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MSC2530818

Name: MSC2530818
Brand: TargetMol
SKU: TQ0266
Price: 60 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. TQ0266Cas No. 1883423-59-3

MSC2530818 is an effective, selective and orally available CDK8 inhibitor (IC50: 2.6 nM).

MSC2530818

😃Good

Purity: 98.93%

Catalog No. TQ0266Cas No. 1883423-59-3

MSC2530818 is an effective, selective and orally available CDK8 inhibitor (IC50: 2.6 nM).

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$60	In Stock	In Stock
5 mg	$147	In Stock	In Stock
10 mg	$239	In Stock	In Stock
25 mg	$513	In Stock	In Stock
50 mg	$768	-	In Stock
100 mg	$1,070	-	In Stock
1 mL x 10 mM (in DMSO)	$162	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:98.93%

Appearance:Solid

Color:White

Resource Download

COA HNMR LCMS

Product Introduction

Bioactivity

Description	MSC2530818 is an effective, selective and orally available CDK8 inhibitor (IC50: 2.6 nM).
Targets&IC50	CDK8:2.6 nM (cell free)
In vitro	MSC2530818 binds to CDK8 and CDK19 with a similar affinity (4 nM) and shows potent inhibition of phospho-STAT1SER727, a biomarker of CDK8 activity, in SW620 human colorectal carcinoma cells (pSTAT1SER727 IC50=8±2 nM). It also inhibits WNT-dependent transcription in human cancer cell lines with activated WNT signaling, including LS174T (β-catenin mutant, IC50=32±7 nM), COLO205 (APC mutant, IC50=9±1 nM), and WNT3a ligand-dependent reporter readout in PA-1 cells (IC50=52±30 nM). Moreover, MSC2530818 exhibits a low efflux ratio in Caco-2 cells and does not inhibit any cytochrome P450 subtypes.
In vivo	Treatment with MSC2530818 in mice carrying tumors resulted in a notable reduction of tumor growth, presenting T/C ratios of 49% and 57%. This compound was well accepted, showing no impact on the body weight of mice under a daily (qd) administration regimen, aside from controllable body weight loss. Additionally, its pharmacokinetic profile in humans indicates a low clearance (0.14 L/h/kg) and a small volume of distribution at steady-state (0.48 L/kg), leading to a brief estimated terminal half-life of 2.4 hours. Moreover, physiologically based pharmacokinetic simulations predict that MSC2530818 could achieve an oral bioavailability of at least 75% when administered up to a daily dose of 500 mg.
Animal Research	MSC2530818 is assessed in an established SW620 human colorectal cancer xenograft model in female NCr athymic mice. Tumor-bearing mice are treated orally with MSC2530818 (50 mg/kg bid or 100 mg/kg qd) for 16 days. Tumor weights are measured and body weights are monitored [1].

Chemical Properties

Molecular Weight	340.81
Formula	C₁₈H₁₇ClN₄O
Cas No.	1883423-59-3
Smiles	Cc1n[nH]c2ncc(cc12)C(=O)N1CCC[C@H]1c1ccc(Cl)cc1
Relative Density.	1.373 g/cm3 (Predicted)

Storage & Solubility Information

Storage

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 120 mg/mL (352.1 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (11.74 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.9342 mL	14.6709 mL	29.3419 mL	146.7093 mL
5 mM	0.5868 mL	2.9342 mL	5.8684 mL	29.3419 mL
10 mM	0.2934 mL	1.4671 mL	2.9342 mL	14.6709 mL
20 mM	0.1467 mL	0.7335 mL	1.4671 mL	7.3355 mL
50 mM	0.0587 mL	0.2934 mL	0.5868 mL	2.9342 mL
100 mM	0.0293 mL	0.1467 mL	0.2934 mL	1.4671 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

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

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