GW 5074
Based on 6 publication(s) in Google Scholar
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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.13%
- CAS No.: 220904-83-6
- Formule: C15H8Br2INO2
- Masse moléculaire:520.94
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
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Publications Citing Use of MedChemExpress (MCE) GW 5074
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WB
Activité biologique
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C-Raf 9 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| HeLa | IC50 |
2.5 μM
Compound: 2; GW305074X
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Inhibition of recombinant His6-tagged Kif15 ATPase activity (N420 residues) (unknown origin) expressed in HeLa cells using microtubule as substrate preincubated for 15 mins followed by ATP addition and measured after 20 mins by ADP-Glo luminescence assay
Inhibition of recombinant His6-tagged Kif15 ATPase activity (N420 residues) (unknown origin) expressed in HeLa cells using microtubule as substrate preincubated for 15 mins followed by ATP addition and measured after 20 mins by ADP-Glo luminescence assay
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[PMID: 30528696] |
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.
Chemical Information
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CAS No. 220904-83-6
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Appearance Solid
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Masse moléculaire 520.94
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Formule C15H8Br2INO2
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Color Light yellow to yellow
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SMILES
O=C1NC2=C(/C1=C/C3=CC(Br)=C(C(Br)=C3)O)C=C(C=C2)I
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (6)
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Journal Impact Factor
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Most Recent
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Carbohydr Polym
Innate immune receptors co-recognition of polysaccharides initiates multi-pathway synergistic immune response. [Abstract]2023 Apr 1:305:120533. PMID: 36737186 -
Cell Death Discov
Dual role of PID1 in regulating apoptosis induced by distinct anticancer-agents through AKT/Raf-1-dependent pathway in hepatocellular carcinoma. [Abstract]2023 Apr 28;9(1):139. PMID: 37117198 -
Oncogene
RAF1 contributes to cell proliferation and STAT3 activation in colorectal cancer independently of microsatellite and KRAS status. [Abstract]2023 May;42(20):1649-1660. PMID: 37020037 -
Sci Rep
Blocking C-Raf alleviated high-dose small-volume radiation-induced epithelial mesenchymal transition in mice lung. [Abstract]2020 Jul 7;10(1):11158. PMID: 32636458
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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Biochem J
Conservation of structure, function and inhibitor binding in UNC-51-like kinase 1 and 2 (ULK1/2). [Abstract]2019 Mar 12;476(5):875-887. PMID: 30782972 -
Ann Transl Med
Upregulated miR-155 inhibits inflammatory response induced by C. albicans in human monocytes derived dendritic cells via targeting p65 and BCL-10. [Abstract]2019 Dec;7(23):758. PMID: 32042774
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocole
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (282 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Chin PC, et al. The c-Raf inhibitor GW5074 provides neuroprotection in vitro and in an animal model of neurodegeneration through a MEK-ERK and Akt-independent mechanism. J Neurochem, 2004, 90(3), 595-608. [Content Brief]
[2]. Lei Y, et al. The Raf-1 inhibitor GW5074 and NSC 34521 suppress sidestream smoke-induced airway hyperresponsiveness in mice. Respir Res, 2008, 9(1), 71. [Content Brief]
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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