AZ 12799734 |
| Katalog-Nr.GC50589 |
AZ 12799734 ist ein selektiver, oral aktiver TGFBR1-Kinase-Inhibitor mit einem IC50 von 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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