A 77-01

Name: A 77-01
Brand: Tocris Bioscience
SKU: 6712

Tocris Bioscience, part of Bio-Techne | Catalog # 6712

Citations (1)

COA / SDS

Potent inhibitor of TGF-βRI

Key Product Details

Description:	Potent inhibitor of TGF-βRI
Chemical Name:	4-[3-(6-Methyl-2-pyridinyl)-1H-pyrazol-4-yl]quinoline
Purity:	≥98% (HPLC)
Molecular Weight:	286.33

View Full Technical Details for A 77-01

Technical Data
Citations

Biological Activity for A 77-01

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).

Compound Libraries for A 77-01

A 77-01 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for A 77-01

M. Wt	286.33
Formula	C₁₈H₁₄N₄
Storage	Store at +4°C
Purity	≥98% (HPLC)
CAS Number	607737-87-1
PubChem ID	10469233
InChi Key	KJTYZDORHCDZPS-UHFFFAOYSA-N
Smiles	CC1=NC(C2=NNC=C2C3=CC=NC4=C3C=CC=C4)=CC=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 A 77-01

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	28.63	100
	1eq. HCl	14.32	50

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 will affect the solvent volumes required to prepare stock solutions.

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

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References for A 77-01

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