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R-268712
$80 – $1,207
Products Details
Product 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].
Web ID
– HY-12953
Storage Temperature
– -20°C, 3 years; 4°C, 2 years (Powder)
Shipping
– Room Temperature
Applications
– Cancer-Kinase/protease
Molecular Formula
– C20H18FN5O
References
– [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.
CAS Number
– 879487-87-3
Molecular Weight
– 363.39
Compound Purity
– 99.78
SMILES
– FC1=C(C2=CN(CCO)N=C2)C=C(C3=CNN=C3C4=CC=CC(C)=N4)C=C1
Clinical Information
– No Development Reported
Research Area
– Cancer; Inflammation/Immunology; Cardiovascular Disease
Solubility
– DMSO : 125 mg/mL (ultrasonic)
Target
– Anaplastic lymphoma kinase (ALK);TGF-beta/Smad;TGF-β Receptor
Isoform
– ALK5
Pathway
– Protein Tyrosine Kinase/RTK;Stem Cell/Wnt;TGF-beta/Smad
Product type
– Reference compound
Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.
