CDK8-IN-11 hydrochloride
CDK8-IN-11 hydrochloride is a potent and selective CDK8 inhibitor with an IC50 value of 46 nM. CDK8-IN-11 hydrochloride inhibits WNT/β-catenin signaling pathway. CDK8-IN-11 hydrochloride can be used in the research of colon cancer.
For research use only. We do not sell to patients.
- Formula: C19H16ClF3N4O2
- Molecular Weight:424.80
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
CDK8-IN-11 (compound 29, 200 nM) hydrochloride shows inhibitory effects against CDK8 by 73.6% [1].
CDK8-IN-11 (0-50 μM, 48 h) hydrochloride inhibits cell proliferation in HCT-116, HHT-29, SW480, CT-26, GES-1 cells[1].
CDK8-IN-11 (0-4 μM, 48 h) hydrochloride inhibits the phosphorylation of STAT1 at Ser727 mediated by CDK8 in HCT-116 cells[1].
CDK8-IN-11 (0-4 μM, 24 h) hydrochloride suppresses canonical WNT/β-catenin signaling pathways and deregulates β-catenin-mediated transcription in HCT-116 cells[1].
CDK8-IN-11 (0.5-2 μM, 48 h) hydrochloride increases the number of cells in the G1 phase in HCT-116 cells[1].
CDK8-IN-11 (0-4 μM) hydrochloride reverses Sorafenib (HY-10201) resistance of HCT-116 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT-116, HHT-29, SW480, CT-26, GES-1 cells
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Concentration:0.08, 0.4, 2, 10, and 50 μM
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Incubation Time:48 h
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Result:Inhibited cell proliferation with IC50 values of 1.2, 0.7, 2.4, 5.5, 62.7 nM respectively.
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Cell Line:HCT-116 cell
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Concentration:0, 1, 2, 4 μM
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Incubation Time:48 h
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Result:Inhibited the phosphorylation of STAT1 at Ser727 without affecting the JAK-regulated phosphorylation at Tyr701.
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Cell Line:HCT-116 cell
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Concentration:0.5-2 μM
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Incubation Time:48 h
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Result:Increased the number of cells in the G1 phase with an obvious decreased percentage of cells in the G2/M and S phase in HCT-116 cells.
CDK8-IN-11 (1000 mg/kg, oral gavage, ICR mice) hydrochloride shows no obvious abnormal behavior within 7 days[1].
CDK8-IN-11 (10 mg/kg, p.o.; 2 mg/kg, i.v., rats) hydrochloride shows moderate permeability with an apparent permeability coefficient value of 1.8 × 10 6 cm/s[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CT-26 xenograft mice[1]
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Dosage:10 and 40 mg/kg
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Administration:Oral adminstration (p.o.)
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Result:Reduced the tumor volume, reduced β-catenin and c-Myc level in tumor.
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Animal Model:Reduced the tumor volume, reduced β-catenin and c-Myc level in tumor.
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Dosage:10 mg/kg (p.o.), 2 mg/kg (i.v.)
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Administration:Oral adminstration (p.o.) or intravenous injection (i.v.)
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Result:Pharmacokinetic profile of CDK8-IN-11 (compound 29).
dose (mg/kg) T1/2 (h) Tmax (h) Cmax (ng/mL) F (%) 10 (p.o.) 1.1 0.8 453 31.7 2 (i.v.) 0.5 318
Chemical Information
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Molecular Weight 424.80
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Formula C19H16ClF3N4O2
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SMILES
O=C(NC1=CC=CC(C(F)(F)F)=C1)NC2=CC=C(OC3=CC=C(N)N=C3)C=C2.[H]Cl
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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)
CDK8-IN-11 hydrochloride Related Classifications
HY-151463A Related Classifications
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