1. NT157

NT157  (Synonyms: Tyrphostin NT157)

Cat. No.: HY-100037 Purity: 99.19%
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NT157 (Tyrphostin NT157) is a selective IRS-1/2 inhibitor that induces Ser-phosphorylation and consequently the degradation of IRS-1/2. NT157 (Tyrphostin NT157) is a first-in-class anti-cancer agent that also targets Stat3 signaling pathway.

For research use only. We do not sell to patients.

NT157 Chemical Structure

NT157 Chemical Structure

CAS No. : 1384426-12-3

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 176 In-stock
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2 mg USD 90 In-stock
5 mg USD 160 In-stock
10 mg USD 250 In-stock
25 mg USD 470 In-stock
50 mg USD 740 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE NT157

WB

    NT157 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2018 Jul 4;9(1):2611.  [Abstract]

    Western blot of Gr-1+CD11b+myeloid cells collected from spleen of 4T1 tumor-bearing mice treated with NT157 (n=5).
    • Biological Activity

    • Purity & Documentation

    • Customer Review

    Description

    NT157 (Tyrphostin NT157) is a selective IRS-1/2 inhibitor that induces Ser-phosphorylation and consequently the degradation of IRS-1/2. NT157 (Tyrphostin NT157) is a first-in-class anti-cancer agent that also targets Stat3 signaling pathway[1][2].

    IC50 & Target

    IRS-1/2[1]; Stat3[2]

    In Vitro

    NT157 (0.3-3 μM; 72 hours) shows a strong dose-dependent inhibition of growth in all cell lines tested, and the IC50 s ranges from 0.3 to 0.8 μM[1].
    NT157 (1-3 μM; 24 hours) induces cell cycle arrest in MG-63 and U-2OS OS cells[1].
    NT157 (1-3 μM; 48 hours) downregulates the Tyr-phosphorylation of IRS-1 in the MG-63 and U-2OS cells[1].

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

    Cell Proliferation Assay[1]

    Cell Line: MG-63, OS-19, and U-2OS cells
    Concentration: 0.3, 1, 3 μM
    Incubation Time: 72 hours
    Result: Showed a strong dose-dependent inhibition of growth, and the IC50s ranges from 0.3 to 0.8 μM.

    Cell Cycle Analysis[1]

    Cell Line: MG-63, U-2OS OS cells
    Concentration: 1, 3 μM
    Incubation Time: 24 hours
    Result: Induced cell cycle arrest in the G2/M phase.

    Western Blot Analysis[1]

    Cell Line: MG-63, U-2OS OS cells
    Concentration: 1, 3 μM
    Incubation Time: 48 hours
    Result: Downregulated the Tyr-phosphorylation of IRS-1 in the MG-63 and U-2OS cells.
    In Vivo

    NT157 (50 mg/kg; i.p.; three times per week for 6 weeks) significantly delayed tumor growth in castrated mice bearing LNCaP xenografts [3].

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

    Animal Model: 6- to 8- week-old male athymic nude mice (LNCaP xenografts)[3]
    Dosage: 50 mg/kg
    Administration: i.p.; three times per week for 6 weeks
    Result: Significantly delayed tumor growth.
    Molecular Weight

    412.26

    Formula

    C16H14BrNO5S

    CAS No.
    Appearance

    Solid

    SMILES

    S=C(NCC1=CC(O)=C(O)C(O)=C1)/C=C/C2=CC(O)=C(O)C(Br)=C2

    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 : ≥ 30 mg/mL (72.77 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.4257 mL 12.1283 mL 24.2565 mL
    5 mM 0.4851 mL 2.4257 mL 4.8513 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)

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (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 (6.06 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 (6.06 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:

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    Dosing volume
    (per animal)

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    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

    Purity: 99.19%

    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 2.4257 mL 12.1283 mL 24.2565 mL 60.6413 mL
    5 mM 0.4851 mL 2.4257 mL 4.8513 mL 12.1283 mL
    10 mM 0.2426 mL 1.2128 mL 2.4257 mL 6.0641 mL
    15 mM 0.1617 mL 0.8086 mL 1.6171 mL 4.0428 mL
    20 mM 0.1213 mL 0.6064 mL 1.2128 mL 3.0321 mL
    25 mM 0.0970 mL 0.4851 mL 0.9703 mL 2.4257 mL
    30 mM 0.0809 mL 0.4043 mL 0.8086 mL 2.0214 mL
    40 mM 0.0606 mL 0.3032 mL 0.6064 mL 1.5160 mL
    50 mM 0.0485 mL 0.2426 mL 0.4851 mL 1.2128 mL
    60 mM 0.0404 mL 0.2021 mL 0.4043 mL 1.0107 mL
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    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.

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    Product Name:
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