ETC-206
This product is for research use only, not for human use. We do not sell to patients.
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| Size | Price | Stock |
|---|---|---|
| 250mg | $1200 | Check With Us |
| 500mg | $1800 | Check With Us |
| 1g | $2700 | Check With Us |
: Cat #: V20752 CAS #: 1464151-33-4 Purity ≥ 98%
Description: ETC-206 is a novel, potent and selective MNK1/2 inhibitor with IC50 of 64 nM for MNK1 and IC50 of 84 nM for MNK2.
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| Molecular Weight (MW) | 408.45 |
|---|---|
| Molecular Formula | C25H20N4O2 |
| CAS No. | 1464151-33-4 |
| SMILES Code | N#CC1=CC=C(C2=CN=C3C=CC(C4=CC=C(C(N5CCOCC5)=O)C=C4)=CN32)C=C1 |
| Synonyms | ETC-206; ETC 206; ETC206; Tinodaser |
| Protocol | In Vitro | Tinodasertib (ETC-206) inhibits eIF4E phosphorylation in HeLa cell line with an IC50 of 321 nM. The anti-proliferative effects of ETC-206 are assessed in vitro, using CellTiter-Glo viability assay against 25 hematological cancer cell lines including the K562 cell line that overexpresses eIF4E (K562 o/e eIF4E). The IC50s are 1.71 μM, 3.36 μM, 3.70 μM, 4.81 μM, 5.13 μM, 5.05 μM, 6.70 μM, 9.76 μM, and 48.8 μM for SU-DHL-6, GK-5, MC 116, P3HR-1, DOHH2, MPC-11, Ramos.2G6.4C10, AHH-1, and K562 o/e eIF4E cells, 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.)). |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.4483 mL | 12.2414 mL | 24.4828 mL | 48.9656 mL |
| 5mM | 0.4897 mL | 2.4483 mL | 4.8966 mL | 9.7931 mL |
| 10mM | 0.2448 mL | 1.2241 mL | 2.4483 mL | 4.8966 mL |
| 20mM | 0.1224 mL | 0.6121 mL | 1.2241 mL | 2.4483 mL |
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Step Two: Enter the in vivo formulation
%DMSO
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%ddH2O
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Method for preparing DMSO master liquid:
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Method for preparing in vivo formulation:
Take
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DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
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