[CAS NO. 911417-87-3] Belumosudil (KD025)

Name: Belumosudil (KD025)
Brand: Arctom Scientific
SKU: SLK-S7936

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PRODUCTS SPECIFICATIONS [911417-87-3]

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Catalog

SLK-S7936

Brand

Selleck

CAS

911417-87-3

DESCRIPTION [911417-87-3]

Overview

MDL	MFCD23098791
Molecular Weight	452.51
Molecular Formula	C26H24N6O2
SMILES	N(C=1C2=C(N=C(N1)C3=CC(OCC(NC(C)C)=O)=CC=C3)C=CC=C2)C=4C=C5C(=CC4)NN=C5

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.2099 mL	11.0495 mL	22.0990 mL
5 mM	0.4420 mL	2.2099 mL	4.4198 mL
10 mM	0.2210 mL	1.1049 mL	2.2099 mL
50 mM	0.0442 mL	0.2210 mL	0.4420 mL

Description

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

Targets

ROCK2 ^[1] (Cell-free assay)	ROCK2 ^[1] (Cell-free assay)
41 nM(Ki)	60 nM

In vitro

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. KD025 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.

References

[1] Lee JH, et al. Ann Clin Transl Neurol. 2014, 1(1), 2-14.
[2] Zanin-Zhorov A, et al. Proc Natl Acad Sci U S A. 2014, 111(47), 16814-16819.
[3] Flynn R, et al. Blood. 2016. pii: blood-2015-10-678706.
[4] Swiatlowska P, et al. Sci Adv. 2022 Apr 15;8(15):eabm3471.

Synonyms

Acetamide, 2-[3-[4-(1H-indazol-5-ylamino)-2-quinazolinyl]phenoxy]-N-(1-methylethyl)-

2-[3-[4-(1H-Indazol-5-ylamino)-2-quinazolinyl]phenoxy]-N-(1-methylethyl)acetamide

2-[3-[4-[(1H-Indazol-5-yl)amino]quinazolin-2-yl]phenoxy]-N-isopropylacetamide

SLx 2119

KD 025

Belumosudil

2-{3-[4-(1H-indazol-5-ylamino)quinazolin-2-yl]phenoxy}-N-(propan-2-yl)acetamide

2-[3-[4-(1H-Indazol-5-ylamino)quinazolin-2-yl]phenoxy]-N-propan-2-ylacetamide