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Submit ReviewGW 441756 is a potent, selective inhibitor of the NGF receptor tyrosine kinase A (TrkA) (IC50 = 2 nM). Displays > 100-fold selectivity over a range of other kinases.
Sold for research purposes under agreement from GlaxoSmithKline.
M. Wt | 275.31 |
Formula | C17H13N3O |
Storage | Store at RT |
Purity | ≥99% (HPLC) |
CAS Number | 504433-23-2 |
PubChem ID | 16219401 |
InChI Key | NXNQLECPAXXYTR-UHFFFAOYSA-N |
Smiles | CN1C=C(C=C2C(=O)NC3=CC=CN=C23)C2=C1C=CC=C2 |
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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 4.13 | 15 |
The following data is based on the product molecular weight 275.31. 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 |
---|---|---|---|
0.15 mM | 24.22 mL | 121.08 mL | 242.15 mL |
0.75 mM | 4.84 mL | 24.22 mL | 48.43 mL |
1.5 mM | 2.42 mL | 12.11 mL | 24.22 mL |
7.5 mM | 0.48 mL | 2.42 mL | 4.84 mL |
References are publications that support the biological activity of the product.
Wood et al (2004) Discovery and in vitro evaluation of potent TrkA kinase inhibitors: oxindole and aza-oxindoles. Bioorg.Med.Chem.Lett. 14 953 PMID: 15013000
If you know of a relevant reference for GW 441756, please let us know.
Keywords: GW 441756, GW 441756 supplier, Potent, selective, TrkA, inhibitors, inhibits, Neurotrophin, Receptors, Receptor, Tyrosine, Kinases, RTKs, GW441756, GlaxoSmithKline, GSK, Trk, 2238, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for GW 441756 include:
Edwards et al (2011) Effect of brain- and tumor-derived connective tissue growth factor on glioma invasion. J Natl Cancer Inst 103 1162 PMID: 21771732
Wang et al (2008) Cellular assays for high-throughput screening for modulators of Trk receptor tyrosine kinases. Curr Chem Genomics 1 27 PMID: 20161825
Lawn et al (2015) Neurotrophin signaling via TrkB and TrkC receptors promotes the growth of brain tumor-initiating cells. Nat Chem Biol 290 3814 PMID: 25538243
Rees et al (2016) Correlating chemical sensitivity and basal gene expression reveals mechanism of action. Oncotarget 12 109 PMID: 26656090
Donatien et al (2018) Granulocyte-macrophage colony-stimulating factor receptor expression in clinical pain disorder tissues and role in neuronal sensitization. Pain Rep 3 e676 PMID: 30534627
Do you know of a great paper that uses GW 441756 from Tocris? Please let us know.
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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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