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A 77-01 Potent ALK5 inhibitor

Catalog No.A3132
Size Price Stock Qty
10mM (in 1mL DMSO)
$120.00
In stock
10mg
$102.00
In stock
25mg
$187.00
In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

A 77-01

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Chemical Properties

Cas No. 607737-87-1 SDF Download SDF
Synonyms A77-01;A-77-01
Chemical Name 4-[5-(6-methylpyridin-2-yl)-1H-pyrazol-4-yl]quinoline
Canonical SMILES CC1=CC=CC(=N1)C2=C(C=NN2)C3=CC=NC4=CC=CC=C34
Formula C18H14N4 M.Wt 286.33
Solubility Soluble in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

Transforming growth factor (TGF)-β signaling facilitates tumor growth and metastasis in advanced cancer. Use of inhibitors of TGF-β signaling may thus be a novel strategy for the treatment of patients with such cancer. A-77-01 is a close analogue of A-83-01 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.
In vitro: A-77-01 and A-83–01 almost completely inhibited the transcriptional activation induced by the constitutively active TGF-β type I receptor (ALK5-TD). A-77-01 and A-83-01 were five to 10 times more potent than the ALK-5 inhibitor SB-431542. In contrast, treatment with 1 μM A-77-01 or 1 μM A-83-01 had no effects on BMP-induced transcriptional activity. However, A-83-01, but not A-77–01, weakly suppressed the transcriptional activity induced by BMP4 at concentrations above 3 μM. A-83-01 and A-77-01 had weak effects on osmotic shock-induced p38 MAPK activity only at high concentrations. A-83-01 and A-77-01 restored the expression of E-cadherin and repressed that of fibronectin and N-cadherin more efficiently than SB-431542 [1].
In vivo: No animal in-vivo data available currently.
Clinical trial: A-77-01 is currently in the preclinical developlent stage and no clinical data are available.
Reference:
[1] Tojo M, Hamashima Y, Hanyu A, Kajimoto T, Saitoh M, Miyazono K, Node M, Imamura T. The ALK-5 inhibitor A-83-01 inhibits Smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-beta. Cancer Sci. 2005;96(11):791-800.