1. MAPK/ERK Pathway
  2. Raf

LGX818 (Synonyms: Encorafenib)

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

LGX818 is a highly potent RAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAFV600E (EC50=4 nM).

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 USD 143 In-stock
Estimated Time of Arrival: December 31
1 mg USD 80 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 190 In-stock
Estimated Time of Arrival: December 31
25 mg USD 290 In-stock
Estimated Time of Arrival: December 31
50 mg USD 450 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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    LGX818 purchased from MCE. Usage Cited in: Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093.

    Western blot analysis of selected MAPK and AKT/mTOR pathway components in Trametinib- and Temsirolimus-treated cells.

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    Description

    LGX818 is a highly potent RAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAFV600E (EC50=4 nM).

    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
    Solvent & Solubility
    In Vitro: 

    10 mM in DMSO

    Preparing
    Stock Solutions
    Concentration Solvent 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
    *Please refer to the solubility information to select the appropriate solvent.
    References
    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]

    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
    Molecular Weight

    540.01

    Formula

    C₂₂H₂₇ClFN₇O₄S

    CAS No.

    1269440-17-6

    SMILES

    O=C(OC)N[[email protected]@H](C)CNC1=NC=CC(C2=CN(C(C)C)N=C2C3=CC(Cl)=CC(NS(=O)(C)=O)=C3F)=N1

    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

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

    Cat. No.: HY-15605