| Identification | Back Directory | [Name]
3-(6-Methylpyridin-2-yl)-N-phenyl-4-(quinolin-4-yl)-1H-pyrazole-1-carbothioamide, Sodium salt | [CAS]
2828431-89-4 | [Synonyms]
3-(6-Methylpyridin-2-yl)-N-phenyl-4-(quinolin-4-yl)-1H-pyrazole-1-carbothioamide, Sodium salt
1H-Pyrazole-1-carbothioamide, 3-(6-methyl-2-pyridinyl)-N-phenyl-4-(4-quinolinyl)-, sodium salt (1:1) | [Molecular Formula]
C25H20N5NaS | [MOL File]
2828431-89-4.mol | [Molecular Weight]
445.52 |
| Hazard Information | Back Directory | [Uses]
A 83-01 sodium is a potent inhibitor of TGF-β type I receptor ALK5 kinase, ALK4 and ALK7, with IC50s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively[1]. | [in vivo]
A 83-01 (50, 150 and 500 μg/mouse, i.p.) sodium significantly improves survival of the mice without body weight or neurobehavioral appearances[2].
A 83-01 (0.5 mg/kg, i.p.) sodium shows a significantly strong antitumor effect in mice bearing M109 cells[3]. | [IC 50]
ALK5: 12 nM (IC50); ALK4: 45 nM (IC50); ALK7: 7.5 nM (IC50) | [References]
[1] Tojo M, et al. The ALK-5 inhibitor A-83-01 inhibits Smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-beta. Cancer Sci. 2005 Nov;96(11):791-800. DOI:10.1111/j.1349-7006.2005.00103.x
[2] Yamamura S, et al. The activated transforming growth factor-beta signaling pathway in peritoneal metastases is a potential therapeutic target in ovarian cancer. Int J Cancer. 2012 Jan 1;130(1):20-8. DOI:10.1002/ijc.25961
[3] Taniguchi Y, et al. Enhanced antitumor efficacy of folate-linked liposomal doxorubicin with TGF-β type I receptor inhibitor. Cancer Sci. 2010 Oct;101(10):2207-13. DOI:10.1111/j.1349-7006.2010.01646.x |
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