ChemicalBook > CAS DataBase List > ETC-206

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

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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

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene

Product number: CS-0046041
Product name: ETC-206
Purity: 99.76%
Packaging: 5mg
Price: $220
Updated: 2021/12/16

ChemScene

Product number: CS-0046041
Product name: ETC-206
Purity: 99.76%
Packaging: 10mg
Price: $340
Updated: 2021/12/16

Axon Medchem

Product number: Axon3340
Product name: ETC-206
Purity: 99%
Packaging: 25mg
Price: $506
Updated: 2021/12/16

ChemScene

Product number: CS-0046041
Product name: ETC-206
Purity: 99.76%
Packaging: 25mg
Price: $680
Updated: 2021/12/16

ChemScene

Product number: CS-0046041
Product name: ETC-206
Purity: 99.76%
Packaging: 50mg
Price: $980
Updated: 2021/12/16

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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 (t_1/2=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

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1464151-33-4, ETC-206Related Search:

ETC-206

ETC-1907206)

ETC-206 (ETC206

Benzonitrile, 4-[6-[4-(4-morpholinylcarbonyl)phenyl]imidazo[1,2-a]pyridin-3-yl]-

ETC-206 (AUM 001)

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

4-(6-(4-(morpholine-4-carbonyl)phenyl)imidazo[1,2-a]pyridin-3-yl)benzonitrile

Tinodasertib

ETC-206, 10 mM in DMSO

Tinodasertib (ETC-206)

ETC-206 (AUM 001) ，S6658

1464151-33-4