1. Cell Cycle/DNA Damage Stem Cell/Wnt JAK/STAT Signaling
  2. CDK STAT
  3. 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.

CDK8/19-IN-2 Chemical Structure

CDK8/19-IN-2 Chemical Structure

CAS No. : 3024381-54-9

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Description

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[1].

IC50 & Target

CDK8/CycC

2.08 nM (IC50)

CDK19/CycC

2.49 nM (IC50)

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

CDK8/19-IN-2 (compound 12) (3-10 mg/kg, orally by gavage, once per day) inhibits tumor growth[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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]
Dosage: 3 mg/kg, 10 mg/kg
Administration: orally by gavage, once per day
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.
Molecular Weight

494.17

Formula

C17H20Br2F2N4O

CAS No.
SMILES

BrC1=C(C=C2N(C(N3CCNCC3)=NC2=C1C(F)F)C4CCOCC4)Br

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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CDK8/19-IN-2
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HY-158377
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