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MSC2530818 CDK inhibitor

Name: MSC2530818
Brand: Selleck Chemicals
SKU: S8387
Availability: InStock
Rating: 5 (8 reviews)

Cat.No.S8387

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.

Chemical Structure

Molecular Weight: 340.81

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Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
SDS
Datasheet

99.94

Related Targets	HSP PD-1/PD-L1 ROCK Wee1 DNA/RNA Synthesis Microtubule Associated Ras KRas Aurora Kinase Casein Kinase
Other CDK Inhibitors	Ro-3306 JNJ-7706621 AZD4573 Enitociclib (BAY 1251152) SEL120 (SEL120-34A) hydrochloride Samuraciclib (ICEC0942) hydrochloride ON123300 AS2863619 PF-07220060 (CDK4/6-IN-6) SY-5609 INX-315 Tagtociclib (PF-07104091)

Solubility

In vitro
Batch:

DMSO : 68 mg/mL (199.52 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 68 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.450mg/ml (10.12mM)
	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.700mg/ml (4.99mM)

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

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
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	340.81	Formula	C₁₈H₁₇ClN₄O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1883423-59-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC1=C2C=C(C=NC2=NN1)C(=O)N3CCCC3C4=CC=C(C=C4)Cl

Mechanism of Action

Targets/IC₅₀/Ki	CDK8 (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^SER727 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. This compound 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 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/27490956/ [2] https://pubmed.ncbi.nlm.nih.gov/33915078/

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