MedKoo Cat#: 414223 | Name: Belumosudil mesylate
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Belumosudil, also known as KD-025 and WHO11343, is an orally bioavailable inhibitor of ROCK-II that is greater than 200-fold selective over ROCK-I (IC50s = 105 nM and 24 µM, respectively). Belumosudil (SLx-2119; 40 µM) induces significant down-regulations of Tsp-1 and CTGF mRNA levels in PASMC. Belumosudil (KD025; 100, 200 or 300 mg/kg, i.p.) dose-dependently reduces infarct volume after transient middle cerebral artery occlusion. It is used in the treatment of Autoimmune Diseases. Belumosudil was approved in 2021 in USA To treat chronic graft-versus-host disease after failure of at least two prior lines of systemic therapy

Chemical Structure

Belumosudil mesylate
Belumosudil mesylate
CAS#2109704-99-4 (mesylate)

Theoretical Analysis

MedKoo Cat#: 414223

Name: Belumosudil mesylate

CAS#: 2109704-99-4 (mesylate)

Chemical Formula: C27H28N6O5S

Exact Mass: 0.0000

Molecular Weight: 548.62

Elemental Analysis: C, 59.11; H, 5.14; N, 15.32; O, 14.58; S, 5.84

Price and Availability

Size Price Availability Quantity
1g USD 450.00 2 Weeks
2g USD 750.00 2 Weeks
5g USD 1,650.00 2 Weeks
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Synonym
Belumosudil mesylate; KD 025; KD-025; KD025; WHO11343; WHO-11343; WHO 11343; SLx 2119; SLx2119; SLx-2119;
IUPAC/Chemical Name
2-(3-(4-(1H-indazol-5-ylamino)quinazolin-2-yl)phenoxy)-N-(propan-2-yl)acetamide methanesulfonate (1:1)
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)
SMILES Code
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
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 548.62 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Jagasia M, Lazaryan A, Bachier CR, Salhotra A, Weisdorf DJ, Zoghi B, Essell J, Green L, Schueller O, Patel J, Zanin-Zhorov A, Weiss JM, Yang Z, Eiznhamer D, Aggarwal SK, Blazar BR, Lee SJ. ROCK2 Inhibition With Belumosudil (KD025) for the Treatment of Chronic Graft-Versus-Host Disease. J Clin Oncol. 2021 Apr 20:JCO2002754. doi: 10.1200/JCO.20.02754. Epub ahead of print. PMID: 33877856.