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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)
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.
| 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
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.
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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
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
Do you know of a great paper that uses PF 06273340 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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