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ETC-206

Catalog No. T15250 CAS 1464151-33-4

ETC-206 is a selective inhibitor of MNK1 and MNK2 (IC50s: 64 nM and 86 nM).

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ETC-206, CAS 1464151-33-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 34.00
2 mg	In stock	$ 48.00
5 mg	In stock	$ 80.00
10 mg	In stock	$ 147.00
25 mg	In stock	$ 253.00
50 mg	In stock	$ 397.00
100 mg	In stock	$ 589.00
500 mg	In stock	$ 1,280.00
1 mL * 10 mM (in DMSO)	In stock	$ 89.00

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Purity: 99.7%

Purity: 98.11%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	ETC-206 is a selective inhibitor of MNK1 and MNK2 (IC50s: 64 nM and 86 nM).
Targets&IC50	MNK1:64 nM, MNK2:86 nM
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.
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.])).

Molecular Weight	408.45
Formula	C25H20N4O2
CAS No.	1464151-33-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (122.41 mM)

References and Literature

1. Yang H, et al. Optimization of Selective Mitogen-Activated Protein Kinase Interacting Kinases 1 and 2 Inhibitors for the Treatment of Blast Crisis Leukemia. J Med Chem. 2018 May 24;61(10):4348-4369.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Highly Selective Inhibitor Library Target-Focused Phenotypic Screening Library Bioactive Compounds Library Max MAPK Inhibitor Library Anti-Prostate Cancer Compound Library Kinase Inhibitor Library Anti-Obesity Compound Library Anti-Liver Cancer Compound Library Reprogramming Compound Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

ETC-206 1464151-33-4 MAPK MNK MAP kinase interacting kinase Inhibitor inhibit MAPK interacting kinase ETC 206 ETC206 Mitogen activated protein kinase interacting kinase inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.