1. MAPK/ERK Pathway
  2. Raf
  3. PLX8394

PLX8394 

Cat. No.: HY-18972 Purity: 99.94%
Handling Instructions

PLX8394 is a potent and selective Raf inhibitor, with an IC50 of appr 5 nM for BRAFV600E.

For research use only. We do not sell to patients.

PLX8394 Chemical Structure

PLX8394 Chemical Structure

CAS No. : 1393466-87-9

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 72 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 100 In-stock
Estimated Time of Arrival: December 31
50 mg USD 320 In-stock
Estimated Time of Arrival: December 31
100 mg USD 520 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Top Publications Citing Use of Products

    PLX8394 purchased from MCE. Usage Cited in: Cancer Discov. 2018 Sep;8(9):1130-1141.

    BRAF V600E or V600E/L514V are transiently transfected in SKBR3 for 24 hr. Then the cells are treated with 1 μM Lapatinib for 1 hr, followed by treatment with DMSO or the RAF inhibitors indicated for 1 hr (the dose for PLX7904 is 1 μM).

    View All Raf Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    PLX8394 is a potent and selective Raf inhibitor, with an IC50 of appr 5 nM for BRAFV600E.

    IC50 & Target[1]

    BRafV600E

    5 nM (IC50)

    In Vitro

    PLX8394 potently inhibits phosphorylation of ERK1/2 in PRT #3 and PRT #4 cells at >25 nM and in addition to parental cells at 10 nM. PLX8394 effectively reduces cyclin D3 and cyclin D1, phosphorylation of retinoblastoma protein, and expression of cyclin A2 in parental cells and PRT #3 and PRT #4 cells. PLX8394 inhibits ERK1/2 phosphorylation and the growth of vemurafenib-resistant cells harboring either a BRAF V600K/L505H double mutation or an transposon-induced, N-terminal truncated form of BRAF[1]. PLX8394 significantly impairs tumor cell growth and suppresses MAPK signaling in LA cell lines expressing either endogenous V600E or non-V600 mutant forms of BRAF[2].

    In Vivo

    PLX8394 (150 mg/kg/d) substantially suppresses tumor growth, MAPK pathway signaling and tumor cell proliferation in these H1755 xenograft tumors without overt toxicity in mice. PLX8394 combines with erlotinib yields plasma erlotinib concentrations of >1 μM[2].

    Clinical Trial
    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 39 mg/mL (71.89 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8432 mL 9.2161 mL 18.4322 mL
    5 mM 0.3686 mL 1.8432 mL 3.6864 mL
    10 mM 0.1843 mL 0.9216 mL 1.8432 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.08 mg/mL (3.83 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [1]

    For MTT assays, 2×103 cells are seeded in triplicate in 96 wells in their regular culture medium (containing PLX4720 for PRT lines). Next day, cells are washed twice with PBS and then the medium is replenished containing the indicated RAF inhibitor. Medium is changed 48 hours later and after a further 48 hours, 10 μL of 5 mg/mL MTT reagent is added to wells, and incubated for three hours. Formazan crystals are then solubilized overnight with a 1:10 dilution of 0.1 M glycine (pH 10.5) in DMSO. Wells are then analyzed at 450 nM in a Multiskan® Spectrum spectrophotometer. Results depicted are normalized to DMSO conditions and are a composite of three independent experiments. Error bars shown are representative of the standard error of mean (SEM).

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

    Animal Administration
    [2]

    H1755 tumor xenografts are generated by injection of 5×106 cells in a 50/50 mixture for matrigel and PBS into 6- to 8-wk-old female NOD/SCID mice. Mice are randomized to treatment groups once tumors reach an average size of 150 mm3. H1755 cells are s.c. implanted and allowed to grow to appr 200 mm3 (4 wk after implantation). Mice are then treated with vehicle, vemurafenib, or PLX8394 for 15 d. The vehicle for daily oral gavage is PEG 400 [20% (vol/vol)], tocopheryl polyethylene glycol succinate (TPGS) [5% (vol/vol)], water [75% (vol/vol)]. PLX8394 is dissolved in PEG 400 [20% (vol/vol)], TPGS [5% (vol/vol)], and water [75% (vol/vol)] and vortexed continuously throughout the dosing period. PLX8394 is given daily by oral gavage at a dose of 150 mg/kg/d.

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

    References
    Molecular Weight

    542.53

    Formula

    C₂₅H₂₁F₃N₆O₃S

    CAS No.

    1393466-87-9

    SMILES

    O=C(C1=C(F)C(NS(=O)(N2CC[[email protected]@H](F)C2)=O)=CC=C1F)C3=CNC4=C3C=C(C=N4)C5=CN=C(C6CC6)N=C5

    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.94%

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product name

     

    Salutation

    Applicant name *

     

    Email address *

    Phone number *

     

    Organization name *

    Country or Region *

     

    Requested quantity *

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    PLX8394
    Cat. No.:
    HY-18972
    Quantity:

    PLX8394

    Cat. No.: HY-18972