Encorafenib (LGX818)
For research use only.
Catalog No.S7108
14 publications
CAS No. 1269440-17-6
Encorafenib (LGX818) is a highly potent RAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing B-RAF(V600E) with EC50 of 4 nM. Phase 3.
2 Customer Reviews
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Whole cell lysates from NRAS- or BRAF-mutant melanoma cells treated with encorafenib or/and binimetinib or DMSO as a control for 24 h were subjected to Western blot analysis to detect pERK, ERK and β-Actin. Experiment shown is a representative of three independent experiments.
Clin Cancer Res, 2017, 23(20):6203-6214. Encorafenib (LGX818) purchased from Selleck.
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(E) A375 and G361 cells were transfected with GFP-mRFP-LC3 for 24 h, then they were treated the same as in (D) for 4 and 24 h. Images were taken with a confocal microscope.
Cancer Lett, 2016, 370(2):332-44.. Encorafenib (LGX818) purchased from Selleck.
Purity & Quality Control
Choose Selective Raf Inhibitors
Biological Activity
| Description | Encorafenib (LGX818) is a highly potent RAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing B-RAF(V600E) with EC50 of 4 nM. Phase 3. | |||||||||||||||||||||||
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| Features | Orally bioavailable RAF-selective inhibitor. | |||||||||||||||||||||||
| Targets |
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| In vitro |
In the A375 (BRAFV600E) human melanoma cell line LGX818 suppresses phospho-ERK (EC50 = 3 nM) leading to potent inhibition of proliferation (EC50 = 4 nM). No significant activity is observed against a panel of 100 kinases (IC50 > 900 nM) and LGX818 does not inhibit proliferation of > 400 cell lines expressing wild-type BRAF. Contributing to the high potency of LGX818 is the extremely slow off-rate from BRAFV600E which is not observed with other RAF inhibitors. In biochemical assays the dissociation half-life is >24 hours which translated into sustained target inhibition in cells following drug wash-out. [1] |
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| Cell Data |
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| Assay |
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| In vivo | LGX818 treatment at oral doses as low as 6 mg/kg resulted in strong (75%) and sustained (>24 hours) decrease in phospho-MEK, even following clearance of drug from circulation in single dose PK/PD studies in human melanoma xenograft models (BRAFV600E). LGX818 induces tumor regression in multiple BRAF mutant human tumor xenograft models grown in immune compromised mice and rats at doses as low as 1 mg/kg. Consistent with the in vitro data, LGX818 is inactive against BRAF wild-type tumors at doses up to 300 mg/kg bid, with good tolerability and linear increase in exposure. Efficacy is also achieved in a more disease-relevant spontaneous metastatic melanoma and a model of melanoma brain metastasis. LGX818 is a potent and selective RAF kinase inhibitor with unique biochemical properties that contribute to an excellent pharmacological profile. [1] |
Protocol
Solubility (25°C)
| In vitro | DMSO | 100 mg/mL (185.18 mM) |
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| Ethanol | 100 mg/mL (185.18 mM) | |
| Water | Insoluble |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 540.01 |
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| Formula | C22 H27 Cl F N7 O4 S |
| CAS No. | 1269440-17-6 |
| Storage |
powder in solvent |
| Synonyms | N/A |
| Smiles | CC(C)N1C=C(C(=N1)C2=C(C(=CC(=C2)Cl)NS(=O)(=O)C)F)C3=NC(=NC=C3)NCC(C)NC(=O)OC |
In vivo Formulation Calculator (Clear solution)
| Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment) | ||||||||||
| Dosage | mg/kg |  |
Average weight of animals | g | |
Dosing volume per animal | ul | |
Number of animals | |
| Step 2: Enter the in vivo formulation () | ||||||||||
| % DMSO % % Tween 80 % ddH2O | ||||||||||
| CalculateReset | ||||||||||
Calculation results:
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
Bio Calculators
Molarity Calculator
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).
Dilution Calculator
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Molarity Calculator
Clinical Trial Information
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
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| NCT02834364 | Active not recruiting | Drug: Encorafenib|Drug: Binimetinib | Relapsed or Refractory Multiple Myeloma|Patients With BRAFV600 E or BRAFV600K Mutation | University of Heidelberg Medical Center|Array BioPharma|German Cancer Research Center|Coordinating Centre for Clinical Trials Heidelberg|University Hospital Heidelberg | June 2016 | Phase 2 |
| NCT02278133 | Completed | Drug: WNT974|Drug: LGX818|Biological: Cetuximab | Metastatic Colorectal Cancer | Array BioPharma | December 2014 | Phase 1|Phase 2 |
| NCT01909453 | Active not recruiting | Drug: LGX818|Drug: MEK162|Drug: vemurafenib | Melanoma | Pfizer | September 12 2013 | Phase 3 |
| NCT01543698 | Active not recruiting | Drug: LGX818|Drug: MEK162|Drug: LEE011 | Solid Tumors Harboring a BRAF V600 Mutation | Pfizer | May 30 2012 | Phase 1|Phase 2 |
| NCT01436656 | Active not recruiting | Drug: LGX818 | Melanoma and Metastatic Colorectal Cancer | Pfizer | September 5 2011 | Phase 1 |
Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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