CDK8-IN-16
CDK8-IN-16 (Compound 51) is an orally active dual inhibitor for CDK8 and CDK19 wih IC50 of 5.1 nM and 5.6 nM. CDK8-IN-16 inhibits the phospho-STAT1SER727 with an IC50 of 17.9 nM in SW620 cell, inhibits WNT signaling pathway with an IC50 of 7.2 nM in 7dF3 cell. CDK8-IN-16 exhibits good pharmacokinetic characteristics in rat models with an oral bioavailability of 57%.
For research use only. We do not sell to patients.
- CAS No.: 1860885-61-5
- Formula: C23H22N6O2
- Molecular Weight:414.46
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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CDK8 5.1 nM (IC50) |
CDK19 5.6 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SW-620 | IC50 |
17.9 nM
Compound: 51
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In vivo inhibition of STAT1 phosphorylation at ser727 in human SW620 cells harboring APC mutation xenografted in mouse administered through oral gavage every 24 hrs measured after 2 to 24 hrs post last dose by Western blot analysis
In vivo inhibition of STAT1 phosphorylation at ser727 in human SW620 cells harboring APC mutation xenografted in mouse administered through oral gavage every 24 hrs measured after 2 to 24 hrs post last dose by Western blot analysis
|
[PMID: 27326329] |
Chemical Information
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CAS No. 1860885-61-5
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Molecular Weight 414.46
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Formula C23H22N6O2
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SMILES
O=C(N1CC(C1)OC)C2=NC3=C(C4=CC=C(C5=CN(C)N=C5)C=C4)C=NC(N)=C3C=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)