PF-4708671
Based on 29 publication(s) in Google Scholar
PF-4708671 is a potent cell-permeable S6K1 inhibitor with a Ki of 20 nM and IC50 of 160 nM.
For research use only. We do not sell to patients.
- Purity: 99.87%
- CAS No.: 1255517-76-0
- Formula: C19H21F3N6
- Molecular Weight:390.41
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) PF-4708671
More- Cancer Discov. 2022 Aug 5;12(8):1984-2005. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- J Infection. 2019 Sep;79(3):262-276. [Abstract]
- Cell Rep Med. 2025 May 29:102163. [Abstract]
- Genes Dis. 2025 Oct 3.
- Int J Biol Macromol. 2025 Sep 25;330(Pt 1):147928. [Abstract]
- Free Radic Biol Med. 2022 Dec 7;194:184-198. [Abstract]
- Diabetes. 2024 Aug 13:db240240. [Abstract]
- Cell Rep. 2021 Jun 22;35(12):109277. [Abstract]
- Antioxidants (Basel). 2026 Mar 25;15(4):413. [Abstract]
- Cancer Cell Int. 2024 Dec 19;24(1):409. [Abstract]
- Food Biosci. April 2022, 101571.
- Acta Neuropathol Commun. 2025 Sep 24;13(1):198. [Abstract]
- Int J Mol Sci. 2026 Feb 17;27(4):1915. [Abstract]
- Int J Mol Sci. 2024 Sep 28;25(19):10461. [Abstract]
- Matrix Biol. 2025 Oct 17:S0945-053X(25)00104-0. [Abstract]
- iScience. 2025 Sep 12;28(10):113552. [Abstract]
- Pestic Biochem Physiol. 2023 Apr:191:105362. [Abstract]
- Mol Pain. 2025 Jan-Dec:21:17448069251376198. [Abstract]
- Front Neurol. 2018 Apr 9:9:208. [Abstract]
- J Proteomics. 2016 Mar 16:136:13-24. [Abstract]
- bioRxiv. 2025 Aug 21.
- Research Square Preprint. 2024 Jan 31.
- bioRxiv. 2023 Feb 15.
- Oxid Med Cell Longev. 2022 Aug 25:2022:9148257. [Abstract]
- Research Square Preprint. 2021 Sep.
- Patent. US20200376102A1.
- Patent. US20200376146A1.
- bioRxiv. 2020 Apr.
Customer Validation & Images
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IF
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IF
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IF
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In Vivo Efficacy Study
Biological Activity
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S6K1 160 nM (IC50) |
S6K1 20 nM (Ki) |
S6K2 65 μM (IC50) |
PF-4708671 inhibits the activity of full-length S6K1 in vitro with a Ki of 20 nM, and S6K1 isolated from IGF1-stimulated HEK293 cells with an IC50 of 0.16 μM, and only inhibits very weakly the closely related S6K2 isoform (IC50 of 65 μM). PF-4708671 inhibits RSK1 (IC50 of 4.7 μM) and RSK2 (IC50 of 9.2 μM) over 20-fold less potently than S6K1. PF4708671 inhibits MSK1 (IC50 of 0.95 μM) 4-fold more weakly than S6K1[1]. HCT116 cells are treated with (i) vehicle (DMSO), (ii) OSI-906 (5 μM), (iii) PF-4708671 (10 μM), and (iv) OSI-906 (5 μM)+PF-4708671 (10 μM) for various amounts of time. HCT116 cells treated with OSI-906 alone (closed square) or PF4708671 alone (open circle) slightly inhibit cell growth. In contrast, proliferation in HCT116 cells is significantly inhibited after a 2-day treatment with the combination of OSI-906 and PF-4708671 (closed circle). A similar result is also observed when SW480 cells are treated with the combination of OSI-906 and PF-4708671. Colony formation also significantly reduces in OSI-906+PF-4708671-treated cells comparing with vehicle, OSI-906 alone, or PF-4708671 alone treated HCT116 or SW480 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1255517-76-0
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Appearance Solid
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Molecular Weight 390.41
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Formula C19H21F3N6
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Color White to off-white
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SMILES
FC(C1=CC=C2N=C(CN3CCN(C4=NC=NC=C4CC)CC3)NC2=C1)(F)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (29)
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Journal Impact Factor
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Most Recent
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Cancer Discov
2022 Aug 5;12(8):1984-2005. PMID: 35674408
PF-4708671 purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2022 Aug 5;12(8):1984-2005. [Abstract]
PF4708671 (20 nM, 1 h+ 1h) blocked IGF1-mediated SG formation in hPDAC cells but had no impact on SG formation in the absence of IGF1.
