Home Tools

CDK8-IN-11

Catalog No. T61742 CAS 2839338-28-0

CDK8-IN-11 is a potent and selective inhibitor of CDK8, demonstrating an IC50 of 46 nM, and effectively targets the WNT/β-catenin signaling pathway. This compound has potential applications in colon cancer research [1].

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

CDK8-IN-11, CAS 2839338-28-0

Pack Size	Availability	Price/USD	Quantity
50 mg	10-14 weeks	$ 788.00
100 mg	10-14 weeks	$ 1,110.00

Bulk Inquiry

This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

Chemical Properties

Storage & Solubility Information

Description	CDK8-IN-11 is a potent and selective inhibitor of CDK8, demonstrating an IC50 of 46 nM, and effectively targets the WNT/β-catenin signaling pathway. This compound has potential applications in colon cancer research [1].
In vitro	CDK8-IN-11, identified as compound 29 at a concentration of 200 nM, demonstrates a 73.6% inhibition of CDK8, along with a substantial inhibitory effect on cell proliferation across various cell lines (HCT-116, HHT-29, SW480, CT-26, GES-1) at concentrations ranging from 0-50 μM over 48 hours. Furthermore, at concentrations of 0-4 μM for the same duration, it hinders the CDK8-mediated phosphorylation of STAT1 at Ser727 in HCT-116 cells. This compound also disrupts canonical WNT/β-catenin signaling pathways and interferes with β-catenin-mediated transcription in HCT-116 cells at 0-4 μM over 24 hours, while promoting an increase in the G1 phase cell population within a concentration range of 0.5-2 μM over 48 hours. Moreover, it effectively reverses Sorafenib resistance in HCT-116 cells at concentrations between 0-4 μM. Through cell proliferation assays and Western blot analysis, CDK8-IN-11 is shown to inhibit cell growth and STAT1 phosphorylation at precise concentrations without affecting JAK-regulated phosphorylation at Tyr701, alongside adjustments in the cell cycle, culminating in decreased G2/M and S phases in HCT-116 cells.
In vivo	CDK8-IN-11, at dosages of 10 and 40 mg/kg administered orally (p.o.), effectively inhibits tumor growth in CT-26 xenograft mice, significantly reducing both tumor volume and levels of β-catenin and c-Myc in the tumor. Additionally, a high dose of 1000 mg/kg given orally to ICR mice showed no signs of abnormal behavior within a seven-day observation period. Furthermore, CDK8-IN-11 demonstrated moderate permeability in rats with dosages of 10 mg/kg (p.o.) and 2 mg/kg (intravenously, i.v.), evidenced by an apparent permeability coefficient of 1.8 × 10^6 cm/s. The pharmacokinetic profile of CDK8-IN-11 in rats included a half-life (T 1/2) of 1.1 hours, a time to reach maximum concentration (T max) of 0.8 hours, and a maximum concentration (C max) of 453 ng/mL after oral administration (10 mg/kg), with a bioavailability (F) of 31.7%. Conversely, the intravenous administration (2 mg/kg) resulted in a T 1/2 of 0.5 hours and a C max of 318 ng/mL.

Molecular Weight	388.34
Formula	C19H15F3N4O2
CAS No.	2839338-28-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

CDK8-IN-11 2839338-28-0 inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.