1. MAPK/ERK Pathway
  2. Raf

LGX818 (Synonyms: Encorafenib)

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  

* Please select Quantity before adding items.

Top Publications Citing Use of Products

Featured Recommendations

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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
View MoreCollapse
References
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
[1]

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 MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
M.Wt

540.01

Formula

C₂₂H₂₇ClFN₇O₄S

CAS No.

1269440-17-6

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

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.

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number

 

Organization name *

Country *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
LGX818
Cat. No.:
HY-15605
Quantity: