Structure
Trametinib, Inhibitor
Trametinib (GSK1120212)
Purity
99.71%
Synonyms
Trametinib; N/A; Trametinib (GSK1120212); Trametinib, inhibitor
Purity/Purification
99.71%
Form/Format
POWDER
Application Notes
Preparing Stock Solution: 1mg / 5mg / 10mg :
1mM : 1.625 ml / 8.1249 ml / 16.2499 ml
5mM : 0.325 ml / 1.625 ml / 3.250 ml
10mM : 0.1625 ml / 0.8125 ml / 1.625 ml
50mM : 0.0325 ml / 0.1625 ml / 0.325 ml
Please select the appropriate solvent to prepare the stock solution, according to the solubility of the product in different solvents. Please use it as soon as possible.
1mM : 1.625 ml / 8.1249 ml / 16.2499 ml
5mM : 0.325 ml / 1.625 ml / 3.250 ml
10mM : 0.1625 ml / 0.8125 ml / 1.625 ml
50mM : 0.0325 ml / 0.1625 ml / 0.325 ml
Please select the appropriate solvent to prepare the stock solution, according to the solubility of the product in different solvents. Please use it as soon as possible.
CAS Number
871700-17-3
Molecular Formula
C26H23FIN5O4
Solubility
DMSO: 7.86 mg/mL (12.77 mM),
Ethanol: < 1 mg/mL (insoluble or slightly soluble),
(< 1 mg/ml refers to the product slightly soluble or insoluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble),
(< 1 mg/ml refers to the product slightly soluble or insoluble)
Targets(IC50)
Apoptosis, Autophagy, MEK
Appearance
Solid
Analytical Data
HNMR: Consistent with structure
HPLC: Consistent with structure
HPLC: Consistent with structure
Conclusion
The test results consistent with structure
In vitro Activity
METHODS:
Mouse intrahepatic cholangiocarcinoma cells SB1, LD-1 and human intrahepatic cholangiocarcinoma cells EGI-1 were treated with Trametinib (0-10,000 nM) for 48 h, and cell growth inhibition was detected by MTT.
RESULTS:
Trametinib dose-dependently inhibited the growth of SB1, LD-1 and EGI-1 cells with IC50 of 41.48 nM, 56.10 nM and 27.89 nM, respectively. [1]
METHODS:
Human colon cancer cells RKO were treated with Trametinib (200 nmol/L) for 30 h. The expression levels of target proteins were detected by Western Blot.
RESULTS:
Trametinib significantly reduced the levels of p-ERK and p-AKT. [2]
METHODS:
Human glioma cells U87 and U251 were incubated with Trametinib (50 nM) for 6-72 h. Apoptosis was detected by Flow Cytometry.
RESULTS:
Trametinib induced a significant increase in apoptosis in U87 and U251 cells, and Trametinib induced late apoptosis but not early apoptosis in glioma cells.
Mouse intrahepatic cholangiocarcinoma cells SB1, LD-1 and human intrahepatic cholangiocarcinoma cells EGI-1 were treated with Trametinib (0-10,000 nM) for 48 h, and cell growth inhibition was detected by MTT.
RESULTS:
Trametinib dose-dependently inhibited the growth of SB1, LD-1 and EGI-1 cells with IC50 of 41.48 nM, 56.10 nM and 27.89 nM, respectively. [1]
METHODS:
Human colon cancer cells RKO were treated with Trametinib (200 nmol/L) for 30 h. The expression levels of target proteins were detected by Western Blot.
RESULTS:
Trametinib significantly reduced the levels of p-ERK and p-AKT. [2]
METHODS:
Human glioma cells U87 and U251 were incubated with Trametinib (50 nM) for 6-72 h. Apoptosis was detected by Flow Cytometry.
RESULTS:
Trametinib induced a significant increase in apoptosis in U87 and U251 cells, and Trametinib induced late apoptosis but not early apoptosis in glioma cells.
In vivo Activity
METHODS:
To detect anti-tumor activity in vivo, Trametinib (0.3-1 mg/kg) was orally administered to BALB/c-nu/nu mice bearing human colorectal cancer tumors HT-29 and COLO205 once daily for fourteen days.
RESULTS:
Trametinib treatment significantly inhibited the growth of human colorectal cancer tumors, indicating antitumor activity in vivo. [4]
METHODS:
To assay antitumor activity in vivo, Trametinib (5 mg/kg) was injected intraperitoneally three times a week for fourteen days into NSG mice bearing human B-lymphoblastic leukemia tumors KOPN8 and COLO205.
