A 77-01Potent ALK5 inhibitor CAS# 607737-87-1 |
2D Structure
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Quality Control & MSDS
3D structure
Package In Stock
Number of papers citing our products
Cas No. | 607737-87-1 | SDF | Download SDF |
PubChem ID | 10469233 | Appearance | Powder |
Formula | C18H14N4 | M.Wt | 286.33 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Solubility | DMSO : 25 mg/mL (87.31 mM; Need ultrasonic) | ||
Chemical Name | 4-[5-(6-methylpyridin-2-yl)-1H-pyrazol-4-yl]quinoline | ||
SMILES | CC1=CC=CC(=N1)C2=C(C=NN2)C3=CC=NC4=CC=CC=C34 | ||
Standard InChIKey | KJTYZDORHCDZPS-UHFFFAOYSA-N | ||
Standard InChI | 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) | ||
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. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. |
A 77-01 Dilution Calculator
A 77-01 Molarity Calculator
1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
1 mM | 3.4925 mL | 17.4624 mL | 34.9247 mL | 69.8495 mL | 87.3118 mL |
5 mM | 0.6985 mL | 3.4925 mL | 6.9849 mL | 13.9699 mL | 17.4624 mL |
10 mM | 0.3492 mL | 1.7462 mL | 3.4925 mL | 6.9849 mL | 8.7312 mL |
50 mM | 0.0698 mL | 0.3492 mL | 0.6985 mL | 1.397 mL | 1.7462 mL |
100 mM | 0.0349 mL | 0.1746 mL | 0.3492 mL | 0.6985 mL | 0.8731 mL |
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. |
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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.
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