R-268712

R-268712

• CAS Number: 879487-87-3
• UNSPSC Description: 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].
• Target Antigen: 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
• Field of Research: Cancer; Inflammation/Immunology; Cardiovascular Disease
• Assay Protocol: https://www.medchemexpress.com/R-268712.html
• Purity: 99.88
• 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 Weight: 363.39
• 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.
• Shipping Conditions: Room Temperature
• Storage Conditions: -20°C, 3 years; 4°C, 2 years (Powder)
• Clinical Information: No Development Reported