AZ 12799734 |
| Catalog No.GC50589 |
AZ 12799734 es un inhibidor selectivo de la quinasa TGFBR1 activo por vía oral con una IC50 de 47 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1117684-36-2
Sample solution is provided at 25 µL, 10mM.
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Potent inhibitor of transforming growth factor-β type I receptor (TGF-βRI; ALK5) (IC50 = 17 nM in cellular inhibition assay and 47 nM in TGF-β-induced luciferase activity assay). Also inhibits ALK4, ALK6 and ALK7 at concentrations under 10 μM. Inhibits BMP signaling, phosphorylation of SMAD1 and SMAD2, and TGF-β-induced epithelial cell migration in vitro. Displays cardiotoxicity in vivo. Orally bioavailable.
Goldberg et al (2009) Rapid generation of a high quality lead for transforming growth factor-beta (TGF-beta) type I receptor (ALK5). J.Med.Chem. 52 7901 PMID:19736928 |Anderton et al (2011) Induction of heart valve lesions by small-molecule ALK5 inhibitors. Toxicol.Pathol. 39 916 PMID:21859884 |Spender et al (2019) Preclinical evaluation of AZ12601011 and AZ12799734, inhibitors of transforming growth factor β superfamily type 1 receptors. Mol.Pharmacol. 95 222 PMID:30459156
Average Rating: 5 (Based on Reviews and 3 reference(s) in Google Scholar.)
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