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R-268712

CAT: 0804-HY-12953-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-12953-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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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].
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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
ALK5

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