2. MAPK/ERK Pathway Autophagy
  3. Ribosomal S6 Kinase (RSK) Autophagy
  4. PF-4708671

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.

PF-4708671 Chemical Structure

PF-4708671 Chemical Structure

CAS No. : 1255517-76-0

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Customer Review

Based on 21 publication(s) in Google Scholar

PF-4708671 Related Antibodies

Top Publications Citing Use of Products

    PF-4708671 purchased from MedChemExpress. Usage Cited in: J Proteomics. 2016 Feb 2;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.

    View All Ribosomal S6 Kinase (RSK) Isoform Specific Products:

    View All Isoforms
    p70S6K RSK1 RSK2 RSK3 RSK4

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    PF-4708671 is a potent cell-permeable S6K1 inhibitor with a Ki of 20 nM and IC50 of 160 nM.

    IC50 & Target[1]

    S6K1

    160 nM (IC50)

    S6K1

    20 nM (Ki)

    S6K2

    65 μM (IC50)

    In Vitro

    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.

    PF-4708671 Related Antibodies
    In Vivo

    The tumor growth rate in mice treated with the combination of OSI-906+PF-4708671 is significantly slower than that of OSI-906 alone (P=0.0189) or PF4708671 alone (P=0.0165) treated mice. The average tumor volume in the OSI-906+PF-4708671-treated mice is approximately 50% of that in mice treated with OSI-906 (P=0.0056) or PF-4708671 alone (P<0.001) at the end of a 15-day treatment[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Molecular Weight

    390.41

    Formula

    C19H21F3N6
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    FC(C1=CC=C2N=C(CN3CCN(C4=NC=NC=C4CC)CC3)NC2=C1)(F)F
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5614 mL 12.8070 mL 25.6141 mL
    5 mM 0.5123 mL 2.5614 mL 5.1228 mL
    View the 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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

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    In Vivo:

    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.

    • Protocol 1

      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.
    • Protocol 2

      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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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.
    Purity & Documentation
    References
    Cell Assay
    [2]

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References

    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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    PF-4708671 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    PF-47086711255517-76-0PF4708671PF 4708671Ribosomal S6 Kinase (RSK)AutophagyS6KInhibitorinhibitorinhibit

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