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 番号: 1860885-61-5
- 分子式: C23H22N6O2
- 分子量:414.46
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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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
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[PMID: 27326329] |
化学情報
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CAS 番号 1860885-61-5
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分子量 414.46
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
CDK8-IN-16 関連分類
HY-171174 関連分類
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