Name: Trametinib (GSK1120212)
Price: 188.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    Trametinib (also known as GSK1120212 or JTP 74057), originally identified as a p15 inductive compound, is a novel and potent allosteric inhibitor of MEK kinase, which exhibits ATP non-competitive inhibition against MEK1 and MEK2 kinase. It has demonstrated broad antitumor activities in a variety of tumor xgenograft models, including HT-29 and COLO205 colorectal tumor cell lines. Trametinib induces expression of p15 and p27, reduces cyclin D1 levels, and causes dephosphorylation of RB protein and G1-phase arrest with a reduction of TS expression in HT-29 cells. It also effectively inhibits p-ERK 1/2 resulting in cell growth inhibition in tumor cell lines harboring B-RAF mutant.
- Properties
  - Alternative Name
    
    Trametinib, GSK-1120212, GSK1120212, Mekinist, JTP74057, JTP-74057; N-[3-[3-cyclopropyl-5-(2-fluoro-4-iodoanilino)-6,8-dimethyl-2,4,7-trioxopyrido[4,3-d]pyrimidin-1-yl]phenyl]acetamide
    
    CAS Number
    
    871700-17-3
    
    Molecular Formula
    
    C26H23FIN5O4
    
    Molecular Weight
    
    615.39
    
    Appearance
    
    A solid
    
    Purity
    
    99.44%
    
    Solubility
    
    insoluble in H2O; insoluble in EtOH; ≥15.38 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Wendy S. Chen, Yan Liang, et al. "Single-cell transcriptomics reveals opposing roles of Shp2 in Myc-driven liver tumor cells and microenvironment." Cell Rep. 2021 Nov 9;37(6):109974. PMID:34758313
    2. Gabriele Manzella, Leonie D. Schreck, et al. "Phenotypic profiling with a living biobank of primary rhabdomyosarcoma unravels disease heterogeneity and AKT sensitivity." Nature Communications volume 11, Article number: 4629 (2020). PMID:32934208
    3. Xu WF, Wang ZJ, et al. "Huai Qi Huang-induced Apoptosis via Down-regulating PRKCH and Inhibiting RAF/MEK/ERK Pathway in Ph+ Leukemia Cells." Curr Med Sci. 2020;40(2):354-362. PMID:32337697
    4. Ruibin Bai, Yajie Zhang, et al. "Isolation, characterization and immunomodulatory activity of oligosaccharides from Codonopsis pilosula." Journal of Functional Foods. Volume 72, September 2020, 104070
    5. Day EK, Sosale NG, et al. "Glioblastoma Cell Resistance to EGFR and MET Inhibition Can Be Overcome via Blockade of FGFR-SPRY2 Bypass Signaling." Cell Rep. 2020;30(10):3383-3396.e7. PMID:32160544
    6. Park SM, Hwang CY, et al. "Feedback analysis identifies a combination target for overcoming adaptive resistance to targeted cancer therapy." Oncogene. 2020;39(19):3803-3820. PMID:32157217
    7. Challa S, Husain K, et al. "Targeting the IκB Kinase Enhancer and Its Feedback Circuit in Pancreatic Cancer." Transl Oncol. 2020;13(2):481–489. PMID:32004866
    8. Satoh TK, Mellett M, et al. "IL-36γ drives skin toxicity induced by EGFR/MEK inhibition and commensal Cutibacterium acnes." J Clin Invest. 2019 Dec 5. pii: 128678. PMID:31805013
    9. Roche SL, Kutsyr O, et al. "Norgestrel, a Progesterone Analogue, Promotes Significant Long-Term Neuroprotection of Cone Photoreceptors in a Mouse Model of Retinal Disease." Invest Ophthalmol Vis Sci. 2019 Jul 1;60(8):3221-3235. PMID:31335948
    10. Juliane Buhl. "The senescence-associated secretory phenotype regulates the growth behavior of pediatric pilocytic astrocytoma." Ruperto Carola University Heidelberg. 2018.
    11. Cho SY, Chae J, et al. "Unstable Genome and Transcriptome Dynamics during Tumor Metastasis Contribute to Therapeutic Heterogeneity in Colorectal Cancers." Clin Cancer Res. 2019 Jan 22. PMID:30670495
    12. Buhl JL, Selt F, et al. "The senescence-associated secretory phenotype mediates oncogene-induced senescence in pediatric pilocytic astrocytoma." Clin Cancer Res. 2018 Dec 7. pii: clincanres.1965.2018. PMID:30530705
    13. Knickelbein K, Tong J, et al."Restoring PUMA induction overcomes KRAS-mediated resistance to anti-EGFR antibodies in colorectal cancer." Oncogene. 2018 May 14. PMID:29755130
    14. Wang YN, Lee HH, et al. "Angiogenin/Ribonuclease 5 Is an EGFR Ligand and a Serum Biomarker for Erlotinib Sensitivity in Pancreatic Cancer." Cancer Cell. 2018 Apr 9;33(4):752-769.e8. PMID:29606349
    15. Sieber J, Wieder N, et al. "GDC-0879, a BRAF(V600E) Inhibitor, Protects Kidney Podocytes from Death." Cell Chem Biol. 2017 Dec 6. PMID:29249695
    16. Hogstad B, Berres ML, et al. "RAF/MEK/extracellular signal-related kinase pathway suppresses dendritic cell migration and traps dendritic cells in Langerhans cell histiocytosis lesions." J Exp Med. 2018 Jan 2;215(1):319-336. PMID:29263218
    17. Yong LK, Lai S, et al. "Overexpression of Semaphorin-3E enhances pancreatic cancer cell growth and associates with poor patient survival." Oncotarget. 2016 Dec 27;7(52):87431-87448. PMID:27911862