PF 4708671
Biological Activity
Cell-permeable inhibitor of p70 ribosomal S6 kinase (S6K1 isoform) (Ki = 20 nM; IC50 = 160 nM). Suppresses the S6K1-mediated phosphorylation of S6, Rictor and mTOR in response to IGF1; displays no effect on the activity of RSK and MSK in vivo. Exhibits no significant inhibition of S6K2 or other AGC kinases (e.g. Akt, PKA and ROCK) in vitro.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
Compound Libraries
PF 4708671 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 390.41 |
| Formula | C19H21F3N6 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1255517-76-0 |
| PubChem ID | 51371303 |
| InChI Key | FBLPQCAQRNSVHB-UHFFFAOYSA-N |
| Smiles | CCC(C=NC=N2)=C2N1CCN(CC4=NC3=CC(C(F)(F)F)=CC=C3N4)CC1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 19.52 | 50 | |
| ethanol | 19.52 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 390.41. Batch specific molecular weights may vary from batch to batch due to solvent 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 | 2.56 mL | 12.81 mL | 25.61 mL |
| 5 mM | 0.51 mL | 2.56 mL | 5.12 mL |
| 10 mM | 0.26 mL | 1.28 mL | 2.56 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.51 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Pearce et al (2010) Characterisation of PF-4708671 a novel and highly specific inhibitor of p70 ribosomal S6 kinase (S6K1). Biochem.J. 431 245 PMID: 20704563
If you know of a relevant reference for PF 4708671, please let us know.
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Keywords: PF4708671 selective inhibitor inhibitors p70 ribosomal S6 kinase S6K1 inhibits cancer Pfizer RSK
5 Citations for PF 4708671
Citations are publications that use Tocris products. Selected citations for PF 4708671 include:
Salmond et al (2015) Mechanistic Target of Rapamycin Complex 1/S6 Kinase 1 Signals Influence T Cell Activation Independently of Ribosomal Protein S6 Phosphorylation. J Immunol 195 4615 PMID: 26453749
Arnold et al (2014) Regulation of cardiac expression of the diabetic marker microRNA miR-29. PLoS One 9 e103284 PMID: 25062042
Al-Ejeh et al (2014) Kinome profiling reveals breast cancer heterogeneity and identifies targeted therapeutic opportunities for triple negative breast cancer. Tuberc Respir Dis (Seoul) 5 3145 PMID: 24762669
Melemedjian et al (2013) mTORC1 inhibition induces pain via IRS-1-dependent feedback activation of ERK. Pain 154 1080 PMID: 23607966
Wang et al (2011) Convergence of the mammalian target of rapamycin complex 1- and glycogen synthase kinase 3-β-signaling pathways regulates the innate inflammatory response. J Immunol 186 5217 PMID: 21422248
Do you know of a great paper that uses PF 4708671 from Tocris? If so please let us know.
