2. MAPK/ERK Pathway Apoptosis
  3. Raf Apoptosis
  4. GW 5074

GW 5074 est un inhibiteur de c-Raf qui est puissant et sélectif avec IC50 de 9 nM, et n'a aucun effet sur les activités de JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 ou c-Fms.

GW 5074 is a potent and selective c-Raf inhibitor with IC50 of 9 nM, and has no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms.

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

GW 5074 Chemical Structure

GW 5074 Chemical Structure

CAS No. : 220904-83-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 84 In-stock
Solution
10 mM * 1 mL in DMSO USD 84 In-stock
Solid
1 mg USD 29 In-stock
5 mg USD 73 In-stock
10 mg USD 119 In-stock
50 mg USD 218 In-stock
100 mg USD 262 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of GW 5074:

GW 5074 Related Antibodies

Top Publications Citing Use of Products

    GW 5074 purchased from MedChemExpress. Usage Cited in: Sci Rep. 2020 Jul 7;10(1):11158.  [Abstract]

    The inhibitory efficiency of GW5074 is evaluated by Western blots with the p–C-Raf expression level in MLE-12 cells. 100 nM GW5074 dramatically reduces the phosphorylation form of C-Raf.

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    BRaf c-Raf Raf

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    GW 5074 is a potent and selective c-Raf inhibitor with IC50 of 9 nM, and has no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms[1][2].

    IC50 & Target[1]

    c-Raf

    9 nM (IC50)

    In Vitro

    GW5074 is a potent and specific inhibitor of c-Raf with IC50 of 9 nM and has no effect of MKK6, MKK7, p38 MAP kinase and cdks in vitro. However, treatment of neuronal cultures with GW5074 permits accumulation of activating modifications on c-Raf and also B-Raf. The inhibition of LK-induced apoptosis by GW5074 in cerebellar granule neurons is not MEK-ERK-dependent. GW5074 delays down-regulation of Akt activity but inhibits apoptosis by an Akt-independent mechanism. GW5074 affects Ras, nuclear factor-kappa B and c-jun. GW5074 inhibits cell death caused by neurotoxins in granule cells and other neuronal types[1].

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

    GW 5074 Related Antibodies
    In Vivo

    GW5074 (5 mg/Kg) completely prevents extensive bilateral striatal lesions induced by 3-NP in mice[1]. GW5074 suppresses sidestream smoke-induced airway hyperresponsiveness in mice[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Molecular Weight

    520.94

    Formula

    C15H8Br2INO2
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C1NC2=C(/C1=C/C3=CC(Br)=C(C(Br)=C3)O)C=C(C=C2)I
    Shipping

    Room temperature in continental US; may vary elsewhere.
    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 : 100 mg/mL (191.96 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9196 mL 9.5980 mL 19.1961 mL
    5 mM 0.3839 mL 1.9196 mL 3.8392 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    V1

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    C2

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    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

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

      Solubility: ≥ 2.5 mg/mL (4.80 mM); Suspended solution

      This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.49%

    COA (252 KB)

    Handling Instructions (2659 KB)
    References
    Kinase Assay
    [1]

    Briefly, for each assay 5-10 mU of purified kinase is used. For GSK3β, cdk1, cdk2, cdk3, cdk5, the kinase is incubated with 1 μM GW5074 in a buffer containing 8 mM MOPS, pH 7.2, 0.2 mM EDTA, 10 mM magnesium acetate and [c-33P-ATP] for 40 min at room temperature. Kinase activity is quantified by measuring 33P incorporation by spotting an aliquot on P30 filters, washing in 50 mM phosphoric acid and scintillation counting. The buffer composition for c-Raf, JNK1, JNK2, JNK3, MEK1, MKK6, MKK7 is 50 mM Tris pH 7.5, 0.1 mM EGTA, 10 mM magnesium acetate and [c-33P-ATP]. The peptide substrates used are as follows: For c-Raf, 0.66 mg/mL MBP; for cdks, 0.1 mg/mL histone H1; for JNKs, 3 μM ATF2; for MEK1, 1 μM MAPK2; for MKK6, 1 μM of SAPK2a and for MKK7, 2 μM JNK1α.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Cell Assay
    [1]

    Befiy, the tetrazolium salt MTT is added to the cultures at a final concentration of 1 mg/mL, and incubation of the culture is continued in the CO2 incubator for a Hirther 30 min at 37°C. The assay is stopped by adding lysis buffer [20% sodium dodecyi sulfate (SDS) in 50% N,N-dimethyl formamide, pH 4.7], The absorbance is measured spectrophotometrically at 570 nm after an ovemight incubation at room temperature. The absorbance of a well without cells is used as background and subtracted. Data are presented as mean±standard deviation. Statistical analysis is perfomied using ANOVA and Student-Neuman-Keuls' test. Besides MTT assays, viability is also quantitied using the tluorescein-diacetate method and by DAPI staining (which reveals apoptotic nuclei as condensed or fragmented). The results using these assays are similar to those obtained with the MTT assay.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    The Tru-Scan® activity monitoring system is used to assess locomotor activity on mice on the day following the 5 days of injection with saline, 3-NP or a combination of 3-NP and GW5074 (7 animals in each group). The animal is placed in a Perspex arena (25.9×25.9 cm) witb infrared beams spaced at 0.6-inch intervals in the X-Y plane. The arena is also equipped with a second infrared beam system at the Z plane positioned 2.54 cm above the X-Y plane. In this system the movement of the animal is accurately assessed by interruptions in 17×17-grid system created by the infrared beams in both the X-Y and Z planes. The animal is allowed to remain in the arena for 15 min, with data collection performed during this period using the Tru Scan Line interface box and Tm Scan 99 software, operating through a Pentium PC. The following behavioral parameters are selected: (i) Total movements episodes: each movement in the flor plane is a series of coordinate changes with no rest for at least I sample interval; (ii) total movement distance: the sum of all vectored A-Y coordinate changes in the floor plane; (iii) mean velocity: the mean velocity of all X-Y coordinate change defined movements; and (iv) vertical plane entries: the total number of times any part of the animal entered the vertical plane (Z plane).

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

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9196 mL 9.5980 mL 19.1961 mL 47.9902 mL
    5 mM 0.3839 mL 1.9196 mL 3.8392 mL 9.5980 mL
    10 mM 0.1920 mL 0.9598 mL 1.9196 mL 4.7990 mL
    15 mM 0.1280 mL 0.6399 mL 1.2797 mL 3.1993 mL
    20 mM 0.0960 mL 0.4799 mL 0.9598 mL 2.3995 mL
    25 mM 0.0768 mL 0.3839 mL 0.7678 mL 1.9196 mL
    30 mM 0.0640 mL 0.3199 mL 0.6399 mL 1.5997 mL
    40 mM 0.0480 mL 0.2400 mL 0.4799 mL 1.1998 mL
    50 mM 0.0384 mL 0.1920 mL 0.3839 mL 0.9598 mL
    60 mM 0.0320 mL 0.1600 mL 0.3199 mL 0.7998 mL
    80 mM 0.0240 mL 0.1200 mL 0.2400 mL 0.5999 mL
    100 mM 0.0192 mL 0.0960 mL 0.1920 mL 0.4799 mL
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    GW 5074 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    GW 5074220904-83-6GW5074GW-5074RafApoptosisRaf kinasesInhibitorinhibitorinhibit

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