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Submit ReviewGNF 5837
Description: Potent Trk inhibitor; inhibits TrkA, TrkB and TrkC
Chemical Name: 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
Purity: ≥98% (HPLC)
Biological Activity 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.
Compound Libraries for GNF 5837
GNF 5837 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for GNF 5837
| M. Wt | 535.49 |
| Formula | C28H21F4N5O2 |
| Storage | Store at +4°C |
| Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for GNF 5837
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 53.55 | 100 | |
| ethanol | 5.35 | 10 |
Preparing Stock Solutions for GNF 5837
The following data is based on the product molecular weight 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.
| Concentration / Solvent Volume / Mass | 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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Product Datasheets for GNF 5837
References for GNF 5837
References are publications that support the biological activity of the product.
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
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Keywords: GNF 5837, GNF 5837 supplier, GNF5837, Trk, receptors, TrkA, TrkB, TrkC, pan-Trk, inhibitors, inhibits, antiproliferative, Receptors, 4559, Tocris Bioscience
3 Citations for GNF 5837
Citations are publications that use Tocris products. Selected citations for GNF 5837 include:
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
Do you know of a great paper that uses GNF 5837 from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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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.
Huntington's Disease Poster
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.