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 No.: 1860885-61-5
- 화학식: C23H22N6O2
- 분자량:414.46
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
제품 설명
IC50 & Target
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CDK8 5.1 nM (IC50) |
CDK19 5.6 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SW-620 | IC50 |
17.9 nM
Compound: 51
|
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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분자량 414.46
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocol
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Protocol for Pharmacokinetic Study
Pharmacokinetic studies quantify how an organism handles a drug over time through absorption, distribution, metabolism, and excretion, and the core experimental readout is the concentration-time profile of parent drug and, when relevant, metabolites in biological matrices such as plasma, whole blood, urine, bile, or tissue. Pharmacokinetic analysis links dose, route, exposure, clearance, half-life, distribution, bioavailability, and systemic exposure to drug efficacy and toxicity hypotheses rather than measuring a signaling pathway directly. The literature links pharmacokinetics to drug-development phenotypes by showing that drug metabolism and pharmacokinetics influence compound progression, exposure-response interpretation, safety margins, dosing strategy, and failure risk during discovery and development. DMPK science contributes to compound optimization by integrating physicochemical properties, in vitro metabolism, transporter behavior, in vivo exposure, and pharmacodynamic contex
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)