Home Cell Cycle CDK inhibitor MSC2530818 For research use only.

MSC2530818

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 Chemical Structure

MSC2530818 Chemical Structure

CAS: 1883423-59-3

Selleck's MSC2530818 has been cited by 7 publications

Purity & Quality Control

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

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Biological Activity

Description 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.
Targets
CDK8 [1]
(Cell-free assay)
2.6 nM
In vitro
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. MSC2530818 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
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].
Animal Research Animal Models NCr athymic mice
Dosages 50 mg/kg bid or 100 mg/kg qd
Administration p.o.

Chemical Information & Solubility

Molecular Weight 340.81 Formula

C18H17ClN4O
CAS No. 1883423-59-3 SDF Download MSC2530818 SDF
Smiles CC1=C2C=C(C=NC2=NN1)C(=O)N3CCCC3C4=CC=C(C=C4)Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 68 mg/mL ( (199.52 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 68 mg/mL

Water : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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