ETC-206 NEW
| Price | $30 | $48 | $88 |
| Package | 2mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: ETC-206 | CAS No.: 1464151-33-4 |
| Purity: 99.79% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | ETC-206 |
| Description | ETC-206 is a selective inhibitor of MNK1 and MNK2 (IC50s: 64 nM and 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.])). |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 55 mg/mL (134.66 mM) |
| Keywords | MAP kinase interacting kinase | ETC-206 | Inhibitor | MNK | inhibit | MAPK interacting kinase | ETC 206 | ETC206 | Mitogen activated protein kinase interacting kinase |
| Inhibitors Related | SLV-2436 | EB1 | QL-X-138 | QL-X-138 HCl | MK2-IN-3 hydrate | DS12881479 | Tomivosertib | CGP 57380 | AZ7550 |
| Related Compound Libraries | Highly Selective Inhibitor Library | Reprogramming Compound Library | Bioactive Compound Library | Pain-Related Compound Library | Kinase Inhibitor Library | Anti-Obesity Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Anti-Liver Cancer Compound Library | MAPK Inhibitor Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
- Address: 36?Washington?Street, Wellesley?Hills
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