879487-87-3

879487-87-3 structure

Name: R 268712
Chemical Name: R-268712
CAS Number: 879487-87-3
Molecular Formula: C₂₀H₁₈FN₅O
Molecular Weight: 363.388
Catalog: Signaling Pathways TGF-beta/Smad TGF-β Receptor
Create Date: 2018-03-03 20:44:59
Modify Date: 2024-02-01 18:52:27
R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM.IC50 value: 2.5 nM [1]Target: ALK5in vitro: R-268712 is a novel and specific inhibitor of activin receptor-like kinase 5 (ALK5), a transforming growth factor β (TGF-β) type I receptor. R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM, an approximately 5000-fold more selectivity for ALK5 than p38 mitogen-activated protein kinase (MAPK). R-268712 is a weak inhibitor of p38 MAP kinase (IC50: 12.1 μM).[1]in vivo: Oral administration of R-268712 at doses of 1, 3 and 10 mg/kg also inhibited the development of renal fibrosis in a dose-dependent manner in a unilateral ureteral obstruction (UUO) model. [1]

Name	R-268712
Synonyms	1H-Pyrazole-1-ethanol, 4-[2-fluoro-5-[5-(6-methyl-2-pyridinyl)-1H-pyrazol-4-yl]phenyl]- 2-(4-{2-Fluoro-5-[5-(6-methyl-2-pyridinyl)-1H-pyrazol-4-yl]phenyl}-1H-pyrazol-1-yl)ethanol

Description	R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM.IC50 value: 2.5 nM [1]Target: ALK5in vitro: R-268712 is a novel and specific inhibitor of activin receptor-like kinase 5 (ALK5), a transforming growth factor β (TGF-β) type I receptor. R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM, an approximately 5000-fold more selectivity for ALK5 than p38 mitogen-activated protein kinase (MAPK). R-268712 is a weak inhibitor of p38 MAP kinase (IC50: 12.1 μM).[1]in vivo: Oral administration of R-268712 at doses of 1, 3 and 10 mg/kg also inhibited the development of renal fibrosis in a dose-dependent manner in a unilateral ureteral obstruction (UUO) model. [1]
Related Catalog	Signaling Pathways >> TGF-beta/Smad >> TGF-β Receptor Research Areas >> Cancer
References	[1]. Terashima H, et al. R-268712, an orally active transforming growth factor-β type I receptor inhibitor, prevents glomerular sclerosis in a Thy1 nephritis model. Eur J Pharmacol. 2014 Jul 5;734:60-6.