Chemical Property of Belumosudil
Chemical Property:
- Boiling Point:682.6±55.0 °C(Predicted)
- PKA:13?+-.0.40(Predicted)
- PSA：108.31000
- Density:1.318±0.06 g/cm3(Predicted)
- LogP:5.73340
- Storage Temp.:2-8°C(protect from light)
- Solubility.:Soluble in DMSO (25 mg/ml)
- XLogP3:4.8
- Hydrogen Bond Donor Count:3
- Hydrogen Bond Acceptor Count:6
- Rotatable Bond Count:7
- Exact Mass:452.19607403
- Heavy Atom Count:34
- Complexity:678
- Purity/Quality:
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99%, *data from raw suppliers
KD025 *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
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SDS file from LookChem
Useful:
- Canonical SMILES:CC(C)NC(=O)COC1=CC=CC(=C1)C2=NC3=CC=CC=C3C(=N2)NC4=CC5=C(C=C4)NN=C5
- Recent ClinicalTrials:Safety and Efficacy of Oral Belumosudil in Black or African American, American Indian or Alaska Native, and Native Hawaiian or Other Pacific Islander Male and Female Participants Aged 12 Years and Above With Chronic Graft Versus Host Disease (cGVHD) After At Least 2 Prior Lines of Systemic Therapy
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Description
KD 025 is an inhibitor of Rho-associated kinase 2 (ROCK2; IC50 = 0.105 μM). It is selective for ROCK2 over ROCK1 (IC50 = 24 μM). KD 025 (10 μM) decreases the expression of connective tissue growth factor (CTGF) and induces remodeling of the actin cytoskeleton in isolated human ileal fibrotic smooth muscle cells. It inhibits heat-killed C. albicans- or S. epidermidis-induced production of IL-17 in isolated human peripheral blood mononuclear cells (PBMCs) when used at concentrations ranging from 1.25 to 10 μM. KD 025 (100 and 200 mg/kg) reduces infarct volume in a mouse model of cerebral ischemia induced by transient middle cerebral artery occlusion (MCAO). It decreases disease severity in a mouse model of sclerodermatous chronic graft versus host disease (GVHD) when administered at a dose of 150 mg/kg. Formulations containing KD 025 have been used in the treatment of chronic GVHD.
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Uses
KD 025 is an inhibitor of Rho-associated protein kinase II (ROCK-II), a serine/threonine kinase that regulates the formation of actin stress fibers and focal adhesions, smooth muscle contraction, and gene expression (1, 2). KD025 has been shown to reduce infarct volume after transient middle cerebral artery occlusion (2).
