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Technical Data
| Formula | C19H21F3N6 |
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| Molecular Weight | 390.41 | CAS No. | 1255517-76-0 | |
| Solubility (25°C)* | In vitro | Ethanol | 40 mg/mL (102.45 mM) | |
| DMSO | 30 mg/mL (76.84 mM) | |||
| Water | Insoluble | |||
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* <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.) |
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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. | ||
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| Targets |
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| 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
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Data from [Data independently produced by PLoS One, 2014, 9(2), e90388]
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Data from [Data independently produced by , , Front Immunol, 2017, 7:685]
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Data from [Data independently produced by , , Mol Cancer Ther, 2015, 14(3): 799-809]
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Data from [Data independently produced by , , Oncotarget, 2016, 7(8):9163-74]
Selleck's PF-4708671 has been cited by 58 publications
| 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 |
| 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 |
| Sustained oncogenic signaling in the cytostatic state enables targeting of non-proliferating persistent cancer cells [ Cancer Res, 2022, can.21.2908] | PubMed: 35792658 |
| Acetyltanshinone IIA reduces the synthesis of cell cycle-related proteins by degrading p70S6K and subsequently inhibits drug-resistant lung cancer cell growth [ Pharmacol Res, 2022, 179:106209] | PubMed: 35398238 |
RETURN POLICY
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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.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.