Art. -Nr.: HY-151463

CDK8-IN-11

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CDK8-IN-11 is a potent and selective CDK8 inhibitor with an IC₅₀ value of 46 nM. CDK8-IN-11 inhibits WNT/β-catenin signaling pathway. CDK8-IN-11 can be used in the research of colon cancer.

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Reinheit: 98.18%
CAS. Nr.: 2839338-28-0
Formel: C₁₉H₁₅F₃N₄O₂
Molecular Weight:388.34

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

CDK8-IN-11 Chemical Structure

CAS. Nr.: 2839338-28-0

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

CDK8

46 nM (IC₅₀)

Alle Wnt Isoform-spezifische Produkte anzeigen :

Alle CDK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CT26	GI₅₀	5.5 μM Compound: 29	Antiproliferative activity against human CT26 cells assessed as cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human CT26 cells assessed as cell viability incubated for 48 hrs by MTT assay	[PMID: 36126227]
GES1	GI₅₀	62.7 μM Compound: 29	Cytotoxicity against human GES1 cells assessed as cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human GES1 cells assessed as cell viability incubated for 48 hrs by MTT assay	[PMID: 36126227]
HCT-116	GI₅₀	1.2 μM Compound: 29	Antiproliferative activity against human HCT-116 cells assessed as cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as cell viability incubated for 48 hrs by MTT assay	[PMID: 36126227]
HCT-116	GI₅₀	17.5 μM Compound: 29	Antiproliferative activity against sorafenib-resistant human HCT-116 cells assessed as cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against sorafenib-resistant human HCT-116 cells assessed as cell viability incubated for 48 hrs by MTT assay	[PMID: 36126227]
HT-29	GI₅₀	0.7 μM Compound: 29	Antiproliferative activity against human HT-29 cells assessed as cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human HT-29 cells assessed as cell viability incubated for 48 hrs by MTT assay	[PMID: 36126227]
SW480	GI₅₀	2.4 μM Compound: 29	Antiproliferative activity against human SW480 cells assessed as cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human SW480 cells assessed as cell viability incubated for 48 hrs by MTT assay	[PMID: 36126227]

In Vitro

CDK8-IN-11 (compound 29, 200 nM) shows inhibitory effects against CDK8 by 73.6% ^[1].
CDK8-IN-11 (0-50 μM, 48 h) inhibits cell proliferation in HCT-116, HHT-29, SW480, CT-26, GES-1 cells^[1].
CDK8-IN-11 (0-4 μM, 48 h) inhibits the phosphorylation of STAT1 at Ser727 mediated by CDK8 in HCT-116 cells^[1].
CDK8-IN-11 (0-4 μM, 24 h) 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) increases the number of cells in the G1 phase in HCT-116 cells^[1].
CDK8-IN-11 (0-4 μM) 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.

Cell Proliferation Assay^[1]

Cell Line:

HCT-116, HHT-29, SW480, CT-26, GES-1 cells
Concentration:

0.08, 0.4, 2, 10, and 50 μM
Incubation Time:

48 h
Result:

Inhibited cell proliferation with IC₅₀ values of 1.2, 0.7, 2.4, 5.5, 62.7 nM respectively.

Western Blot Analysis^[1]

Cell Line:

HCT-116 cell
Concentration:

0, 1, 2, 4 μM
Incubation Time:

48 h
Result:

Inhibited the phosphorylation of STAT1 at Ser727 without affecting the JAK-regulated phosphorylation at Tyr701.

Cell Cycle Analysis^[1]

Cell Line:

HCT-116 cell
Concentration:

0.5-2 μM
Incubation Time:

48 h
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.

In Vivo

CDK8-IN-11 (compound 29, 10 and 40 mg/kg, p.o.) inhibits tumor growth in CT-26 xenograft mice^[1].
CDK8-IN-11 (1000 mg/kg, oral gavage, ICR mice) shows no obvious abnormal behavior within 7 days^[1].
CDK8-IN-11 (10 mg/kg, p.o.; 2 mg/kg, i.v., rats) shows moderate permeability with an apparent permeability coefficient value of 1.8 × 10⁶ cm/s^[1].

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

Animal Model:

CT-26 xenograft mice^[1]
Dosage:

10 and 40 mg/kg
Administration:

Oral adminstration (p.o.)
Result:

Reduced the tumor volume, reduced β-catenin and c-Myc level in tumor.

Animal Model:

Rats (pharmacokinetic assay)^[1]
Dosage:

10 mg/kg (p.o.), 2 mg/kg (i.v.)
Administration:

Oral adminstration (p.o.) or intravenous injection (i.v.)
Result:

Pharmacokinetic profile of CDK8-IN-11 (compound 29).

dose (mg/kg) T_1/2 (h) T_max (h) C_max (ng/mL) F (%)

10 (p.o.) 1.1 0.8 453 31.7

2 (i.v.) 0.5 318

Chemical Information

CAS. Nr. 2839338-28-0
Appearance Solid
Molecular Weight 388.34
Formel C₁₉H₁₅F₃N₄O₂
Color Light yellow to yellow
SMILES

O=C(NC1=CC=CC(C(F)(F)F)=C1)NC2=CC=C(OC3=CC=C(N)N=C3)C=C2
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 250 mg/mL (643.77 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5751 mL

12.8753 mL

25.7506 mL

5 mM

0.5150 mL

2.5751 mL

5.1501 mL

10 mM

0.2575 mL

1.2875 mL

2.5751 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Yao Yao Yan, et al. Design and Synthesis of a 2-Amino-pyridine Derivative as a Potent CDK8 Inhibitor for Anti-colorectal Cancer Therapy. J Med Chem. 2022 Sep 20. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5751 mL	12.8753 mL	25.7506 mL	64.3766 mL
	5 mM	0.5150 mL	2.5751 mL	5.1501 mL	12.8753 mL
	10 mM	0.2575 mL	1.2875 mL	2.5751 mL	6.4377 mL
	15 mM	0.1717 mL	0.8584 mL	1.7167 mL	4.2918 mL
	20 mM	0.1288 mL	0.6438 mL	1.2875 mL	3.2188 mL
	25 mM	0.1030 mL	0.5150 mL	1.0300 mL	2.5751 mL
	30 mM	0.0858 mL	0.4292 mL	0.8584 mL	2.1459 mL
	40 mM	0.0644 mL	0.3219 mL	0.6438 mL	1.6094 mL
	50 mM	0.0515 mL	0.2575 mL	0.5150 mL	1.2875 mL
	60 mM	0.0429 mL	0.2146 mL	0.4292 mL	1.0729 mL
	80 mM	0.0322 mL	0.1609 mL	0.3219 mL	0.8047 mL
	100 mM	0.0258 mL	0.1288 mL	0.2575 mL	0.6438 mL

Keywords

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dose (mg/kg)	T_1/2 (h)	T_max (h)	C_max (ng/mL)	F (%)
10 (p.o.)	1.1	0.8	453	31.7
2 (i.v.)	0.5		318

CDK8-IN-11

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Stem Cell Signaling Compound Library

Wnt/Hedgehog/Notch Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Neuroprotective Compound Library

Anti-Breast Cancer Compound Library

Anti-Blood Cancer Compound Library

Transcription Factor-Targeted Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Antihypertensive Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Extracellular Vesicles (EVs) Compound Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Alle Wnt Isoform-spezifische Produkte anzeigen

Alle CDK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CDK8-IN-11 Related Classifications

HY-151463 Related Classifications