoma cell line that harbors the B-Raf V600E mutation. A375-luc cells engineered to express luciferase is plated to 384-well white clear bottom plates as 1,500 cells/50 μL/well in DMEM containing 10% FBS. Test compounds, dissolved in 100% DMSO at appropriate concentrations, are transferred to the cells by a robotic Pin Tool (100 mL). The cells are incubated for 2 days at 25°C, then 25 μL of BrightGloTM is added to each well and the plates are read by luminescence. The concentration of each compound for 50% inhibition (IC50) is calculated by non-linear regression using XL Fit data analysis software. wild type and V600E B-Raf.







Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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