Trametinib (DMSO solvate)

SKU: orb1301426

Description

Trametinib (DMSO solvate), also known as GSK1120212, is a highly potent and selective allosteric inhibitor of MEK1 and MEK2 kinases with an IC50 of 2 nM. It is widely used in both in vitro and in vivo cancer research, particularly for studying the MAPK/ERK pathway in melanoma, NSCLC, and other malignancies.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1187431-43-1
• MW: 693.53
• Purity: >99.99% (May vary between batches)
• Formula: C₂₈H₂₉FIN₅O₅S
• SMILES: CS(C)=O.CC(=O)Nc1cccc(c1)-n1c2c(C)c(=O)n(C)c(Nc3ccc(I)cc3F)c2c(=O)n(C2CC2)c1=O
• Target: MEK,Apoptosis
• Solubility: DMSO:1.3 mg/mL (1.87 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (1.44 mM)

Bioactivity

• Target IC50:
  MEK1/2:2 nM
• In Vivo:
  Trametinib DMSO solvate was then evaluated in vivo in an A549 (KRAS mutant cell line) xenograft model, orally dosing daily for 21 days (qd × 21).Near complete tumor growth inhibition was observed at 5.0 and 2.5 mg/kg [92 and 87% tumor growth inhibition (TGI), respectively] and to a lesser degree at 0.5 and 0.1 mg/kg (62 and 58% TGI). [Notably, although 5 mg/kg was the maximally tolerated dose (MTD) , 3 mg/kg is the typically observed MTD.] Dose-dependent antitumor activity with GSK1120212 (DMSO solvate) treatment has been similarly reported for several other KRAS and BRAF mutant tumor models.
• In Vitro:
  Trametinib DMSO solvate displays remarkable potency in cellular assays for ERK1/2 phosphorylation and growth inhibition and excellent in vivo activity. Inhibition of the MEK ERK pathway offers a very promising therapeutic strategy for cancers with activating mutant Ras and Raf, and GSK1120212 (DMSO solvate) has been advanced into phase III trials for advanced or metastatic BRAF mutant melanoma as well as phase I and II studies in subjects with solid tumors or leukemia.

Storage & Handling

• Storage: keep away from direct sunlight,keep away from moisture,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

type, Trametinib, Trametinib (DMSO solvate), Trametinib dimethyl sulfoxide, Trametinib DMSO solvate, JTP74057, JTP-74057, JTP-74057 (DMSO solvate), JTP 74057, inhibit, Mitogen-activated protein kinase kinase, orally, Inhibitor, MEK1/2, MEK, MAPKK, MAP2K, GSK 1120212, GSK1120212, GSK-1120212, GSK-1120212 (DMSO solvate), AIA, Adjuvant-induced, arthritis, Apoptosis, CIA, collageninduced, DMSO solvate

Chemical structure of Trametinib (DMSO solvate)

Compound Identifiers

PubChem CID

50992434