Trametinib, also known as GSK1120212, is a n orally bioavailable inhibitor of mitogen-activated protein kinase kinase (MEK MAPK/ERK kinase) with potential antineoplastic activity. Trametinib specifically binds to and inhibits MEK 1 and 2, resulting in an inhibition of growth factor-mediated cell signaling and cellular proliferation in various cancers. MEK 1 and 2, dual specificity threonine/tyrosine kinases often upregulated in various cancer cell types, play a key role in the activation of the RAS/RAF/MEK/ERK signaling pathway that regulates cell growth. On May 29, 2013, FDA approved T rametinib.
Chemical Formula: C26H23FIN5O4
Exact Mass: 615.07788
Molecular Weight: 615.39
Elemental Analysis: C, 50.74; H, 3.77; F, 3.09; I, 20.62; N, 11.38; O, 10.40
Appearance: white solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
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.
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.
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.
Trametinib (0.3 mg/kg, 1 mg/kg, p.o.) is effective in inhibiting the HT-29 xenograft growth in a nude mouse xenograft model.
Kasuga A, Nakagawa K, Nagashima F, Shimizu T, Naruge D, Nishina S, Kitamura H, Kurata T, Takasu A, Fujisaka Y, Okamoto W, Nishimura Y, Mukaiyama A, Matsushita H, Furuse J. A phase I/Ib study of trametinib (GSK1120212) alone and in combination with gemcitabine in Japanese patients with advanced solid tumors. Invest New Drugs. 2015 Aug 12. [Epub ahead of print] PubMed PMID: 26259955.
Giurcaneanu C, Nitipir C, Popa LG, Forsea AM, Popescu I, Bumbacea RS. Evolution of Melanocytic Nevi under Vemurafenib, Followed by Combination Therapy with Dabrafenib and Trametinib for Metastatic Melanoma. Acta Dermatovenerol Croat. 2015 Jul;23(2):87-95. Review. PubMed PMID: 26228819.
Modak S, Asante-Korang A, Steinherz LJ, Grana N. Trametinib-induced Left Ventricular Dysfunction in a Child With Relapsed Neuroblastoma. J Pediatr Hematol Oncol. 2015 Aug;37(6):e381-3. doi: 10.1097/MPH.0000000000000364. PubMed PMID: 26181424.
Schick U, Kyula J, Barker H, Patel R, Zaidi S, Gregory C, Hafsi H, Roulstone V, Deutsch E, McLaughlin M, Harrington K. Trametinib radiosensitises RAS- and BRAF-mutated melanoma by perturbing cell cycle and inducing senescence. Radiother Oncol. 2015 Jul 8. pii: S0167-8140(15)00323-0. doi: 10.1016/j.radonc.2015.06.026. [Epub ahead of print] PubMed PMID: 26163092.
Chopra N, Nathan PD. Trametinib in metastatic melanoma. Expert Rev Anticancer Ther. 2015;15(7):749-60. doi: 10.1586/14737140.2015.1060127. PubMed PMID: 26107021.
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