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merck millipore,默克密理博,648451,Trk Inhibitor III, GNF-5837 - CAS 1033769-28-6 - Calbiochem
产品名称：Trk Inhibitor III, GNF-5837 - CAS 1033769-28-6 - Calbiochem
产品型号：648451
The Trk Inhibitor III, GNF-5837 controls the biological activity of Trk. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
merck millipore,默克密理博,648451,Trk Inhibitor III, GNF-5837 - CAS 1033769-28-6 - Calbiochem
- 产品介绍
重要规格表
经验配方 CAS号 C₂₈H₂₁F₄N₅O₂ 1033769-28-6 描述 概述 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 12 nM 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 7 nM, respectively) and in Ba/F3 and RIE cells expressing both TrkA and NGF (IC50 = 42 and 17 nM, respectively) over Mo7e-c-Kit and Rat-A10-PDGFR (IC50 = 1 and 0.5 µM) and Ba/F3-Tel-KDR and wt-Ba/F3 cells (IC50 = 3.0 and 5.6 µM). 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 (50 mg/kg, p.o.). 产品目录编号 648451 品牌系列 Calbiochem®
同义词 (Z)-1-(3-((3-((1H-Pyrrol-2-yl)methylene)-2-oxoindolin-6-yl)amino)-4-methylphenyl)-3-(2-fluoro-5-(trifluoromethyl)phenyl)urea 参考 参考 Albaugh, P., et al. 2012. ACS Med. Chem. Lett. 3, In press. 产品信息 CAS号 1033769-28-6 形式 Orange powder Hill配方 C₂₈H₂₁F₄N₅O₂ 化学配方 C₂₈H₂₁F₄N₅O₂ Molar Mass 535.5 结构配方图像 生物信息 纯度 ≥98% by HPLC 理化信息 溶解度 DMSO 储存和货运信息 货运代码 Ambient Temperature Only
毒性 Standard Handling
储存 +2°C to +8°C
避光 Protect from light
无需冷冻 No
特殊指南 Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C. 包装信息 惰性气体下包装 Packaged under inert gas
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