AZ 12799734

Key Product Details

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 for AZ 12799734

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

Solubility

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.

Select a batch to recalculate based on the batch molecular weight:

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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

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 Documents for AZ 12799734