Trametinib gsk1120212

Manufactured by Selleck Chemicals

Sourced in Germany, Italy, Switzerland

Trametinib (GSK1120212) is a selective inhibitor of mitogen-activated protein kinase kinase (MEK) 1 and MEK2. It is a laboratory reagent intended for research use only.

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Trametinib (439 citations) GSK1120212 (51 citations) Trametinib (GSK1120212-S2673) (3 citations)

16 protocols using trametinib gsk1120212

Cell Culture and Treatment with Targeted Therapies

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LIM1215, HCA7 and HEK-293T cell lines were cultured in DMEM/F-12 + L-Glutamine + 15 mM HEPES (Gibco) supplemented with 10% fetal bovine serum (FBS) (HyClone) and 1% penicillin/streptomycin (Gibco) at 37°C with 5% CO₂. LIM1215 cells were obtained from the Ludwig Institute for Cancer Research, New York, NY, USA and HCA7 and HEK-293T cells were obtained from the American Type Culture Collection (ATCC).
Cetuximab (Erbitux^®) was purchased from Merck Serono, lapatinib (Tykerb/Tyverb^®) from GlaxoSmithKline, and trastuzumab (Herceptin^®) and pertuzumab (Perjeta^®) from Roche. Gefitinib (ZD1839), GDC-0941, trametinib (GSK1120212) and afatinib (BIBW2992) were purchased from Selleck Chemicals. NRG1 was purchased from Peprotech.

Bosch-Vilaró A., Jacobs B., Pomella V., Asbagh L.A., Kirkland R., Michel J., Singh S., Liu X., Kim P., Weitsman G., Barber P.R., Vojnovic B., Ng T, & Tejpar S. (2016). Feedback activation of HER3 attenuates response to EGFR inhibitors in colon cancer cells. Oncotarget, 8(3), 4277-4288.

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Inhibition of ALK4/5/7, MEK1/2 Pathways

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ALK4/5/7 inhibitor LY‐364947 (Calbiochem; #616451) from Merck Millipore (Darmstadt, Germany), MEK1/2 inhibitor Trametinib (GSK1120212; #S2673) from Selleckchem (Bio‐Connect, Huissen, The Netherlands) and ammonium sulfate (#A‐2939) from Sigma–Aldrich (Zwijndrecht, The Netherlands) were used as previously described (Kunnen et al., 2017).

Kunnen S.J., Malas T.B., Semeins C.M., Bakker A.D, & Peters D.J. (2017). Comprehensive transcriptome analysis of fluid shear stress altered gene expression in renal epithelial cells. Journal of Cellular Physiology, 233(4), 3615-3628.

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Inhibiting Cell Signaling Cascades

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Trametinib (GSK1120212) (Catalog No.S2673), AZD6244 (Selumetinib) (Catalog No.S1008), perifosine (KRX-0401) (Catalog No.S1037), wortmannin (KY12420) (Catalog No.S2758), and Ro-3306 (Catalog No. S7747) were purchased from Selleckchem. Thymidine powder (T1895) was purchased from Sigma.

Singh K., Han C., Fleming J.L., Becker A.P., McElroy J., Cui T., Johnson B., Kumar A., Sebastian E., Showalter C.A., Schrock M.S., Summers M.K., Becker V., Tong Z.Y., Meng X., Manring H.R., Venere M., Bell E.H., Robe P.A., Grosu A.L., Haque S.J, & Chakravarti A. (2023). TRIB1 confers therapeutic resistance in GBM cells by activating the ERK and Akt pathways. Scientific Reports, 13, 12424.

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Phosphorylation of HER3 in Cancer Cells

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To induce the phosphorylation of HER3, the cells were stimulated with HRG-β1 (R&D Systems, Milan, Italy), at the concentration of 10 ng/ml for the indicated times. The anti-HER3 antibody patritumab was kindly provided from Daiichi Sankyo (Tokyo, Japan) was used at the concentration of 10 μg/ml. The chemotherapeutic drugs 5-FU and Ox were purchased from Teva Italia (Assago, Mi) and used at the concentration of 50 and 20 μM, respectively. The anti-MEK inhibitor trametinib (GSK-1120212) (Selleckchem, Milan, Italy) was used at the concentration of 5 nM. The treatment were performed at the indicated times.

