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Potent and selective pan-Trk inhibitor (IC50 values are 1, 2 and 6 nM for Trk C, B and A, respectively). Selective for Trk over a panel of ion channels, receptors and other enzymes. Peripherally restricted. Exhibits efficacy in a rodent model of inflammatory pain. Orally bioavailable.
Sold for research purposes under agreement from Pfizer Inc.
|Storage||Store at RT|
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|
Preparing Stock Solutions
The following data is based on the product molecular weight 479.93. 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||2.08 mL||10.42 mL||20.84 mL|
|5 mM||0.42 mL||2.08 mL||4.17 mL|
|10 mM||0.21 mL||1.04 mL||2.08 mL|
|50 mM||0.04 mL||0.21 mL||0.42 mL|
References are publications that support the biological activity of the product.
Skerratt et al (2016) The discovery of a potent, selective, and peripherally restricted pan-Trk inhibitor (PF-06273340) for the treatment of pain. J.Med.Chem. 59 10084 PMID: 27766865
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Keywords: PF 06273340, PF 06273340 supplier, PF06273340, Trk, A, B, C, tropomyosin-related, kinase, receptors, neurotrophins, inhibitors, inhibits, peripherally, restricted, potent, selective, Receptors, 6115, Tocris Bioscience
Citations for PF 06273340
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Reviews for PF 06273340
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Measured cancer cell viability upon treatment with this drug at various concentrations including 5 and 10 uM. In addition, compared it to a specific siRNA.
Literature in this Area
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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.
Huntington's Disease Poster
Huntington's disease (HD) is a monogenic neurodegenerative disorder, which is characterized by the prevalent loss of GABAergic medium spiny neurons (MSN) in the striatum. This poster summarizes the MSN intracellular signaling pathways implicated in the pathology of HD, as well as highlighting the use of iPSCs for HD modeling.
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.
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.