PF-4708671 purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2022 Aug 5;12(8):1984-2005. [Abstract]
PF4708671 (20 nM, 1 h + 1 h) impaired SRPK2 phosphorylation and attenuated the partitioning of SRPK2 into SGs in IGF1-treated cells to levels comparable to those in the absence of IGF1.
PF-4708671 purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2022 Aug 5;12(8):1984-2005. [Abstract]
Treatment of DIO mice with PF4708671 (I.P., 50 mg/kg, once per day for 39 days) led to diminished phosphorylation of the S6 protein in orthotopic tumors.
PF-4708671 purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2022 Aug 5;12(8):1984-2005. [Abstract]
PF4708671 (I.P., 50 mg/kg, once per day for 39 days) attenuated SG levels in DIO tumors by ~80% but had no effect on SG levels in tumors in ST mice.
PF-4708671 purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2022 Aug 5;12(8):1984-2005. [Abstract]
PF4708671 (I.P., 50 mg/kg, once per day for 39 days) impaired mPDAC growth in DIO mice but had no effect on mPDAC growth in ST mice.
PF-4708671 purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2022 Aug 5;12(8):1984-2005. [Abstract]
PF4708671 (I.P., 50 mg/kg, once per day for 39 days) enhanced cell death specifically in DIO tumors but had no impact on proliferation in DIO or ST tumors.
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Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
J Infection
Interferon regulatory factor 1 eliminates mycobacteria by suppressing p70 S6 kinase via mechanistic target of rapamycin signaling. [Abstract]2019 Sep;79(3):262-276. PMID: 31226272 -
Cell Rep Med
Insulin- and exercise-induced phosphoproteomics of human skeletal muscle identify REPS1 as a regulator of muscle glucose uptake. [Abstract]2025 May 29:102163. PMID: 40482643 -
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Int J Biol Macromol
Autophagic damage in senescent bone marrow mesenchymal stromal cells: Impact on Piezo1 expression during osteoporosis progression. [Abstract]2025 Sep 25;330(Pt 1):147928. PMID: 41015372 -
Free Radic Biol Med
TrkB agonist N-acetyl serotonin promotes functional recovery after traumatic brain injury by suppressing ferroptosis via the PI3K/Akt/Nrf2/Ferritin H pathway. [Abstract]2022 Dec 7;194:184-198. PMID: 36493983 -
Diabetes
2024 Aug 13:db240240. PMID: 39137120 -
Cell Rep
TOR signaling regulates liquid phase separation of the SMN complex governing snRNP biogenesis. [Abstract]2021 Jun 22;35(12):109277. PMID: 34161763 -
Antioxidants (Basel)
Alpha-Lipoic Acid Inhibits IFN-γ-Induced PD-L1 Expression in Prostate Cancer Cells and Enhances T-Cell-Mediated Anti-Tumor Cytotoxicity. [Abstract]2026 Mar 25;15(4):413. PMID: 42072056 -
Cancer Cell Int
Proapoptotic role of CDK1 in overcoming paclitaxel resistance in ovarian cancer cells in response to combined treatment with paclitaxel and duloxetine. [Abstract]2024 Dec 19;24(1):409. PMID: 39702300 -
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Acta Neuropathol Commun
RNF168 dephosphorylation ameliorates cognitive decline in Aβ-based mouse models of Alzheimer's disease. [Abstract]2025 Sep 24;13(1):198. PMID: 40993809 -
Int J Mol Sci
2026 Feb 17;27(4):1915. PMID: 41752050 -
Int J Mol Sci
S6K1 Controls DNA Damage Signaling Modulated by the MRN Complex to Induce Radioresistance in Lung Cancer. [Abstract]2024 Sep 28;25(19):10461. PMID: 39408794 -
Matrix Biol
Phosphorylation of UDP-glucose dehydrogenase increases glycosaminoglycan biosynthesis and promotes tumor cell motility, spheroid growth, and therapeutic resistance. [Abstract]2025 Oct 17:S0945-053X(25)00104-0. PMID: 41110727 -
iScience
Phosphorylation of plectin by Akt3 promotes triple-negative breast cancer cell invasive migration. [Abstract]2025 Sep 12;28(10):113552. PMID: 41079612 -
Pestic Biochem Physiol
Mechanisms underlying the effects of low concentrations of chlorantraniliprole on development and reproduction of the fall armyworm, Spodoptera frugiperda. [Abstract]2023 Apr:191:105362. PMID: 36963952 -
Mol Pain
Inhibition of mTOR/S6K1/Gli1 signaling alleviates morphine-induced thermal hyperalgesia and tolerance. [Abstract]2025 Jan-Dec:21:17448069251376198. PMID: 40968661 -
Front Neurol
Inhibition of mTORC1 Signaling Reverts Cognitive and Affective Deficits in a Mouse Model of Parkinson's Disease. [Abstract]2018 Apr 9:9:208. PMID: 29686643 -
J Proteomics
2016 Mar 16:136:13-24. PMID: 26844761
PF-4708671 purchased from MedChemExpress. Usage Cited in: J Proteomics. 2016 Mar 16:136:13-24. [Abstract]
mTORC1 regulates KPNA2 transcription but not S6K1- and 4E-BP1-dependent translation. KPNA2 abundances in response to S6K1 inhibition are detected by Western blot analysis in WT and TSC2−/− MEFs.