RESULTS:
Trametinib monotherapy delayed the progression of leukemia, but was not sufficient to prevent leukemia growth.
To detect anti-tumor activity in vivo, Trametinib (0.3-1 mg/kg) was orally administered to BALB/c-nu/nu mice bearing human colorectal cancer tumors HT-29 and COLO205 once daily for fourteen days.
RESULTS:
Trametinib treatment significantly inhibited the growth of human colorectal cancer tumors, indicating antitumor activity in vivo. [4]
METHODS:
To assay antitumor activity in vivo, Trametinib (5 mg/kg) was injected intraperitoneally three times a week for fourteen days into NSG mice bearing human B-lymphoblastic leukemia tumors KOPN8 and COLO205.
RESULTS:
Trametinib monotherapy delayed the progression of leukemia, but was not sufficient to prevent leukemia growth.
Kinase Assay
A Raf-MEK-ERK cascade kinase assay was carried out as previously described. Briefly, nonphosphorylated myelin basic protein (MBP) was coated onto an ELISA plate, and the active form of B-Raf/c-Raf was mixed with unphosphorylated MEK1/MEK2 and ERK2 in 10 uM ATP and 12.5 mM MgCl2 containing MOPS buffer in the presence of various concentrations of JTP-74057. The phosphorylation of MBP was detected by the anti-phosphoMBP antibody. Kinase inhibitory activities against a total of 99 kinases were tested by kinase profiler at 10 uM ATP [1].
Cell Research
These cells were maintained in media recommended by the providers. Exponentially growing cells were precultured in 96-well tissue culture plates for 24 h and then exposed to JTP-74057. Cell growth was determined by an in vitro toxicology assay kit, sulforhodamine B based. For combination studies, two compounds were simultaneously added to the HT-29 cells and incubated for 72 h. In the presence of various concentrations of compound A, the 50% inhibitory concentration (IC50) values of compound B were determined. Then, the fixed concentration of compound A versus the IC50 value of compound B was plotted. Conversely, the IC50 values of compound A were determined in the presence of various concentrations of compound B and plotted [1].
Animal Research
Female BALB/c-nu/nu mice were used. On day 0, HT-29 cells or COLO205 cells suspended in ice-cold HBSS (-) were inoculated subcutaneously into the right flank of the mice at 5x10^6 cells/100 ul/site or 1x10^6 cells/100 ul/site, respectively. The acetic acid-solvated form of JTP-74057 was dissolved in 10% Cremophor EL-10% PEG400 and was administered orally once daily for 14 days from the day when the mean tumor volume reached 100 mm^3. The tumor length [L (mm)] and width [W (mm)] were measured using a micro gauge twice a week after the commencement of dosing, and the tumor volume was calculated using the following formula: tumor volume (mm^3) = L x W x W/2. All procedures relating to the use of animals in this study were reviewed and approved by the Institutional Animal Care and Use Committee of Japan Tobacco [1].
Preparation and Storage
Powder: -20°C
In Solvent: -80°C
In Solvent: -80°C
Structure
Structure
Related Product Information for Trametinib, inhibitor
Trametinib (GSK1120212) is a MEK inhibitor that inhibits MEK1 and MEK2 (IC50=0.7/0.9 nM) with ATP non-competitive and oral activity. Trametinib activates autophagy and induces apoptosis.
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Product Notes
The Trametinib (Catalog #AAA14578) is an Inhibitor and is intended for research purposes only. The product is available for immediate purchase. Preparing Stock Solution: 1mg / 5mg / 10mg : 1mM : 1.625 ml / 8.1249 ml / 16.2499 ml 5mM : 0.325 ml / 1.625 ml / 3.250 ml 10mM : 0.1625 ml / 0.8125 ml / 1.625 ml 50mM : 0.0325 ml / 0.1625 ml / 0.325 ml Please select the appropriate solvent to prepare the stock solution, according to the solubility of the product in different solvents. Please use it as soon as possible. Researchers should empirically determine the suitability of the Trametinib for an application not listed in the data sheet. Researchers commonly develop new applications and it is an integral, important part of the investigative research process. It is sometimes possible for the material contained within the vial of "Trametinib, Inhibitor" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.Precautions
All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.Disclaimer
Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.Item has been added to Shopping Cart
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