MSC2530818

Catalog No.S8387 Batch:S838701

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Technical Data

Formula

C18H17ClN4O
Molecular Weight 340.81 CAS No. 1883423-59-3
Solubility (25°C)* In vitro DMSO 68 mg/mL (199.52 mM)
Ethanol 68 mg/mL (199.52 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
3.45mg/ml
5% DMSO 95% Corn oil
1.7mg/ml
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 Study:

[1]
  • Animal Models

    NCr athymic mice

  • Dosages

    50 mg/kg bid or 100 mg/kg qd

  • Administration

    p.o.

Selleck's MSC2530818 has been cited by 7 publications

Organoids at the PUB: The Porcine Urinary Bladder serves As A Pancreatic Niche for Advanced Cancer Modelling [ Adv Healthc Mater, 2022, e2102345] PubMed: 35114730
LATS1 is a central signal transmitter for achieving full type-I interferon activity [ Sci Adv, 2022, 8(14):eabj3887] PubMed: 35394840
Single-cell-resolved differentiation of human induced pluripotent stem cells into pancreatic duct-like organoids on a microwell chip [ Nat Biomed Eng, 2021, 10.1038/s41551-021-00757-2] PubMed: 34239116
Modeling plasticity and dysplasia of pancreatic ductal organoids derived from human pluripotent stem cells [ Cell Stem Cell, 2021, 28(6):1105-1124.e19] PubMed: 33915078
Differentiation of human pluripotent stem cells into pancreatic duct-like organoids [ STAR Protoc, 2021, 2(4):100913] PubMed: 34917972
A kinase-independent role for CDK8 in BCR-ABL1+ leukemia. [ Nat Commun, 2019, 10(1):4741] PubMed: 31628323
A kinase-independent role for CDK8 in BCR-ABL1+ leukemia [ Nature Communications, 2019, ] PubMed: None

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.