1. Cell Cycle/DNA Damage
  2. CDK
  3. MSC2530818


Cat. No.: HY-101611 Purity: 99.69%
Handling Instructions

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.

MSC2530818 Chemical Structure

MSC2530818 Chemical Structure

CAS No. : 1883423-59-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 198 In-stock
Estimated Time of Arrival: December 31
5 mg USD 180 In-stock
Estimated Time of Arrival: December 31
10 mg USD 310 In-stock
Estimated Time of Arrival: December 31
25 mg USD 660 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1130 In-stock
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100 mg USD 1950 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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

IC50 & Target[1]


2.6 nM (IC50)

In Vitro

MSC2530818 binds to CDK8 and CDK19 with similar affinity (4 nM). Potent inhibition of phospho-STAT1SER727, an established biomarker of CDK8 activity, in SW620 human colorectal carcinoma cells is also observed (pSTAT1SER727 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].

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].

Molecular Weight







O=C(N1[[email protected]](C2=CC=C(Cl)C=C2)CCC1)C3=CN=C(NN=C4C)C4=C3


Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 125 mg/mL (366.77 mM)

*"≥" means soluble, but saturation unknown.

Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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.
Animal Administration

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].

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


Purity: 99.69%

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MSC2530818MSC 2530818MSC-2530818CDKCyclin dependent kinaseInhibitorinhibitorinhibit

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