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A77-01 (607737-87-1)

A 77-01 is 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.

Not Intended for Therapeutic Use. For research use only.

CAS: 607737-87-1 Category

A77-01 (607737-87-1) Description:

A-77-01 is a potent inhibitor of the TGF-β1 receptor ALK5 (IC50 = 25 nM).It has no effects on BMP-regulated transcriptional activity or MAPK pathways. A-77-01 efficiently prevents the growth inhibitory effects of TGF-β on lung epithelial Mv1Lu cells. It completely blocks phosphorylation of SMAD2 by TGF-β in human keratinocyte HaCaT cells at 1 µM. A-77-01 prevents morphological and gene expression changes characteristic of epithelial-to-mesenchymal transition in NMuMG cells treated with TGF-β.

Target: ALK5 A-77-01 is a close analogue of A-83-01(Axon 1421) and has a very similar biological profile of A-83-01. A-83-01 is found to decompose to A-77-01 under certain circumstances and A-77-01 is likely an active component or metabolite of its prodrug A-83-01.

A77-01 (607737-87-1) Specifications:

Product Name A77-01
Synonyms A 77-01; A-77-01.
Chemical Name 4-[5-(6-methylpyridin-2-yl)-1~{H}-pyrazol-4-yl]quinoline
Purity >98%
CAS Number 607737-87-1
Molecular Formula C18H14N4
Molecular Weight 286.338 g/mol
Monoisotopic Mass 286.122 g/mol
MDL number MFCD07367791
InChi Code InChI=1S/C18H14N4/c1-12-5-4-8-17(21-12)18-15(11-20-22-18)13-9-10-19-16-7-3-2-6-14(13)16/h2-11H,1H3,(H,20,22)
Form powder
Color white
Solubility  Soluble in DMSO (20 mg/ml), and ethanol (20 mg/ml).
Storage Temp.  0 – 4 C for short term (days to weeks), or -20 C for long term (months).
Shelf life >2 years if stored properly
Handling Protect from air and light
Application An inhibitor of ALK5 with an IC50 of 25nM


RIDADR NONH for all modes of transport


  • M Tojo et al. The ALK5 inhibitor A-83-01 inhibits smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-β. Cancer. Sci. 2005, 96, 791-800.
  • J Sawyer et al. Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-β type I receptor kinase domain. J of Medicinal Chemistry. 2003, 46, 3953-3956.