| 产品详情 |
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| Product Name | Trk Inhibitor III, GNF-5837 |
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| Description | Purity ~98% (HPLC). An orally bioavailable oxindole compound that and acts as a potent, reversible and type II DFG-out inhibitor of pan-Trk activity (IC50=8 and 12nM for TrkA and TrkB). Shown to target Trk (tropomyosin receptor kinase) ATP binding cleft and an immediately adjacent hydrophobic pocket. Preferentially arrests the proliferation of Ba/F3 cells fused with Tel-TrkA, Tel-TrkB and Tel-TrkC (IC50=11, 9 and 7nM, respectively) and in Ba/F3 and RIE cells expressing both TrkA and NGF (IC50=42 and 17nM, respectively) over Mo7e-c-Kit and Rat-A10-PDGFR (IC50=1 and 0.5uM) and Ba/F3-Tel-R and wt-Ba/F3 cells (IC50=3.0 and 5.6uM). Displays ~100-fold greater selectivity among a panel of 59 closely related kinases and in 33 cellular kinase assays. Weakly active against relevant cytochrome P450 isozymes and hERG channel, and exhibit adequate microsomal stability, pharmacokinetic profile and efficacy in mice and rats. Suppresses tumor growth in a mouse RIE-TrkAmNGF xenograft model (50mg/kg, p. |
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| Size | 10mg |
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| Concentration | n/a |
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| Applications | n/a |
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| Other Names | Trk Inhibitor III, GNF-5837 ((Z)-1-(3-((3-((1H-Pyrrol-2-yl)methylene)-2-oxoindolin-6-yl)amino)-4-methylphenyl)-3-(2-fluoro-5-(trifluoromethyl)phenyl)urea) |
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| Gene, Accession, CAS # | n/a |
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| Catalog # | 217847 |
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| Order / More Info | Trk Inhibitor III, GNF-5837 from UNITED STATES BIOLOGICAL |
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| Product Specific References | n/a |
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