CDK8/19-IN-2
CDK8/19-IN-2 (compound 12) is an orally active and potent cyclin-dependent kinase 8/19 (CDK8 and CDK19) inhibitor, with IC50 values of 2.08 and 2.49 nM, respectively. CDK8/19-IN-2 can be used for acute myeloid leukemia (AML), breast cancer, and lymphoma research.
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- CAS. Nr.: 3024381-54-9
- Formel: C17H20Br2F2N4O
- Molecular Weight:494.17
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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
- Reinheit & Dokumentation
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Help & FAQs
Biologische Aktivität
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CDK8/CycC 2.08 nM (IC50) |
CDK19/CycC 2.49 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| MDA-MB-231 | IC50 |
40 nM
Compound: 12
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Inhibition of cell growth in human MDA-MB-231 cells
Inhibition of cell growth in human MDA-MB-231 cells
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[PMID: 38690856] |
| MV4-11 | IC50 |
5.7 nM
Compound: 12
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Antiproliferative activity against human MV4-11 cells incubated for 5 days by CellTiter-Glo luminescent cell viability assay
Antiproliferative activity against human MV4-11 cells incubated for 5 days by CellTiter-Glo luminescent cell viability assay
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[PMID: 38690856] |
CDK8/19-IN-2 (compound 12) inhibits the proliferation of MV4-11 human AML cells (IC50 = 5.719 nM)[1].
CDK8/19-IN-2 (0-10 μM) dose-dependently decreases phosphorylation of STAT1 on serine 727 (p-STAT1 S727)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c nude mice (6-8 weeks, human AML cell line MV4-11 were inoculated subcutaneously at the right flanks of animals)[1]
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Dosage:3 mg/kg, 10 mg/kg
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Administration:orally by gavage, once per day
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Result:Resulted in a dose-dependent inhibition of tumor growth, reaching end point tumor growth inhibition (TGI) of 29%, and 76% at 3 and 10 mg/kg, respectively, without affecting body weight.
Chemical Information
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CAS. Nr. 3024381-54-9
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Molecular Weight 494.17
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Formel C17H20Br2F2N4O
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SMILES
BrC1=C(C=C2N(C(N3CCNCC3)=NC2=C1C(F)F)C4CCOCC4)Br
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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)
CDK8/19-IN-2 Related Classifications
HY-158377 Related Classifications
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