An inhibitor of MKNK1 and MKNK2
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ETC-206

Item No. 36501

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[6-[4-(4-morpholinylcarbonyl)phenyl]imidazo[1,2-a]pyridin-3-yl]-benzonitrile
CAS Number
1464151-33-4
Molecular Formula
C25H20N4O2
Formula Weight
408.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 3 mg/mlDMSO: 1 mg/mlEthanol: Slightly solublePBS (pH 7.2): 0.2 mg/ml
SMILES
N#CC1=CC=C(C2=CN=C3C=CC(C4=CC=C(C(N5CCOCC5)=O)C=C4)=CN32)C=C1
InChi Code
InChI=1S/C25H20N4O2/c26-15-18-1-3-20(4-2-18)23-16-27-24-10-9-22(17-29(23)24)19-5-7-21(8-6-19)25(30)28-11-13-31-14-12-28/h1-10,16-17H,11-14H2
InChi Key
FWRFPHJSGLYXTD-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $106

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    10 mg

    $181

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    25 mg

    $291

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    50 mg

    $526

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    Cayman Chemical
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    ETC-206 is an inhibitor of MAPK-interacting serine/threonine kinase 1 (MKNK1) and MKNK2 (IC50s = 0.064 and 0.086 µM, respectively).1 It is selective for MKNK1 and MKNK2 over a panel of 104 kinases at 1 µM. ETC-206 inhibits phosphorylation of eukaryotic translation initiation factor 4E (eIF4E) in HeLa cells (IC50 = 0.321 µM). In vivo, ETC-206 enhances tumor growth inhibition induced by dasatinib (Item No. 11498) in a K562 mouse xenograft model. It also prevents weight gain in a mouse model of high-fat diet-induced obesity when administered at a dose of 100 mg/kg.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Yang, H., Chennamaneni, L.R., Ho, M.W.T., 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. 61(10), 4348-4369 (2018).

    2. Sandeman, L.Y., Kang, W.X., Wang, X., et al. Disabling MNK protein kinases promotes oxidative metabolism and protects against diet-induced obesity. Mol. Metab. 42, 101054 (2020).