[CAS NO. 1883423-59-3] MSC2530818

Name: MSC2530818
Brand: Arctom Scientific
SKU: SLK-S8387

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PRODUCTS SPECIFICATIONS [1883423-59-3]

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Catalog

SLK-S8387

Brand

Selleck

CAS

1883423-59-3

DESCRIPTION [1883423-59-3]

Overview

MDL	-
Molecular Weight	340.81
Molecular Formula	C18H17ClN4O
SMILES	O=C(N1[C@H](C2=CC=C(Cl)C=C2)CCC1)C3=CN=C(NN=C4C)C4=C3

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume 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
50 mM	0.0587 mL	0.2934 mL	0.5868 mL

Description

MSC2530818, a inhibitor with the 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-STAT1 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).

References

[1] Czodrowski P, et al. J Med Chem. 2016, 59(20):9337-9349.
[2] Breunig M, et al. Cell Stem Cell. 2021 Jun 3;28(6):1105-1124.e19.