Trametinib [871700-17-3]
Cat# HY-10999-10mg
Size : 10mg
Brand : MedChemExpress
Tramétinib (GSK1120212; JTP-74057) est un inhibiteur de MEK, qui est actif par voie orale, qui inhibe MEK1 et MEK2 avec des IC50s d'environ 2 nM. Trametinib active l'autophagie et induit l'apoptose.
Trametinib (GSK1120212; JTP-74057) ist ein oral aktiver MEK-Inhibitor, der MEK1 und MEK2 mit IC50s von etwa 2 nM hemmt. Trametinib aktiviert die autophagy und induziert die apoptosis.
Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis.
For research use only. We do not sell to patients.
Trametinib Chemical Structure
CAS No. : 871700-17-3
Size | Price | Stock | Quantity |
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Free Sample (0.1 - 0.5 mg) | Apply Now | ||
Solid + Solvent | |||
10 mM * 1 mL
in DMSO
ready for reconstitution
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USD 66 | In-stock | |
Solution | |||
10 mM * 1 mL in DMSO | USD 66 | In-stock | |
Solid | |||
5 mg | USD 38 | In-stock | |
10 mg | USD 60 | In-stock | |
50 mg | USD 96 | In-stock | |
100 mg | USD 143 | In-stock | |
500 mg | USD 430 | In-stock | |
1 g | Get quote | ||
5 g | Get quote |
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Based on 171 publication(s) in Google Scholar
Other Forms of Trametinib:
- Trametinib (DMSO solvate) In-stock
- Trametinib-d4 Get quote
- Trametinib-13C6 Get quote
- Trametinib-13C,d3 Get quote
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- •Harvard Medical School LINCS LIBRARY
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Trametinib purchased from MedChemExpress. Usage Cited in: Int J Cancer. 2019 Mar 15;144(6):1379-1390. [Abstract]
- Western blot confirmed increased MAPK pathway activity in NEC-DUE2 cells when compared to NECDUE1. Treatment with PLX4032 (1 μM), GSK2118436A (100 nM), or Trametinib (100 nM) for 4 hours leads to decreased MAPK signaling in NEC-DUE2 cells. Lysates are immunoblotted for the proteins indicated.
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Trametinib purchased from MedChemExpress. Usage Cited in: Oncogenesis. 2019 Nov 4;8(11):65. [Abstract]
- Western blot analysis of p-ERK and ERK protein levels in cell lysates of H1975 treated with AMPC, Trametinib for 24 h. The levels of the total ERK was used as an input control.
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Trametinib purchased from MedChemExpress. Usage Cited in: J Cell Sci. 2019 May 31;132(11):jcs224071. [Abstract]
- Western blots of phosphorylated active ERK1/2 (pERK) and total ERK1/2 (ERK) for MDA MB 231 Sel2 and MDA MB 435 Sel1 populations following treatment with DMSO vehicle, 0.5 μM Trametinib or 10 μM U0126 for 18 h.
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Trametinib purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2018 Mar;8(3):354-369. [Abstract]
- MEK inhibitor Trametinib (GSK1120212) achieves target inhibition at 3mg/kg.
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Trametinib purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Western blot analysis of selected MAPK and AKT/mTOR pathway components in Trametinib- and CCI-779-treated cells.
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Trametinib purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Sep 5;37(1):218. [Abstract]
- WB for ERRα, IDH3A, c-Myc and Cyclin D1 in the HCT116 and SW480 cells treated with the indicated concentrations of Trametinib (0-100 nM) or DMSO for 48 h.
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Trametinib purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2018 Oct 9;115(41):E9570-E9579. [Abstract]
- presentative Western blots used to measure the efficiencies of kinase inhibitors in reducing ERK1/2 phosphorylation in control, ERK1/2 inhibitor (FR180204 and SCH772984; 10 μM)-treated or MEK1/2 inhibitor (GSK1120212; 10 μM)-treated ARPE-19 and H1299 cells.
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Trametinib purchased from MedChemExpress. Usage Cited in: Eur J Cancer. 2018 Aug;99:37-48. [Abstract]
- Western blot detection of cleaved PARP in H358, SW480 and HCT-116 cell lines treated with BMS-354825 (100 nM), Trametinib (400 nM) or combination for 48 h. DMSO is used as the treatment control.
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Trametinib purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2018 Jan 8;495(2):1846-1850. [Abstract]
- Western blot analysis of phosphorylated ERK2, and ERK2 in microvesicle-depleted fraction (15 μg of protein) derived from viruses obtained from 10 nM Trametinib-treated CEM/LAV-1 cells.
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Trametinib purchased from MedChemExpress. Usage Cited in: Patent. US20180161326A1.
- Trametinib (100 nM) and PLX4032 (10 μM) in combination have little effect on PARP-1 cleavage in A375 and UACC-62 cells, but significant PARP-1 cleavage and reduction in procaspase-3 level are observed via Western blot with the addition of PAC-1 (12 μM).
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Trametinib purchased from MedChemExpress. Usage Cited in: Patent. US20180169102A1.
- The presence or absence of the pERK protein are measured through western blotting using the brain hemispheres of trametinib-administered 5×FAD mice.
