R-268712

R-268712 is an orally active and selective ALK-5 inhibitor, with an IC50 of 2.5 nM. R-268712 inhibits the phosphorylation of Smad3 in a dose-dependent manner with an IC50 of 10.4 nM. R-268712 suppresses glomerulonephritis as well as glomerulosclerosis by inhibiting TGF-β signaling, which can be used in studies of renal fibrosis and cancer[1][2].

Product Specifications

CAS Number

[879487-87-3]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Anaplastic lymphoma kinase (ALK) ; TGF-beta/Smad; TGF-β Receptor

Type

Reference compound

Related Pathways

Protein Tyrosine Kinase/RTK; Stem Cell/Wnt; TGF-beta/Smad

Applications

Cancer-Kinase/protease

Field of Research

Cancer; Inflammation/Immunology; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/R-268712.html

Purity

99.92

Solubility

DMSO : 125 mg/mL (ultrasonic)

Smiles

FC1=C(C2=CN(CCO)N=C2)C=C(C3=CNN=C3C4=CC=CC(C)=N4)C=C1

Molecular Formula

C20H18FN5O

Molecular Weight

363.39

Precautions

H302, H315, H319, H335

References & Citations

[1]Terashima H, et al. Attenuation of pulmonary fibrosis in type I collagen-targeted reporter mice with ALK-5 inhibitors. Pulm Pharmacol Ther. 2019 Feb;54:31-38.|[2]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. |[3]Wang H, et al. Development of small molecule inhibitors targeting TGF-β ligand and receptor: Structures, mechanism, preclinical studies and clinical usage. Eur J Med Chem. 2020 Apr 1;191:112154.