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Oxid Med Cell Longev
Alpha-Ketoglutarate Alleviates Neuronal Apoptosis Induced by Central Insulin Resistance through Inhibiting S6K1 Phosphorylation after Subarachnoid Hemorrhage. [Abstract]2022 Aug 25:2022:9148257. PMID: 36062190 -
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Solvent & Solubility
DMSO : 33.33 mg/mL (85.37 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.40 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.40 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
GEO, HT29, SW480, and HCT116 cells are used. The effects of OSI-906 or the combination of OSI-906 and PF-4708671 on cell proliferation is determined with XTT and clonogenic assays. XTT assays are performed using the Cell Proliferation Kit II (XTT). For clonogenic assays, cells (1×103 cells/well) are seeded on a 6-well plate and subsequently treated with drugs (OSI-906 5 μM, PF-4708671 10 μM). After 1 week of incubation, cells are stained with 1% crystal violet, and the number of colonies is counted and recorded[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
Five- to 6-week-old female athymic nude mice (Hsd:Athymic Nude-Foxn1nu) are randomly assigned to the following groups (5 mice/group). For injection of HT29-L and HT29-P cells, mice are treated with vehicle (25 mM tartaric acid) or OSI-906 (30 mg/kg) for 12 days. For injection of HCT116 cells, mice are treated with (i) vehicle (25 mM tartaric acid); (ii) OSI-906 alone (30 mg/kg); (iii) PF-4708671 alone (60 mg/kg); and (iv) OSI-906 (30 mg/kg)+PF-4708671 (60 mg/kg) and treated with drugs orally for 14 days. Vehicle and OSI-906 are given once per day and PF-4708671 is given once every other day. Twenty-four hours after the last treatment, the mice are sacrificed and the tumor weights were measured[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (282 KB)
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SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Portuguese - PT (479 KB)
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Handling Instructions (2659 KB)
References
[1]. Pearce LR, et al. Characterization of PF-4708671, a novel and highly specific inhibitor of p70 ribosomal S6 kinase (S6K1). Biochem J. 2010 Oct 15;431(2):245-55. [Content Brief]
[2]. Zhang Y, et al. Inhibition of p70S6K1 Activation by Pdcd4 Overcomes the Resistance to an IGF-1R/IR Inhibitor in Colon Carcinoma Cells. Mol Cancer Ther. 2015 Mar;14(3):799-809. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5614 mL | 12.8070 mL | 25.6141 mL | 64.0352 mL |
| 5 mM | 0.5123 mL | 2.5614 mL | 5.1228 mL | 12.8070 mL | |
| 10 mM | 0.2561 mL | 1.2807 mL | 2.5614 mL | 6.4035 mL | |
| 15 mM | 0.1708 mL | 0.8538 mL | 1.7076 mL | 4.2690 mL | |
| 20 mM | 0.1281 mL | 0.6404 mL | 1.2807 mL | 3.2018 mL | |
| 25 mM | 0.1025 mL | 0.5123 mL | 1.0246 mL | 2.5614 mL | |
| 30 mM | 0.0854 mL | 0.4269 mL | 0.8538 mL | 2.1345 mL | |
| 40 mM | 0.0640 mL | 0.3202 mL | 0.6404 mL | 1.6009 mL | |
| 50 mM | 0.0512 mL | 0.2561 mL | 0.5123 mL | 1.2807 mL | |
| 60 mM | 0.0427 mL | 0.2135 mL | 0.4269 mL | 1.0673 mL | |
| 80 mM | 0.0320 mL | 0.1601 mL | 0.3202 mL | 0.8004 mL |
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