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PF-4708671 is a cell-permeable inhibitor of p70 ribosomal S6 kinase (S6K1 isoform) .In cell-free assays, PF-4708671(PF4708671) is potent for S6K1(Ki50=20 nM, IC50=160 nM).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $47 | In Stock | |
10 mg | $70 | In Stock | |
25 mg | $113 | In Stock | |
50 mg | $153 | In Stock | |
100 mg | $279 | In Stock | |
1 mL x 10 mM (in DMSO) | $77 | In Stock |
Description | PF-4708671 is a cell-permeable inhibitor of p70 ribosomal S6 kinase (S6K1 isoform) .In cell-free assays, PF-4708671(PF4708671) is potent for S6K1(Ki50=20 nM, IC50=160 nM). |
Targets&IC50 | p70 S6K1:160 nM |
In vivo | PF-4708671 inhibits the phosphorylation of S6 protein mediated by S6K1 in response to IGF-1 (Insulin-like Growth Factor 1) and can also induce the phosphorylation of the T-loop and hydrophobic motif of S6K1 through mTORC1 (mTOR complex 1). |
Kinase Assay | Affinity determination: Purified activated FAK kinase domain (amino acids 410–689) is reacted with 50 μM ATP, and 10 μg/well of a random peptide polymer of Glu and Tyr (molar ratio of 4:1), poly(Glu/Tyr) in kinase buffer (50 mM HEPES, pH 7.5, 125 mM NaCl, 48 mM MgCl2) for 15 min. Phosphorylation of poly(Glu/Tyr) is challenged with serially diluted compounds at 1/2-Log concentrations starting at a top concentration of 1 μM. Each concentration is run in triplicate. Phosphorylation of poly(Glu/Tyr) is detected with a general anti-phospho-tyrosine (PY20) antibody, followed by horseradish peroxidase-conjugated goat anti-mouse IgG antibody. The standard horseradish peroxidase substrate 3, 3', 5, 5'-tetramethylbenzidine is added, and Optical Density readings at 450 nm are obtained following the addition of stop solution (2 M H2SO4). The IC50 values are determined using the Hill slope model. |
Alias | PF4708671 |
Molecular Weight | 390.41 |
Formula | C19H21F3N6 |
Cas No. | 1255517-76-0 |
Smiles | CCc1cncnc1N1CCN(Cc2nc3cc(ccc3[nH]2)C(F)(F)F)CC1 |
Relative Density. | 1.348 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 19.5 mg/mL (50 mM) Ethanol: 19.5 mg/mL (50 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO/Ethanol
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