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Trametinib purchased from MedChemExpress. Usage Cited in: Sci Rep. 2017 Mar 28;7:45332. [Abstract]
- Trametinib, a MEK1/2 inhibitor, strongly inhibits growth and partially reverses GW786034 resistance of GW786034-resistant clones.Trametinib-induced inhibition of phosphorylation of ERK1/2 in SS clones is assessed by Western blot analysis with anti-ERK1/2 and anti-phospho-ERK1/2 antibodies. SS clones are pre-treated using 10 nMtrametinib for 2 hours.
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Trametinib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Feb 28;8(9):14835-14846. [Abstract]
- MEK inhibition results in reduced ERK phosphorylation.A. Western blot analysis of SEM and KOPN8 exposed to 500 nM of MEK inhibitor or vehicle control (DMSO) for 6, 24 and 48 hours. Both cell lines almost completely lose ERK phosphorylation (p-ERK), while total ERK (t-ERK) levels remain unaffected. B. Analysis of MEK phosphorylation (p-MEK) suggests exposure to MEK162 and Selumetinib results in enhanced MEK phosphorylation in both cell lines, whereas total MEK (t-MEK) levels remain constant.
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Trametinib purchased from MedChemExpress. Usage Cited in: Stem Cell Reports. 2016 Jan 12;6(1):74-84. [Abstract]
- Western blot of SKPs treated with varying concentrations of Trametinib (MEKi) or DMSO (Control) for 30 min, probed for pERK1/2 and reprobed for total ERK1/2.
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Trametinib purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2016 Aug;15(8):1859-69. [Abstract]
- Addition of PAC-1 to the combination of PLX4032+Trametinib powerfully synergizes to induce apoptotic death and caspase activity in A375 and UACC-62 cells. Trametinib (100 nM) and PLX4032 (10 μM) in combination have little effect on PARP-1 cleavage in A375 and UACC-62 cells, but significant PARP-1 cleavage and reduction in procaspase-3 level are observed via Western blot with the addition of PAC-1 (12 μM).
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Trametinib purchased from MedChemExpress. Usage Cited in: J Cell Biochem. 2016 Jun;117(6):1340-51. [Abstract]
- HeLa S3 cells that are arrested at the G2/M border by RO-3306 treatment are washed free of RO-3306 and incubated with 10 μM GSK1120212.
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Trametinib purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2015 Sep;5(9):960-71. [Abstract]
- The MEK inhibitor Trametinib effectively inhibits ERK phosphorylation at 30 nM in several EGFR mutant cell lines but has little effect on cell viability.
•Related Screening Libraries:
•Related Small Molecules:
•Related Proteins:
View All MEK Isoform Specific Products:
Biological Activity
Protocol
Purity & Documentation
References
Customer Review
Description | |||||||||||||
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IC50 & Target[1] |
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In Vitro |
Trametinib (GSK1120212;JTP-74057) (0.1-100 nM) blocks tumor necrosis factor-α and interleukin-6 production from peripheral blood mononuclear cells (PBMCs). Trametinib (JTP-74057) inhibits the growth of 9 out of 10 human colorectal cancer cell lines, and they shows cell-cycle arrest at the G1 phase after drug tratment[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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In Vivo |
Adjuvant-induced arthritis (AIA) and type II collageninduced arthritis (CIA) development are suppressed almost completely by 0.1 mg/kg of Trametinib (GSK1120212; JTP-74057) or 10 mg/kg of HWA486[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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Clinical Trial |
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Molecular Weight |
615.39 |
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Formula |
C26H23FIN5O4 |
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CAS No. | |||||||||||||
Appearance |
Solid |
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Color |
White to off-white |
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SMILES |
CC(NC1=CC=CC(N(C2=O)C(C(C(N2C3CC3)=O)=C(N4C)NC5=CC=C(C=C5F)I)=C(C4=O)C)=C1)=O |
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Shipping | Room temperature in continental US; may vary elsewhere. |
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Storage |
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Solvent & Solubility |
In Vitro:
DMSO : 25 mg/mL (40.62 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
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.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 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:
For the following dissolution methods, please prepare the working solution directly.
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage mg/kgAnimal weight Dosing volume Number of animals Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Calculation results:
Working solution concentration:
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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
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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.
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Purity & Documentation | |||||||||||||
References |
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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 |
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DMSO | 1 mM | 1.6250 mL | 8.1249 mL | 16.2499 mL | 40.6246 mL |
5 mM | 0.3250 mL | 1.6250 mL | 3.2500 mL | 8.1249 mL | |
10 mM | 0.1625 mL | 0.8125 mL | 1.6250 mL | 4.0625 mL | |
15 mM | 0.1083 mL | 0.5417 mL | 1.0833 mL | 2.7083 mL | |
20 mM | 0.0812 mL | 0.4062 mL | 0.8125 mL | 2.0312 mL | |
25 mM | 0.0650 mL | 0.3250 mL | 0.6500 mL | 1.6250 mL | |
30 mM | 0.0542 mL | 0.2708 mL | 0.5417 mL | 1.3542 mL | |
40 mM | 0.0406 mL | 0.2031 mL | 0.4062 mL | 1.0156 mL |
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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.
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Inquiry Information
- Product Name:
- Trametinib
- Cat. No.:
- HY-10999
- Quantity:
- MCE Japan Authorized Agent: