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 No.: 3024381-54-9
- Formule: C17H20Br2F2N4O
- Masse moléculaire:494.17
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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- Pureté et documentation
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Help & FAQs
Activité biologique
Description
IC50 & Target
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CDK8/CycC 2.08 nM (IC50) |
CDK19/CycC 2.49 nM (IC50) |
Cellular Effect
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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] |
In Vitro
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.
In Vivo
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 No. 3024381-54-9
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Masse moléculaire 494.17
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Formule C17H20Br2F2N4O
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SMILES
BrC1=C(C=C2N(C(N3CCNCC3)=NC2=C1C(F)F)C4CCOCC4)Br
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CDK8/19-IN-2 Related Classifications
HY-158377 Related Classifications
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