MSC2530818 (C007B-231052)

InformationMSC2530818 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.TargetsCDK8 (Cell-free assay) 2.6 nMIn vitroMSC2530818 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).In vivoMSC2530818 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.

Specifications and Purity: ≥98%

Molecular Formula: C18H17ClN4O

Molecular Weight: 340.81

PubChem CID: 118879529

Isomeric SMILES: CC1=C2C=C(C=NC2=NN1)C(=O)N3CCC[C@H]3C4=CC=C(C=C4)Cl

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