AZ 12799734

Name: AZ 12799734
Brand: Tocris Bioscience
SKU: 6870

Tocris Bioscience, part of Bio-Techne | Catalog # 6870

COA / SDS

Potent TGF-βRI inhibitor

Key Product Details

Description:	Potent TGF-βRI inhibitor
Chemical Name:	4-[[4-[(2.6-Dimethyl-3-pyridinyl)oxy]-2-pyridinyl]amino]benzenesulfonamide
Purity:	≥98% (HPLC)
Molecular Weight:	370.43

View Full Technical Details for AZ 12799734

Technical Data
Citations

Biological Activity for AZ 12799734

AZ 12799734 is a 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.

Compound Libraries for AZ 12799734

AZ 12799734 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for AZ 12799734

M. Wt	370.43
Formula	C₁₈H₁₈N₄O₃S
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	1117684-36-2
PubChem ID	25192277
InChi Key	UEOZXMAOIHDDQE-UHFFFAOYSA-N
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 for AZ 12799734

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

Preparing Stock Solutions for AZ 12799734

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.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.70 mL	13.50 mL	27.00 mL
5 mM	0.54 mL	2.70 mL	5.40 mL
10 mM	0.27 mL	1.35 mL	2.70 mL
50 mM	0.05 mL	0.27 mL	0.54 mL

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References for AZ 12799734

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

Anderton Induction of heart valve lesions by small-molecule ALK5 inhibitors. Toxicol.Pathol. 2011 PMID: 21859884
Spender Preclinical evaluation of AZ12601011 and AZ12799734, inhibitors of transforming growth factor β superfamily type 1 receptors. Mol.Pharmacol. 2019 PMID: 30459156
Goldberg Rapid generation of a high quality lead for transforming growth factor-beta (TGF-beta) type I receptor (ALK5). J.Med.Chem. 2009 PMID: 19736928