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GW6604

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names：
2-phenyl-4-(3-(pyridin-2-yl)-1H-pyrazol-4-yl)pyridine
CAS號：
452342-37-9
MDL Number：
MF(分子式)： C19H14N4 MW(分子量)： 298.34126
EINECS: Reaxys Number:
Pubchem ID: Brand:BIOFOUNT

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中文別名	GW6604
英文別名	GW6604; GW-6604; GW 6604.
CAS號	452342-37-9
Inchi	InChI=1S/C19H14N4/c1-2-6-14(7-3-1)18-12-15(9-11-21-18)16-13-22-23-19(16)17-8-4-5-10-20-17/h1-13H,(H,22,23)
InchiKey	BDCBRQYHYNUWAM-UHFFFAOYSA-N
分子式 Formula	C19H14N4
分子量 Molecular Weight	298.34126
溶解度Solubility
性狀	Solid powder
儲藏條件 Storage conditions	Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).

產(chǎn)品說明	GW6604(CAS:452342-37-9):僅限應(yīng)用于工業(yè)或者科學(xué)研究過程中非醫(yī)療目的，不應(yīng)用于人類或動物的臨床診斷以及治過程療，該產(chǎn)品非藥用，非食用。
Introduction	GW6604 is a potent and selective ALK-5 inhibitor with potent anticancer activity. GW6604 is also a TGF-beta signaling pathway inhibitor. In vitro, GW6604 inhibited autophosphorylation of ALK5 with an IC(50) of 140 nM and in a cellular assay inhibited TGF-beta-induced transcription of PAI-1 (IC(50) 500 nM). In vivo, GW6604 (40 mg kg(-1) p.o.) increased liver regeneration in TGF-beta-overexpressing mice, which had undergone partial hepatectomy. In an acute model of liver disease, GW6604 reduced by 80% the expression of collagen IA1. Inhibition of ALK5 could be an attractive new approach to treatment of liver fibrotic diseases by both preventing matrix deposition and promoting hepatocyte regeneration. ( Br J Pharmacol. 2005 May;145(2)166-77. ).
Application1
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[1]Ciayadi R, Kelso GF, Potdar MK, Harris SJ, Walton KL, Harrison CA, Hearn MT. Identification of protein binding partners of ALK-5 kinase inhibitors. Bioorg Med Chem. 2013 Nov 1;21(21):6496-500. doi: 10.1016/j.bmc.2013.08.038. Epub 2013 Aug 29. PubMed PMID: 24055074.

[2]de Gouville AC, Huet S. Inhibition of ALK5 as a new approach to treat liver fibrotic diseases. Drug News Perspect. 2006 Mar;19(2):85-90. Review. PubMed PMID: 16628263.

[3] de Gouville AC, Boullay V, Krysa G, Pilot J, Brusq JM, Loriolle F, Gauthier JM, Papworth SA, Laroze A, Gellibert F, Huet S. Inhibition of TGF-beta signaling by an ALK5 inhibitor protects rats from dimethylnitrosamine-induced liver fibrosis. Br J Pharmacol. 2005 May;145(2):166-77. PubMed PMID: 15723089; PubMed Central PMCID: PMC1576127.

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