AZ 12799734
Tocris Bioscience, part of Bio-Techne | Catalog # 6870
Potent TGF-βRI inhibitor
Product Description
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.Product Specifications
Molecular Weight
370.43
Formula
C18H18N4O3S
Storage
Store at -20°C
Purity
≥98% (HPLC)
Chemical Name
4-[[4-[(2.6-Dimethyl-3-pyridinyl)oxy]-2-pyridinyl]amino]benzenesulfonamide
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.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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
Product Specific Notices for AZ 12799734
For research use only
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