Bon G., Loria R., Amoreo C.A., Verdina A., Sperduti I., Mastrofrancesco A., Soddu S., Diodoro M.G., Mottolese M., Todaro M., Stassi G., Milella M., De Maria R, & Falcioni R. (2016). Dual targeting of HER3 and MEK may overcome HER3-dependent drug-resistance of colon cancers. Oncotarget, 8(65), 108463-108479.

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Modulating MHC-I Expression in Melanoma

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The BRAF(V600E)-specific inhibitor (BRAFi) dabrafenib GSK2118436 and MEK inhibitor (MEKi) trametinib GSK1120212 (Selleckchem) were used in these studies to inhibit MAPK pathway activation. Melanoma cell lines were seeded at 1.0 × 10⁶ cells in a 12-well plate and cultured in the presence of BRAFi (50nM), MEKi (50nM), or DMSO (solvent control) for different time points. This concentration was chosen because it effectively blocked the MAPK pathway without inducing rapid cell death or toxicity (Suppl. Figs. 1 and 4). Surface MHC-I expression was quantified by staining cells with anti-human HLA A,B,C-APC (W6/32) or anti-human HLA-A2-APC (BB7.2, Biolegend) and measuring fluorescence using a FACScanto II flow cytometer (BD Biosciences). Data were further analyzed using Flowjo analysis software (Treestar).

Bradley S.D., Chen Z., Melendez B., Talukder A., Khalili J.S., Rodriguez-Cruz T., Liu S., Whittington M., Deng W., Li F., Bernatchez C., Radvanyi L.G., Davies M.A., Hwu P, & Lizée G. (2015). BRAF(V600E) co-opts a conserved MHC class I internalization pathway to diminish antigen presentation and CD8+ T-cell recognition of melanoma. Cancer immunology research, 3(6), 602-609.

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Pharmacological Inhibition of Oncogenic Signaling

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Pharmacological inhibitors to MEK1/2 (Trametinib/GSK1120212, MEKi), HDAC (Panobinostat/LBH589, HDACi) and WEE1 (Adavosertib/MK-1775, WEE1i) were acquired from Selleckchem; to MEK5-K2 (BIX02189, MEK5i) was purchased from Tocris. Lestaurtinib/L6307 (mtPKCi), Neratinib (pan-HERi) and Afatinib (EGFRi) were obtained from LC Laboratories, and Midostaurin/PKC412 (mtPKCi), Sotorasib/AMG-510 (KRASi), Darovasertib (PKCAi), Barasertib (AURKBi), Adagrasib/MRTX849 (KRASi) and MG132 (proteasome inhibitor) were purchased from MedChemExpress. Dabrafenib (RAFi) was a kind gift from Imanol Arozarena (Navarrabiomed, Spain).

Macaya I., Roman M., Welch C., Entrialgo-Cadierno R., Salmon M., Santos A., Feliu I., Kovalski J., Lopez I., Rodriguez-Remirez M., Palomino-Echeverria S., Lonfgren S.M., Ferrero M., Calabuig S., Ludwig I.A., Lara-Astiaso D., Jantus-Lewintre E., Guruceaga E., Narayanan S., Ponz-Sarvise M., Pineda-Lucena A., Lecanda F., Ruggero D., Khatri P., Santamaria E., Fernandez-Irigoyen J., Ferrer I., Paz-Ares L., Drosten M., Barbacid M., Gil-Bazo I, & Vicent S. (2023). Signature-driven repurposing of Midostaurin for combination with MEK1/2 and KRASG12C inhibitors in lung cancer. Nature Communications, 14, 6332.

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Human GC Cell Line Cultivation and Drug Treatment

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Human GC cell lines (N87, OE19) were obtained from the American Type Culture Collection (ATCC). All cell lines were cultured in RPMI1640 medium (Life Technologies) with 10% FBS (Life Technologies), penicillin (100 U/mL; Life Technologies), and streptomycin (100 U/mL; Life Technologies). All cells were maintained in a humidified incubator with 5% CO₂ at 37 °C. Drug treatment reagents lapatinib, trastuzumab, LY294002, saracatinib (AZD0530), rapamycin, trametinib (GSK1120212) and copanlisib (BAY 80–6946), 5- FU were purchased from Selleckchem.

