A 77-01

Key Product Details

Product Description

A 77-01 is a potent TGF-βRI (ALK-5) inhibitor (IC₅₀ = 34 nM). Inhibits TGF-β transcriptional activation. Inhibits TGF-β-induced proliferation of lung epithelial cells and SMAD phosphorylation. Inhibits TGF-β-induced epithelial-to-mesenchymal transition (EMT). Also inhibitor of p38 MAPK. Likely active metabolite of A 83-01 (Cat. No. 2939).

Product Specifications for A 77-01

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

Solubility

Preparing Stock Solutions for A 77-01

The following data is based on the product molecular weight 286.33.

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	3.49 mL	17.46 mL	34.92 mL
5 mM	0.70 mL	3.49 mL	6.98 mL
10 mM	0.35 mL	1.75 mL	3.49 mL
50 mM	0.07 mL	0.35 mL	0.70 mL

Calculators

Background References

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

• Sawyer Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-β type I receptor kinase domain. J.Med.Chem. 2003 PMID: 12954047
• Tojo The ALK-5 inhibitor A-83-01 inhibits Smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-β. Cancer Sci. 2005 PMID: 16271073

Product Documents for A 77-01