ETC-206
- Product Name
- ETC-206
- CAS No.
- 1464151-33-4
- Chemical Name
- ETC-206
- Synonyms
- ETC-206;Tinodasertib;ETC-1907206);ETC-206 (ETC206;ETC-206 (AUM 001);Tinodasertib (ETC-206);ETC-206, 10 mM in DMSO;ETC-206 (AUM 001) ，S6658;4-(6-(4-(morpholine-4-carbonyl)phenyl)imidazo[1,2-a]pyridin-3-yl)benzonitrile;Benzonitrile, 4-[6-[4-(4-morpholinylcarbonyl)phenyl]imidazo[1,2-a]pyridin-3-yl]-
- CBNumber
- CB33370680
- Molecular Formula
- C25H20N4O2
- Formula Weight
- 408.45
- MOL File
- 1464151-33-4.mol
ETC-206 Property
- storage temp.
- Store at -20°C
- solubility
- DMSO:66.0(Max Conc. mg/mL);161.58(Max Conc. mM)
- form
- A solid
- color
- Light yellow to yellow
N-Bromosuccinimide Price
- Product number
- CS-0046041
- Product name
- ETC-206
- Purity
- 99.76%
- Packaging
- 5mg
- Price
- $220
- Updated
- 2021/12/16
- Product number
- CS-0046041
- Product name
- ETC-206
- Purity
- 99.76%
- Packaging
- 10mg
- Price
- $340
- Updated
- 2021/12/16
- Product number
- Axon3340
- Product name
- ETC-206
- Purity
- 99%
- Packaging
- 25mg
- Price
- $506
- Updated
- 2021/12/16
- Product number
- CS-0046041
- Product name
- ETC-206
- Purity
- 99.76%
- Packaging
- 25mg
- Price
- $680
- Updated
- 2021/12/16
- Product number
- CS-0046041
- Product name
- ETC-206
- Purity
- 99.76%
- Packaging
- 50mg
- Price
- $980
- Updated
- 2021/12/16
ETC-206 Chemical Properties,Usage,Production
Uses
Tinodasertib (ETC-206) is a selective MNK1 and MNK2 inhibitor with IC50s of 64 nM and 86 nM, respectively.
in vivo
The antitumor effect of ETC-206 is then assessed in a K562 e/o eIF4E mouse xenograft model after oral administration at 25, 50, or 100 mg/kg alone or in combination with a 2.5 mg/kg fixed dose of Dasatinib throughout the study. Dasatinib at 2.5 mg/kg elicits a tumor growth inhibition (TGI) of 88% with one tumor-free animal. In contrast, ETC-206 alone only yields a maximum TGI of 23% at the highest administered dose of 100 mg/kg, which does not impede tumor growth, and is similar to the nontreated animals. ETC-206 with 2.5 mg/kg of Dasatinib not only increases tumor growth inhibition in a dose-dependent manner but, more importantly leads to 2, 5, and 8 out of 8 tumor-free animals at 25, 50, and 100 mg/kg, respectively. The combination of ETC-206 and Dasatinib inhibits tumor growth at all tested doses, and no weight loss is recorded. Both the combination of ETC-206 and Dasatinib and, on the other hand, the dual MNK1/2 and BCR-ABL1 inhibitors prevent tumor growth in the same mouse xenograft model. ETC-206 has moderate terminal elimination half-life (t1/2=1.7 h, and 1.77 h for mouse (1 mg/kg, i.v.), mouse (5 mg/kg, p.o.))[1].
IC 50
MNK1: 64 nM (IC50); MNK2: 86 nM (IC50)
References
[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. DOI:10.1021/acs.jmedchem.7b01714
ETC-206 Preparation Products And Raw materials
Raw materials
Preparation Products
ETC-206 Suppliers
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- United States
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