PF-4708671

Catalog No.S2163 Batch:S216351

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Technical Data

Formula

C19H21F3N6
Molecular Weight 390.41 CAS No. 1255517-76-0
Solubility (25°C)* In vitro DMSO 30 mg/mL (76.84 mM)
Ethanol 8 mg/mL (20.49 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
30%PEG400 0.5%Tween80 5%propylene glycol
30.0mg/ml Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified PEG400 stock solution to 5 μL of Tween80, mix evenly to clarify it; add 50 μL Propylene glycol to the above system, mix evenly to clarify it; then continue to add 645 μL ddH2O to adjust the volume. to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description PF-4708671 is a cell-permeable inhibitor of p70 ribosomal S6 kinase (S6K1 isoform) with Ki/IC50 of 20 nM/160 nM in cell-free assays, 400-fold greater selectivity for S6K1 than S6K2, and 4- and >20-fold selectivity for S6K1 than MSK1 and RSK1/2, respectively. PF-4708671 induces autophagy. First S6K1-specific inhibitor to be reported.
Targets
p70 S6K1 [1]
(Cell-free assay)
160 nM
In vitro PF-4708671 is a piperazinyl-pyrimidine analogue and the first S6K1-specific inhibitor. PF-4708671 does not significantly inhibit the activity of the closely related S6K2 isoform or a number of other AGC kinases (Akt1, Akt2, PKA, PKCα, PKCϵ, PRK2, ROCK2, RSK1, RSK2 or SGK1) . PF-4708671 prevents the S6K1-mediated phosphorylation of S6 protein in response to IGF-1 (insulin-like growth factor 1), while having no effect upon the PMA-induced phosphorylation of substrates of the highly related RSK (p90 ribosomal S6 kinase) and MSK (mitogen- and stress-activated kinase) kinases. PF-4708671 is also found to induce phosphorylation of the T-loop and hydrophobic motif of S6K1, an effect that is dependent upon mTORC1 (mTOR complex 1). PF-4708671 does not affect activity of mTORC1. [1]

Protocol (from reference)

Customer Product Validation

Data from [Data independently produced by PLoS One, 2014, 9(2), e90388]

Data from [Data independently produced by , , Front Immunol, 2017, 7:685]

Data from [Data independently produced by , , Mol Cancer Ther, 2015, 14(3): 799-809]

Data from [Data independently produced by , , Oncotarget, 2016, 7(8):9163-74]

Selleck's PF-4708671 has been cited by 61 publications

mTORC2-driven chromatin cGAS mediates chemoresistance through epigenetic reprogramming in colorectal cancer [ Nat Cell Biol, 2024, 10.1038/s41556-024-01473-0] PubMed: 39080411
Epstein-Barr Virus Latent Membrane Protein 2A (LMP2A) Enhances ATP Production in B Cell Tumors through mTOR and HIF-1α [ Int J Mol Sci, 2024, 25(7)3944] PubMed: 38612754
Duloxetine enhances the sensitivity of non-small cell lung cancer cells to EGFR inhibitors by REDD1-induced mTORC1/S6K1 suppression [ Am J Cancer Res, 2024, 14(3):1087-1100] PubMed: 38590408
STING Suppresses Mitochondrial VDAC2 to Govern RCC Growth Independent of Innate Immunity [ Adv Sci (Weinh), 2023, 10(3):e2203718] PubMed: 36445063
The translational oscillation in oocyte and early embryo development [ Nucleic Acids Res, 2023, 51(22):12076-12091] PubMed: 37950888
Pharmacological inhibition of S6K1 rescues synaptic deficits and attenuates seizures and depression in chronic epileptic rats [ CNS Neurosci Ther, 2023, 10.1111/cns.14475] PubMed: 37736829
mTORC1/ERK1/2 Interplay Regulates Protein Synthesis and Survival in Acute Myeloid Leukemia Cell Lines [ Biology (Basel), 2023, 12(5)676] PubMed: 37237490
Stress Granules determine the Development of Obesity-associated Pancreatic Cancer [ Cancer Discov, 2022, candisc.1672.2021] PubMed: 35674408
S6K1-mediated phosphorylation of PDK1 impairs AKT kinase activity and oncogenic functions [ Nat Commun, 2022, 13(1):1548] PubMed: 35318320
secDrug: a pipeline to discover novel drug combinations to kill drug-resistant multiple myeloma cells using a greedy set cover algorithm and single-cell multi-omics [ Blood Cancer J, 2022, 12(3):39] PubMed: 35264575

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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