SML2819
AZ12799734
≥98% (HPLC)
Synonym(s):
4-[[4-[(2,6-Dimethyl-3-pyridinyl)oxy]-2-pyridinyl]amino]benzenesulfonamide, 4-[[4-[(2,6-Dimethylpyridin-3-yl)oxy]pyridin-2-yl]amino]benzenesulfonamide, AZ 12799734, AZ-12799734
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About This Item
Empirical Formula (Hill Notation):
C18H18N4O3S
CAS Number:
Molecular Weight:
370.43
UNSPSC Code:
12352200
NACRES:
NA.77
Recommended Products
Quality Level
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Biochem/physiol Actions
AZ12799734 is an orally active TGF-β type I receptors active site inhibitor (ALK1/2/3/4/5/6 Kd = 7.1/6.2/40/1/0.74/0.017 μM) that inhibits ALK5-dependent Smad2 nuclear translocation upon TGF-β1 stimulation (IC50 = 17 nM; MDA-MB-468), as well as ALK1/2/3/6-mediated Smad1 and ALK4/5/7-mediated Smad2 phosphorylation (10 μM; NIH3T3 expressing respective constitutively active receptors). AZ12799734 oral administration in rats results in heart valve lesions (200 mg/kg/day for 5 days) and physeal dysplasia (400 mg/kg/day for 6 days), consistent with a critical role of ALK5 in maintaining the integrity of heart valve and physis.
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
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Frederick W Goldberg et al.
Journal of medicinal chemistry, 52(23), 7901-7905 (2009-09-10)
A novel class of 4-pyridinoxy-2-anilinopyridine-based TGF-beta type I receptor (also known as activin-like kinase 5 or ALK5) inhibitors is reported. The binding mode of this scaffold was successfully predicted by analyzing possible docked binding modes of literature inhibitors and novel
Mark J Anderton et al.
Toxicologic pathology, 39(6), 916-924 (2011-08-24)
Aberrant signaling by transforming growth factor-β (TGF-β) and its type I (ALK5) receptor has been implicated in a number of human diseases and this pathway is considered a potential target for therapeutic intervention. Transforming growth factor-β signaling via ALK5 plays
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