Cat. No.: HY-101611

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MSC2530818

3 Cited Publications

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Based on 3 publication(s) in Google Scholar

MSC2530818 is a potent, selective and orally available CDK8 inhibitor with an IC₅₀ of 2.6 nM for CDK8.

For research use only. We do not sell to patients.

Purity: 99.52%
CAS No.: 1883423-59-3
Formula: C₁₈H₁₇ClN₄O
Molecular Weight:340.81

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

MSC2530818 Chemical Structure

CAS No.: 1883423-59-3

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (3)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

MSC2530818 is a potent, selective and orally available CDK8 inhibitor with an IC₅₀ of 2.6 nM for CDK8.

IC₅₀ & Target^[1]

CDK8

2.6 nM (IC₅₀)

All CDK Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	8.5 μM Compound: 25; MSC2530818	Displacement of [3H]BTCP from human recombinant dopamine transporter expressed in CHO cells after 120 mins by scintillation counting method Displacement of [3H]BTCP from human recombinant dopamine transporter expressed in CHO cells after 120 mins by scintillation counting method	[PMID: 27490956]
COLO 205	IC₅₀	9 nM Compound: 25; MSC2530818	Inhibition of CDK8 in human COLO205 cells expressing APC mutant assessed as suppression of WNT pathway by luciferase reporter gene assay Inhibition of CDK8 in human COLO205 cells expressing APC mutant assessed as suppression of WNT pathway by luciferase reporter gene assay	[PMID: 27490956]
HCT-116	IC₅₀	70.25 μM Compound: MSC2530818	Growth inhibition of human HCT116 cells after 72 hrs by Celltiter-glo assay Growth inhibition of human HCT116 cells after 72 hrs by Celltiter-glo assay	[PMID: 30630717]
LS174T	IC₅₀	32 nM Compound: 25; MSC2530818	Inhibition of CDK8 in human LS174T cells expressing beta-catenin mutant assessed as suppression of WNT pathway by luciferase reporter gene assay Inhibition of CDK8 in human LS174T cells expressing beta-catenin mutant assessed as suppression of WNT pathway by luciferase reporter gene assay	[PMID: 27490956]
PA-1	IC₅₀	52 nM Compound: 25; MSC2530818	Inhibition of CDK8 in human PA1 cells assessed as suppression of WNT3a ligand-induced WNT pathway by luciferase reporter gene assay Inhibition of CDK8 in human PA1 cells assessed as suppression of WNT3a ligand-induced WNT pathway by luciferase reporter gene assay	[PMID: 27490956]
SW-620	IC₅₀	52.41 μM Compound: MSC2530818	Growth inhibition of human SW620 cells after 72 hrs by Celltiter-glo assay Growth inhibition of human SW620 cells after 72 hrs by Celltiter-glo assay	[PMID: 30630717]
SW-620	IC₅₀	8 nM Compound: 25; MSC2530818	Inhibition of CDK8 in human SW620 cells assessed as decrease in STAT1 phosphorylation at Ser727 Inhibition of CDK8 in human SW620 cells assessed as decrease in STAT1 phosphorylation at Ser727	[PMID: 27490956]

In Vitro

MSC2530818 binds to CDK8 and CDK19 with similar affinity (4 nM). Potent inhibition of phospho-STAT1^SER727, an established biomarker of CDK8 activity, in SW620 human colorectal carcinoma cells is also observed (pSTAT1^SER727 IC₅₀=8±2 nM). MSC2530818 demonstrates potent inhibition of WNT-dependent transcription in human cancer cell lines that have constitutively activated WNT signaling. For example, MSC2530818 inhibits the reporter-based luciferase readout in several cell lines bearing activating WNT-pathway mutations; LS174T (β-catenin mutant, IC₅₀=32±7 nM), COLO205 (APC mutant, IC₅₀=9±1 nM) and demonstrates inhibition of WNT3a ligand-dependent reporter readout in PA-1 cells (IC₅₀=52±30 nM). MSC2530818 demonstrates minimal activity in the CEREP panel, and demonstrates minimal hERG inhibition. Furthermore, MSC2530818 is a soluble CDK8 inhibitor with high permeability and low efflux ratio in Caco-2 cells and does not inhibit any cytochrome P450 subtypes^[1].

