For research use only. Not for therapeutic Use.
AZ12799734 is a selective, orally active TGFBR1 kinase inhibitor with an IC50 of 47 nM. AZ12799734 is also a pan BMP and TGFβ inhibitor[1].
AZ12799734 inhibits ligand activated SMAD3/4 transcription[1].
AZ12799734 (10 nM; 24 h) inhibits phosphorylation of both SMAD1 and SMAD2[1].
AZ12799734 (500 nM; 36 h) inhibits TGFβ-induced migration in HaCaT epithelial cells[1].
AZ12799734 (0-400 mg/kg/day; p.o.; 3-7 days) induces histopathologic heart valve lesions in rat[2].
AZ12799734 (50 mg/kg; p.o.; once) shows total and free pharmacokinetic (PK) levels in the nude mouse with time over in vitro IC50 of 0.01885 μM[1].
| Catalog Number | I022792 |
| CAS Number | 1117684-36-2 |
| Synonyms | 4-[[4-(2,6-dimethylpyridin-3-yl)oxypyridin-2-yl]amino]benzenesulfonamide |
| Molecular Formula | C18H18N4O3S |
| Purity | ≥95% |
| InChI | InChI=1S/C18H18N4O3S/c1-12-3-8-17(13(2)21-12)25-15-9-10-20-18(11-15)22-14-4-6-16(7-5-14)26(19,23)24/h3-11H,1-2H3,(H,20,22)(H2,19,23,24) |
| InChIKey | UEOZXMAOIHDDQE-UHFFFAOYSA-N |
| SMILES | CC1=NC(=C(C=C1)OC2=CC(=NC=C2)NC3=CC=C(C=C3)S(=O)(=O)N)C |
| Reference | [1]. Spender LC, et al. Preclinical Evaluation of AZ12601011 and AZ12799734, Inhibitors of Transforming Growth Factor β Superfamily Type 1 Receptors. Mol Pharmacol. 2019 Feb;95(2):222-234. [2]. Anderton MJ, et al. Induction of heart valve lesions by small-molecule ALK5 inhibitors. Toxicol Pathol. 2011 Oct;39(6):916-24. |
