AZ 12799734

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Cat.No. 6870 - AZ 12799734 | C18H18N4O3S | CAS No. 1117684-36-2
Description: Potent TGF-βRI inhibitor
Chemical Name: 4-[[4-[(2.6-Dimethyl-3-pyridinyl)oxy]-2-pyridinyl]amino]benzenesulfonamide
Purity: ≥98% (HPLC)
Literature (6)
Pathways (1)

Biological Activity

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.

Technical Data

M. Wt 370.43
Formula C18H18N4O3S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1117684-36-2
PubChem ID 25192277
Smiles CC1=NC(C)=C(OC2=CC=NC(NC3=CC=C(C=C3)[S](N)(=O)=O)=C2)C=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 37.04 100

Preparing Stock Solutions

The following data is based on the product molecular weight 370.43. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.7 mL 13.5 mL 27 mL
5 mM 0.54 mL 2.7 mL 5.4 mL
10 mM 0.27 mL 1.35 mL 2.7 mL
50 mM 0.05 mL 0.27 mL 0.54 mL

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References are publications that support the biological activity of the product.

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

If you know of a relevant reference for AZ 12799734, please let us know.

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Literature in this Area

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Pathways for AZ 12799734


TGF-β Signaling Pathway

The TGF-β signaling pathway is involved in the regulation of growth and proliferation of cells along with migration, differentiation and apoptosis.