Belumosudil mesylate (KD025 mesylate)

Alias: Belumosudil mesylate; KD-025; KD 025; KD025; WHO-11343; WHO 11343; WHO11343; SLx2119; SLx-2119; SLx 2119

Cat No.:V40835 Purity: ≥98%

COA Product Data Instructions for use SDS

Belumosudil mesylate (previously SLx2119; KD025; SLx-2119; KD-025; Rezurock), the mesylate salt of belumosudil, is anorally bioavailable ROCK2 inhibitor approved in 2021 for the treatment of chronic graft versus host disease (cGvHD).

Belumosudil mesylate (KD025 mesylate) Chemical Structure CAS No.: 2109704-99-4
Product category: ROCK

This product is for research use only, not for human use. We do not sell to patients.

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1-708-310-1919 sales@invivochem.com

Other Forms of Belumosudil mesylate (KD025 mesylate):

Belumosudil (KD025, SLx-2119)

Official Supplier of:

Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

Science Adv 2022: 8, eabm9427.

Nature 597, 119–125 (2021)

Cell Stem Cell 2020,26(6):845-861.e12.

Science Trans Med 2023,15(701):eadd7872.

STTT 2023,8(1):91.

Cell Reports 2023,42(4):112313

Science Trans Med 2023, 15: eadd7872.

Cancer Cell 2021,39(4):529-547.e7.

Cancer Discov 2022,12(4):1106-1127.

Immunity 2023,56(3):620-634.e11.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

InvivoChem's Belumosudil mesylate (KD025 mesylate) has been cited by 1 publications

[1]
Belumosudil (KD025, SLx-2119):Am J Physiol Renal Physiol.2019 Oct 1;317(4):F839-F851.

Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

NMR

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information
Biological Data

Product Description

Biological Activity I Assay Protocols (From Reference)

Targets	ROCK2 (IC50 = 105 nM); ROCK1 (IC50 = 24 μM)
ln Vitro	Belumosudil (SLx-2119; 40 µM) significantly reduces the levels of Tsp-1 and CTGF mRNA in PASMC. Five times more background is seen in the microarray hybridized with aRNA from HMVEC treated with belumosudil than in the other arrays[1].
ln Vivo	Belumosudil (KD-025; 100, 200 or 300 mg/kg, i.p.) decreases the infarct volume dose-dependently following a brief middle cerebral artery blockage. Belumosudil works in aged, diabetic, or female mice just as well as it does in healthy adult male mice[2].
References	[1]. Blood Coagul Fibrinolysis . 2008 Oct;19(7):709-18. [2]. Ann Clin Transl Neurol . 2014 Jan 1;1(1):2-14.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula	C₂₇H₂₈N₆O₅S
Molecular Weight	548.61
Elemental Analysis	C, 59.11; H, 5.14; N, 15.32; O, 14.58; S, 5.84
CAS #	2109704-99-4
Related CAS #	Belumosudil;911417-87-3
Appearance	Solid powder
SMILES	O=C(NC(C)C)COC1=CC=CC(C2=NC(NC3=CC4=C(NN=C4)C=C3)=C5C=CC=CC5=N2)=C1.CS(=O)(O)=O
InChi Key	ILQJXEIRBCHLOM-UHFFFAOYSA-N
InChi Code	InChI=1S/C26H24N6O2.CH4O3S/c1-16(2)28-24(33)15-34-20-7-5-6-17(13-20)25-30-23-9-4-3-8-21(23)26(31-25)29-19-10-11-22-18(12-19)14-27-32-22;1-5(2,3)4/h3-14,16H,15H2,1-2H3,(H,27,32)(H,28,33)(H,29,30,31);1H3,(H,2,3,4)
Chemical Name	2-(3-(4-(1H-indazol-5-ylamino)quinazolin-2-yl)phenoxy)-N-(propan-2-yl)acetamide
Synonyms	Belumosudil mesylate; KD-025; KD 025; KD025; WHO-11343; WHO 11343; WHO11343; SLx2119; SLx-2119; SLx 2119
HS Tariff Code	2934.99.9001
Storage	Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)	DMSO: ~12.5 mg/mL (~22.8 mM)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	1.8228 mL	9.1139 mL	18.2279 mL
	5 mM	0.3646 mL	1.8228 mL	3.6456 mL
	10 mM	0.1823 mL	0.9114 mL	1.8228 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Mass

Concentration

Volume

Molecular Weight*

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Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make 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 in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

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Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Clinical Trial Information

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06105554	Not yet recruiting	Drug: Belumosudil mesylate	Multiple Myeloma	M.D. Anderson Cancer Center	April 30, 2024	Phase 1 Phase 2
NCT05918627	Completed	Drug: Belumosudil mesylate Drug: Placebo	Immune System Disorder (Healthy Volunteer)	Kadmon, a Sanofi Company	September 21, 2009	Phase 1
NCT05918614	Completed	Drug: Belumosudil mesylate Drug: Placebo	Immune System Disorder (Healthy Volunteer)	Kadmon, a Sanofi Company	March 28, 2014	Phase 1
NCT05918588	Completed	Drug: Belumosudil mesylate Drug: Placebo	Immune System Disorder (Healthy Volunteer)	Kadmon, a Sanofi Company	November 21, 2013	Phase 1

Biological Data

KD025 selectively inhibited ROCK2 over ROCK1, whereas isoform-nonselective Y27632 inhibited ROCK1 and ROCK2 to a similar extent in a recombinant enzyme system with truncated catalytic domains. IC50 values for each drug are indicated on the graphs. Ann Clin Transl Neurol . 2014 Jan 1;1(1):2-14.

KD025, 100 or 200 mg/kg, was administered (arrows) via oral gavage every 12 h for 48 h (five doses). Ann Clin Transl Neurol . 2014 Jan 1;1(1):2-14.

Vehicle or KD025 was administered (arrows) every 12 h starting 24 h before the onset of 1 h transient fMCAO and continued until sacrifice at 48 h (six doses). Ann Clin Transl Neurol . 2014 Jan 1;1(1):2-14.