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KD025 (Belumosudil) ROCK2 inhibitor

Cat.No.S7936

Belumosudil (KD025, SLx-2119) is an orally available, and selective ROCK2 inhibitor with IC50 and K_i of 60 nM and 41 nM, respectively. Phase 2.

KD025 (Belumosudil) ROCK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 452.51

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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 Dihydrochloride Thiazovivin (TZV) Y-27632 NRL-1049 Ripasudil hydrochloride dihydrate Fasudil (HA-1077) Hydrochloride GSK429286A RKI-1447 GSK269962A HCl Y-39983 Dihydrochloride

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Solubility in DMSO or Water

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble

The solubility data above are all experimental results (not literature values).

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

Water : Insoluble

Ethanol : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 91 mg/mL (201.1 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 91 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

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

Water : Insoluble

Ethanol : Insoluble

The solubility data above are all experimental results (not literature values).

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

Water : Insoluble

Ethanol : Insoluble

The solubility data above are all experimental results (not literature values).

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.

Read more about KD025 (Belumosudil) solubility in DMSO or water

Search directly for a cell line, or select a cell line to find matched working concentrations

Read more about KD025 (Belumosudil) working concentrations for cell culture treatment

Mechanism of Action

Information	KD025 (Belumosudil) is a potent, selective ATP-competitive ROCK2 inhibitor. It affects TGF-β/SMAD and IL-17/STAT3 signaling by competitively binding to the kinase active site, effectively inhibiting fibrosis, epithelial-mesenchymal transition, and pro-inflammatory cytokine production.
Read more about KD025 (Belumosudil) IC50 for cell-based and cell-free assays
Primary Applications and Mechanism of Action

Read more about KD025 (Belumosudil) Mechanism of Action

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

Read more about storage & stability

Read more comparative analysis about KD025 (Belumosudil)

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

Serial Dilutions

Concentration (start):

Dilution-folds:

Computed Result

C1=C0/X	C1:		LOG(C1):
C2=C1/X	C2:		LOG(C2):
C3=C2/X	C3:		LOG(C3):
C4=C3/X	C4:		LOG(C4):
C5=C4/X	C5:		LOG(C5):
C6=C5/X	C6:		LOG(C6):
C7=C6/X	C7:		LOG(C7):
C8=C7/X	C8:		LOG(C8):