Ning G., Zhu Q., Kang W., Lee H., Maher L., Suh Y.S., Michaud M., Silva M., Kwon J.Y., Zhang C, & Lee C. (2021). A novel treatment strategy for lapatinib resistance in a subset of HER2-amplified gastric cancer. BMC Cancer, 21, 923.

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Assessing Kinase Inhibitor Combination

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CC214-1 and CC214-2 were provided by Celgene Corporation (San Diego, U.S.A.) (Mortensen et al., 2013 (link)). Lapatinib ditosylate (GW-572016), trametinib (GSK1120212), XL-765 (SAR245409), U0126, erlotinib and dasatinib were obtained from Selleckchem.

Wei W., Shin Y.S., Xue M., Matsutani T., Masui K., Yang H., Ikegami S., Gu Y., Ken H., Johnson D., Ding X., Hwang K., Kim J., Zhou J., Su Y., Li X., Bonetti B., Chopra R., James C.D., Cavenee W.K., Cloughesy T.F., Mischel P.S., Heath J.R, & Gini B. (2016). Single cell phosphoproteomics resolves adaptive signaling dynamics and informs targeted combination therapy in glioblastoma. Cancer cell, 29(4), 563-573.

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Cytoskeletal Dynamics and Cellular Signaling

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Anti–VE-cadherin (F-8) was from Santa Cruz Biotechnology. Anti-CD31 (89C2) was from Cell Signaling Technologies. 4′,6-Diamidino-2-phenylindole (DAPI), rhodamine phalloidin (1 mg/ml), Alexa Fluor 647 phalloidin (1 mg/ml), and Alexa Fluor–conjugated secondary antibodies were from Life Technologies. For antibody concentrations, see the “Immunofluorescence” and “Western blot and small GTPase activity assays” sections below. Rapamycin, alpelisib (BYL719), Y-27362 2HCl, trametinib (GSK1120212), batimastat (BB-94), EHT1864 2HCl, and PF-3758309 were from Selleckchem.

Aw W.Y., Cho C., Wang H., Cooper A.H., Doherty E.L., Rocco D., Huang S.A., Kubik S., Whitworth C.P., Armstrong R., Hickey A.J., Griffith B., Kutys M.L., Blatt J, & Polacheck W.J. (2023). Microphysiological model of PIK3CA-driven vascular malformations reveals a role of dysregulated Rac1 and mTORC1/2 in lesion formation. Science Advances, 9(7), eade8939.

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Comprehensive Molecular Profiling Protocol

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Trametinib (GSK1120212) (#S2673), PLX4720 (#S1152), PLX4032 (#S1267), PLX8394 (#S7965), AZD5991 (#S8643), MK2206 (#S1078), buparlisib (BKM120) (#S2247), and Navitoclax (#S1001) were purchased from Selleck Chemicals, LLC. DRP-1 (#8570S), BAK (#12105S), Bcl-XL (2762S), Caspase 9 (#9502S), Cleaved caspase 3 (#9661S), HSP90 (#4877S), pERK1/2 (#9101S), pRb S807/811 (#9308S), pT308 AKT (#2965S), pPRAS40 T246 (#2640S), VCAM1 (#13662S), Mcl-1 (#4572S), LAMP-1 (#9091T), Vinculin (#4650S), Tubulin (#2148S), COX-IV (#11967S), cytochrome c (#11940S) cleaved PARP (#9541) and GAPDH (#2118S) antibodies were purchased from Cell Signaling Technology. ERK2 (sc-1647) and AIF (#sc-13116) were purchased from Santa Cruz Biotechnology Inc., γH2AX (ab11174) was purchased from Abcam, Actin (A2066) was purchased from Sigma-Aldrich Co., and Bcl-2 (#51-6511GR) was purchased from BD Biosciences. Goat anti-rabbit IgG Alexa Fluor^TM 488 secondary antibody was purchased from Invitrogen.

Cavallo M.R., Yo J.C., Gallant K.C., Cunanan C.J., Amirfallah A., Daniali M., Sanders A.B., Aplin A.E., Pribitkin E.A, & Hartsough E.J. (2024). Mcl-1 mediates intrinsic resistance to RAF inhibitors in mutant BRAF papillary thyroid carcinoma. Cell Death Discovery, 10, 175.

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