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%.
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- CAS. Nr.: 1860885-61-5
- Formel: C23H22N6O2
- Molecular Weight:414.46
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Help & FAQs
Biologische Aktivität
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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 |
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| 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
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[PMID: 27326329] |
Chemical Information
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CAS. Nr. 1860885-61-5
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Molecular Weight 414.46
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
CDK8-IN-16 Related Classifications
HY-171174 Related Classifications
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