Trametinib [871700-17-3]

Catalog number: HY-10999_100mg
Brand: MedChem Express
Packing: 100 mg
Other sizes: 10 mg
10 mM
50 mg
Price: € 177.00
Expected delivery time: 10 days
Quantity:
Trametinib Chemical Structure
CAS No. : 871700-17-3...

Product specifications for - Trametinib [871700-17-3]

Overview: 
Product group: Chemicals
Category: Other
CAS No.: 871700-17-3
Properties: 
Purity: >98%
Molecular Formula: C26H23FIN5O4
Molecular weight: 615.39
Datasheet: Datasheet
  Research Use Only
UNSPSC: 12352200
Scientific information: 
Scientific info: Trametinib is a potent MEK1/2 inhibitor that specifically inhibits MEK1/2, with an IC90 value of about 2 nM. IC50 & Target: IC50: 2 nM (MEK1/2)[1]In Vitro: Trametinib (0.1-100 nM) blocks tumor necrosis factor-alpha 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-cyclearrest at the G1 phase after drug tratment[1]. The combination of GSK2118436 and Trametinib (GSK1120212) effectively inhibits cell growth, decreases ERK phosphorylation, decreases cyclin D1 protein, and increases p27(kip1) protein in the resistant clones[2].In Vivo: Adjuvant-induced arthritis (AIA) and type II collageninduced arthritis (CIA) development are suppressed almost completely by 0.1 mg/kg of JTP-74057 or 10 mg/kg of Leflunomide. In the CIA, JTP-74057 suppresses collagen-reactive T-cell proliferation ex vivo[1]. Trametinib (0.3 mg/kg, 1 mg/kg, p.o.) effective in inhibiting the HT-29 xenograft growth in a nude mouse xenograft model[2].
Safety information: 
MSDS: MSDS
Additional information: 
Synonyms: HY-10999; GSK1120212; JTP-74057
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Liu H, Murphy CJ, Karreth FA, et al. Identifying and Targeting Sporadic Oncogenic Genetic Aberrations in Mouse Models of Triple-Negative Breast Cancer. Cancer Discov. 2018;8(3):354-369. Read more
Ercan D, Xu C, Yanagita M, et al. Reactivation of ERK signaling causes resistance to EGFR kinase inhibitors. Cancer Discov. 2012;2(10):934-47. Read more
Liu H, Paddock MN, Wang H, et al. The INPP4B Tumor Suppressor Modulates EGFR Trafficking and Promotes Triple-Negative Breast Cancer. Cancer Discov. 2020; Read more
Tricker EM, Xu C, Uddin S, et al. Combined EGFR/MEK Inhibition Prevents the Emergence of Resistance in EGFR-Mutant Lung Cancer. Cancer Discov. 2015;5(9):960-971. Read more
Zheng ZY, Anurag M, Lei JT, et al. Neurofibromin Is an Estrogen Receptor-α Transcriptional Co-repressor in Breast Cancer. Cancer Cell. 2020;37(3):387-402.e7. Read more