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Submit ReviewGNF 5837
说明： Potent Trk inhibitor; inhibits TrkA, TrkB and TrkC
化学名： N-[3-[[2,3-Dihydro-2-oxo-3-(1H-pyrrol-2-ylmethylene)-1H-indol-6-yl]amino]-4-methylphenyl]-N'-[2-fluoro-5-(trifluoromethyl)phenyl]urea
纯度： ≥98% (HPLC)
生物活性 for GNF 5837
GNF 5837 is a potent pan-Trk inhibitor. Displays antiproliferative effects in cellular Ba/F3 assays (IC50 values are 7, 9 and 11 nM for cells containing the fusion proteins Tel-TrkC, Tel-TrkB and Tel-TrkA, respectively). Exhibits selectivity for Trk receptors over a range of kinases, with some activity at PDGFR and c-Kit (IC50 values are 0.87 and 0.91 μM respectively). Orally bioavailable.
化合物库 for GNF 5837
GNF 5837 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for GNF 5837
| 分子量 | 535.49 |
| 公式 | C28H21F4N5O2 |
| 储存 | Store at +4°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1033769-28-6 |
| PubChem ID | 59397065 |
| InChI Key | YYDUWLSETXNJJT-MTJSOVHGSA-N |
| Smiles | O=C2NC1=CC(NC4=C(C)C=CC(NC(NC5=C(F)C=CC(C(F)(F)F)=C5)=O)=C4)=CC=C1/C2=C/C3=CC=CN3 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for GNF 5837
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 53.55 | 100 | |
| ethanol | 5.35 | 10 |
制备储备液 for GNF 5837
以下数据基于产品分子量 535.49。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.87 mL | 9.34 mL | 18.67 mL |
| 5 mM | 0.37 mL | 1.87 mL | 3.73 mL |
| 10 mM | 0.19 mL | 0.93 mL | 1.87 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.37 mL |
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产品说明书 for GNF 5837
参考文献 for GNF 5837
参考文献是支持产品生物活性的出版物。
Albaugh et al (2012) Discovery of GNF-5837, a selective TRK inhibitor with efficacy in rodent cancer tumor models. ACS Med.Chem.Lett. 3 140 PMID: 24900443
If you know of a relevant reference for GNF 5837, please let us know.
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关键词: GNF 5837, GNF 5837 supplier, GNF5837, Trk, receptors, TrkA, TrkB, TrkC, pan-Trk, inhibitors, inhibits, antiproliferative, Receptors, 4559, Tocris Bioscience
3 篇 GNF 5837 的引用文献
引用文献是使用了 Tocris 产品的出版物。 GNF 5837 的部分引用包括：
Hyung-Jun et al (2020) Neurotrophic interactions between neurons and astrocytes following AAV1-Rheb(S16H) transduction in the hippocampus in vivo. Br J Pharmacol 177 668-686 PMID: 31658360
Chao et al (2021) Kv1.1 channels regulate early postnatal neurogenesis in mouse hippocampus via the TrkB signaling pathway. Elife 10 PMID: 34018923
Tsai et al (2017) Brain-derived neurotrophic factor (BDNF) -TrKB signaling modulates cancer-endothelial cells interaction and affects the outcomes of triple negative breast cancer. PLoS One 12 e0178173 PMID: 28604807
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
Depression Poster
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.
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Huntington's disease (HD) is a severe monogenic neurodegenerative disorder, which is characterized by the prevalent loss of GABAergic medium spiny neurons (MSN) in the striatum. This poster summarizes the effects of mutant huntingtin aggregation implicated in the pathology of HD, as well as highlighting the use of iPSCs for HD modeling.
Parkinson's Disease Poster
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.