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

In Vivo

Tumor-bearing mice treated with MSC2530818 shows reduction in tumor growth with T/C ratios (based on final tumor weights) of 49% and 57%, respectively. MSC2530818 is generally well tolerated, with no effects on mouse body weight in the qd administration schedule and manageable body weight loss. The human clearance and volume of distribution at steady-state are estimated to be low (0.14 L/h/kg) and small (0.48 L/kg), respectively, resulting in a short predicted terminal half-life (2.4 h). Physiologically based pharmacokinetics simulations suggested that human oral bioavailability may be ≥75% up to dose level of 500 mg daily^[1].

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

Chemical Information

CAS No. 1883423-59-3
Appearance Solid
Molecular Weight 340.81
Formula C₁₈H₁₇ClN₄O
Color White to off-white
SMILES

O=C(N1[C@H](C2=CC=C(Cl)C=C2)CCC1)C3=CN=C(NN=C4C)C4=C3
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (3)

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Pharmaceuticals (Basel)

New Assay Systems to Characterize the Broad-Spectrum Antiherpesviral and Non-Herpesviral Activity of Cyclin-Dependent Kinase (CDK) 8 Inhibitors. [Abstract]

2025 Oct 16;18(10):1560. PMID: 41155676
bioRxiv

2025 Dec 9.
bioRxiv

2025 Jun 19.

Solvent & Solubility

In Vitro:

DMSO : 110 mg/mL (322.76 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

2.9342 mL

14.6709 mL

29.3419 mL

5 mM

0.5868 mL

2.9342 mL

5.8684 mL

10 mM

0.2934 mL

1.4671 mL

2.9342 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.75 mg/mL (8.07 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.75 mg/mL (8.07 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.75 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.75 mg/mL (8.07 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocol

Animal Administration^[1]

Mice: MSC2530818 is then 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].

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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)

References

[1]. Czodrowski P, et al. Structure-Based Optimization of Potent, Selective, and Orally Bioavailable CDK8 Inhibitors Discovered by High-Throughput Screening. J Med Chem. 2016 Oct 27;59(20):9337-9349. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.9342 mL	14.6709 mL	29.3419 mL	73.3547 mL
	5 mM	0.5868 mL	2.9342 mL	5.8684 mL	14.6709 mL
	10 mM	0.2934 mL	1.4671 mL	2.9342 mL	7.3355 mL
	15 mM	0.1956 mL	0.9781 mL	1.9561 mL	4.8903 mL
	20 mM	0.1467 mL	0.7335 mL	1.4671 mL	3.6677 mL
	25 mM	0.1174 mL	0.5868 mL	1.1737 mL	2.9342 mL
	30 mM	0.0978 mL	0.4890 mL	0.9781 mL	2.4452 mL
	40 mM	0.0734 mL	0.3668 mL	0.7335 mL	1.8339 mL
	50 mM	0.0587 mL	0.2934 mL	0.5868 mL	1.4671 mL
	60 mM	0.0489 mL	0.2445 mL	0.4890 mL	1.2226 mL
	80 mM	0.0367 mL	0.1834 mL	0.3668 mL	0.9169 mL
	100 mM	0.0293 mL	0.1467 mL	0.2934 mL	0.7335 mL

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MSC2530818

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Publications Citing Use of MedChemExpress (MCE) MSC2530818

All CDK Isoforms

Biological Activity

Chemical Information

Publications (3)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

MSC2530818

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Publications Citing Use of MedChemExpress (MCE) MSC2530818

All CDK Isoforms

Biological Activity

Chemical Information

Publications (3)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

MSC2530818 Related Classifications

HY-101611 Related Classifications