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| Product | Description | |
|---|---|---|
| GNF-5837 | GNF-5837 is a potent, selective, and orally bioavailable pan- tropomyosin receptor kinase (TRK) inhibitor which display antiproliferative effects in cellular Ba/F3 assays ( IC 50 values of 7 nM, 9 nM and 11 nM for cells containing the fusion proteins Tel-TrkC , Tel-TrkB and Tel-TrkA , respectively) [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1033769-28-6. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-13491. |  |
| Trk Inhibitor III, GNF-5837 - CAS 1033769-28-6 | The Trk Inhibitor III, GNF-5837 controls the biological activity of Trk. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications. Group: Fluorescence/luminescence spectroscopy. |  |
| 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) | 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.o.). Group: Biochemicals. Grades: Highly Purified. CAS No. 1033769-28-6. Pack Sizes: 10mg. US Biological Life Sciences. |  Worldwide |
| GNF 5837 | GNF 5837 is a potent and selective pan-Trk inhibitor that blocks tumor gowth in a mouse xenograft model derived from RIE cells expressing both TRKA and NGF. GNF 5837 displays antiproliferative effects in cellular Ba/F3 assays with IC50 values of 7, 9 and 11 nM for cells expressing Tel-TrkC, Tel-TrkB and Tel-TrkA respectively. Synonyms: GNF5837; GNF-5837; GNF 5837. 1-[2-fluoro-5-(trifluoromethyl)phenyl]-3-[4-methyl-3-[[(3Z)-2-oxo-3-(1H-pyrrol-2-ylmethylidene)-1H-indol-6-yl]amino]phenyl]urea. CAS No. 1033769-28-6. Molecular formula: C28H21F4N5O2. Mole weight: 535.503. |  |
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