ETC-206

SKU: orb1308323

Description

ETC-206 is a potent and selective small molecule inhibitor of MNK1 and MNK2 kinases, with IC50 values of 64 nM and 86 nM, respectively. It is a valuable research tool for studying MNK function in oncology and inflammation, supporting both in vitro biochemical assays and in vivo disease model studies.

Research Area

Signal Transduction

Key Properties

• CAS Number: 1464151-33-4
• MW: 408.45
• Purity: 99.72%
• Formula: C₂₅H₂₀N₄O₂
• SMILES: O=C(N1CCOCC1)c1ccc(cc1)-c1ccc2ncc(-c3ccc(cc3)C#N)n2c1
• Target: MNK
• Solubility: 10% DMSO+40% PEG300+5% Tween-80+45% Saline:5 mg/mL (12.24 mM);DMSO:55 mg/mL (134.66 mM)

Bioactivity

• Target IC50:
  MNK2:86 nM|MNK1:64 nM
• In Vivo:
  The antitumor efficacy of ETC-206 was evaluated in a K562 e/o eIF4E mouse xenograft model via oral doses of 25, 50, or 100 mg/kg, either as a standalone treatment or in combination with a consistent 2.5 mg/kg dose of Dasatinib throughout the study. Remarkably, when combined with Dasatinib, ETC-206 not only enhanced tumor growth inhibition in a dose-responsive manner but also resulted in tumor clearance in 2, 5, and 8 out of 8 mice at doses of 25, 50, and 100 mg/kg, respectively. This combination effectively suppressed tumor growth across all tested concentrations without causing weight loss in the animals. Independently, ETC-206’s maximum tumor growth inhibition (TGI) was recorded at 23% with the highest dose of 100 mg/kg, a result that was unable to significantly halt tumor progression, aligning closely with outcomes observed in untreated controls. Moreover, both the combination of ETC-206 and Dasatinib and the integration of dual MNK1/2 and BCR-ABL1 inhibitors demonstrated preventative effects on tumor development within this mouse xenograft model. Additionally, ETC-206 displayed a moderate terminal elimination half-life (t1/2=1.7 h, and 1.77 h for mouse (1 mg/kg, intravenous [i.v.]), mouse (5 mg/kg, oral [p.o.])).
• In Vitro:
  ETC-206's anti-proliferative effects were evaluated in vitro across 25 hematological cancer cell lines, including K562 cells overexpressing eIF4E (K562 o/e eIF4E), through a CellTiter-Glo viability assay. The compound efficiently inhibited eIF4E phosphorylation in the HeLa cell line, showing an IC50 of 321 nM. Its IC50 values across other cell lines, including SU-DHL-6, GK-5, MC 116, P3HR-1, DOHH2, MPC-11, Ramos.2G6.4C10, AHH-1, and K562 o/e eIF4E, ranged from 1.71 μM to 48.8 μM, demonstrating varying degrees of efficacy against these cancer cells.

Storage & Handling

• Storage: 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

ETC 206, ETC206, ETC-206, Inhibitor, MAP kinase interacting kinase, MAPK interacting kinase, inhibit, MNK, MNK1, MNK2, Mitogen activated protein kinase interacting kinase

Compound Identifiers

PubChem CID

71766360