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.
For research use only. We do not sell to patients.
- CAS No.: 3024381-54-9
- Formula: C17H20Br2F2N4O
- Molecular Weight:494.17
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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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 No. 3024381-54-9
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Molecular Weight 494.17
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Formula C17H20Br2F2N4O
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SMILES
BrC1=C(C=C2N(C(N3CCNCC3)=NC2=C1C(F)F)C4CCOCC4)Br
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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