PF 06273340

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Description: Potent and selective pan-Trk inhibitor; peripherally restricted
Chemical Name: N-[5-[[2-Amino-7-(2-hydroxy-1,1-dimethylethyl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]carbonyl]-3-pyridinyl]-5-chloro-2-pyridineacetamide
Purity: ≥98% (HPLC)
Datasheet
Citations (1)
Reviews
Literature (3)

Biological Activity for PF 06273340

PF 06273340 is a 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.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Compound Libraries for PF 06273340

PF 06273340 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for PF 06273340

M. Wt 479.93
Formula C23H22ClN7O3
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 1402438-74-7
PubChem ID 66571548
InChI Key BPIWZDNVMQQBQX-UHFFFAOYSA-N
Smiles NC1=NC=C2C(N(C(C)(C)CO)C=C2C(C3=CN=CC(NC(CC4=CC=C(Cl)C=N4)=O)=C3)=O)=N1

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 PF 06273340

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 47.99 100

Preparing Stock Solutions for PF 06273340

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.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets for PF 06273340

Certificate of Analysis / Product Datasheet
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References for PF 06273340

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


If you know of a relevant reference for PF 06273340, please let us know.

View Related Products by Product Action

View all Trk Receptor Inhibitors

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

1 Citation for PF 06273340

Citations are publications that use Tocris products. Selected citations for PF 06273340 include:

Jeongwu et al (2018) Combined c-Met/Trk Inhibition Overcomes Resistance to CDK4/6 Inhibitors in Glioblastoma. Cancer Res 78 4360-4369 PMID: 29844123


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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!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Depression Poster

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 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 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.