MSC2530818

Catalog No.S8387

For research use only.

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

CAS No. 1883423-59-3

Selleck's MSC2530818 has been cited by 5 Publications

Purity & Quality Control

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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

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 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].

Protocol (from reference)

Animal Research:

[1]

  • Animal Models: NCr athymic mice
  • Dosages: 50 mg/kg bid or 100 mg/kg qd
  • Administration: p.o.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 340.81
Formula

C18H17ClN4O

CAS No. 1883423-59-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C2C=C(C=NC2=NN1)C(=O)N3CCCC3C4=CC=C(C=C4)Cl

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

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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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