Home Cell Cycle CDK inhibitor MSC2530818

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MSC2530818 CDK inhibitor

Cat.No.S8387

MSC2530818, a CDK8 inhibitor with the IC50 of 2.6 nM, displays excellent kinase selectivity, biochemical and cellular potency, microsomal stability, and is orally bioavailable.
MSC2530818 CDK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 340.81

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Quality Control

Batch: S838701 DMSO]68 mg/mL]false]Ethanol]68 mg/mL]false]Water]Insoluble]false Purity: 99.94%
99.94

Chemical Information, Storage & Stability

Molecular Weight 340.81 Formula

C18H17ClN4O

 Storage (From the date of receipt)
CAS No. 1883423-59-3 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC1=C2C=C(C=NC2=NN1)C(=O)N3CCCC3C4=CC=C(C=C4)Cl

Solubility

In vitro
Batch:

DMSO : 68 mg/mL (199.52 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 68 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
CDK8 [1]
(Cell-free assay)
2.6 nM
In vitro

MSC2530818 binds to CDK8 and CDK19 with similar affinity (4 nM) and shows potent inhibition of phospho-STAT1SER727 in SW620 human colorectal carcinoma cells (IC50=8 ± 2 nM). It also demonstrates potent inhibition of WNT-dependent transcription in human cancer cell lines that have constitutively activated WNT signaling. This compound is a soluble CDK8 inhibitor with high permeability and low efflux ratio in Caco-2 cells (ER = 1.5) and does not inhibit any cytochrome P450 subtypes (Cyp IC50s > 20 μM)[1].
In vivo

MSC2530818 shows acceptable pharmacokinetics (PK) in all tested preclinical species (mouse, rat, dog). It demonstrates reduction of tumor growth rates of established human SW620 colorectal carcinoma xenografts[1].
References

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