Name: KD025 (Belumosudil)
Brand: Selleck Chemicals
SKU: S7936
Availability: InStock
Rating: 5 (11 reviews)

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Quality Control

Batch: Purity: 99.95%

99.95

Related Targets	CDK HSP PD-1/PD-L1 Wee1 DNA/RNA Synthesis Microtubule Associated Ras KRas Aurora Kinase Casein Kinase
Other ROCK Inhibitors	Y-27632 Ripasudil hydrochloride dihydrate NRL-1049 Y-27632 Dihydrochloride Fasudil (HA-1077) Hydrochloride Thiazovivin (TZV) GSK429286A RKI-1447 GSK269962A HCl Y-39983 Dihydrochloride

Solubility

In vitro
Batch:

DMSO : 90 mg/mL (198.89 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : 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.
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.
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.
Clear solution	5%DMSO 1 35%PEG300 2 2%Tween80 3 58%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	7.000mg/ml (15.47mM)	Taking the 1 mL working solution as an example, add 50 μL of 140 mg/ml clarified DMSO stock solution to 350 μL of PEG300, mix evenly to clarify it; add 20 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 580 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
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.
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.

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	452.51	Formula	C₂₆H₂₄N₆O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	911417-87-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	SLx-2119			Smiles	CC(C)NC(=O)COC1=CC=CC(=C1)C2=NC3=CC=CC=C3C(=N2)NC4=CC5=C(C=C4)NN=C5

Mechanism of Action

Targets/IC₅₀/Ki	ROCK2 (Cell-free assay) 41 nM(Ki) ROCK2 (Cell-free assay) 60 nM
In vitro	Belumosudil (KD025) down-regulates the IL-17 and IL-21 secretion in human PBMCs, and leads to down-regulation of STAT3 phosphorylation, IRF4, and RORγt expression in CD4+ T cells. It also inhibits the secretion of IL-21, IL-17, and IFNγ along with decreasing phosphorylated STAT3 and reduced protein expression of IRF4 and BCL6 in human peripheral blood mononuclear cells.
Kinase Assay	Recombinant ROCK1 and ROCK2 assays
Kinase Assay	Belumosudil (KD025) compound dilutions and reactions are performed in 96-well polystyrene low-binding plates. Filtration is done in 96-well filter plates containing hydrophilic phospho-cellulose cation exchanger membranes. Enzymatic activity of the recombinant ROCK1 and ROCK2 is measured radiometrically in 50 μL of reaction mixture containing assay buffer (50 mmol/L Tris, pH 7.5, 0.1 mmol/L ethyleneglycoltetraacetic acid, 10 mmol/L magnesium acetate and 1 mmol/L dithiothreitol).. The reaction is incubated for 45 min at room temperature and stopped with 25 μL of 3% phosphoric acid. Phosphorylated long S6 peptide is separated from unreacted [[gamma]-³³P]ATP by filtration of the quenched reaction contents through a P30 phosphocellulose filter plate. Each filter is washed three times with 75 μL of 75 mmol/L phosphoric acid and one time with 30 μL of 100% methanol. Filter plates are allowed to dry and 30 μL of OptiPhase ‘SuperMix’ scintillation fluid is added to each well. ³³Phosphorous is quantified in an I450 MicroBeta scintillation counter and corrected by subtracting the radioactivity associated with the background samples. Data are analyzed and expressed as percent inhibition using the formula ((U − B)/(C − B)) × 100 where U is the unknown value, B is the average of staurosporine background wells, and C is the average of control wells. Curve fitting is performed by GraphPad Prism software using sigmoidal dose-response (variable slope) equation type analysis to generate IC50 values. Ki values are calculated from an equation of Ki = IC50/(1 + [S]/Km)), where [S] and Km are the concentration of ATP and the Km value of ATP, respectively.
In vivo	Belumosudil (KD025) (200 mg/kg, p.o.) inhibits ROCK activity in brain and heart, as measured by the degree of MYPT1 phosphorylation. It significantly reduces the area of perfusion defect and tissue loss in the ipsilateral hemisphere. In a collagen-induced arthritis (CIA) mouse model, this compound (200 mg/kg, i.p.) downregulates the progression of collagen-induced arthritis via targeting of the Th17-mediated pathway. It (150 mg/kg, i.p. or p.o.) effectively ameliorates cGVHD in a full MHC-mismatch model of multi-organ system cGVHD with bronchiolitis obliterans syndrome and a minor MHC-mismatch model of sclerodermatous GVHD.
References	[1] https://pubmed.ncbi.nlm.nih.gov/24466563/ [2] https://pubmed.ncbi.nlm.nih.gov/25385601/ [3] https://pubmed.ncbi.nlm.nih.gov/26983850/ [4] https://pubmed.ncbi.nlm.nih.gov/35427166/

Applications

Methods	Biomarkers	Images	PMID
Western blot	pSTAT3 / Bcl6 / pSTAT5 / Blimp1		27436361
ELISA	IL-21 / IL-17 / IFN-γ		25385601

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03919799	Terminated	System; Sclerosis\|Diffuse Cutaneous Systemic Sclerosis	Kadmon a Sanofi Company\|Sanofi	June 26 2019	Phase 2
NCT02841995	Completed	Graft vs Host Disease	Kadmon a Sanofi Company\|Sanofi	September 15 2016	Phase 2
NCT02557139	Completed	Bioavailability	Kadmon Corporation LLC\|Quotient Clinical	September 2015	Phase 1
NCT02317627	Completed	Psoriasis Vulgaris	Kadmon Corporation LLC	December 2014	Phase 2

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KD025 (Belumosudil) ROCK2 inhibitor

Chemical Structure

Molecular Weight: 452.51