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  3. PTC-209

PTC-209 is a specific BMI-1 inhibitor with an IC50 of 0.5 μM in HEK293T cell line. PTC-209 irreversibly impairs colorectal cancer-initiating cells (CICs). PTC-209 shows potent anti-myeloma activity and impairs the tumor microenvironment.

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PTC-209 Chemical Structure

PTC-209 Chemical Structure

CAS No. : 315704-66-6

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10 mM * 1 mL in DMSO
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10 mg USD 154 In-stock
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Customer Review

Based on 13 publication(s) in Google Scholar

Other Forms of PTC-209:

Top Publications Citing Use of Products

    PTC-209 purchased from MedChemExpress. Usage Cited in: Oncogene. 2020 Jan;39(1):17-29.  [Abstract]

    BMI1 inhibitor delays CRPC progression in vivo. C4-2 cells are treated with PTC209.

    PTC-209 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2018 Feb 5;9(1):500.  [Abstract]

    BMI1-specific antagonist inhibits androgen receptor (AR)-signaling pathway. C4-2 (a) or 22Rv1 (b) is treated with PTC209 in indicated concentration for 48 h, BMI1 and AR are tested by western blot, and GAPDH served as loading control.

    PTC-209 purchased from MedChemExpress. Usage Cited in: Cell Stem Cell. 2017 May 4;20(5):621-634.e6.  [Abstract]

    The Combination Therapy of Cisplatin Plus PTC-209 Potently Eradicates Bmi1+ CSCs and Inhibits Tumor Progression by Lineage Tracing. Western blots show that Bmi1 is reduced in tumors treated with PTC-209.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    PTC-209 is a specific BMI-1 inhibitor with an IC50 of 0.5 μM in HEK293T cell line. PTC-209 irreversibly impairs colorectal cancer-initiating cells (CICs). PTC-209 shows potent anti-myeloma activity and impairs the tumor microenvironment[1][2].

    IC50 & Target

    IC50: 0.5 μM (BMI-1, in HT1080 tumor cells)[1]

    In Vitro

    PTC-209 (0.01-10 μM; 24-72 hours) induces a concentration- and time-dependent decrease in the cellular viability of all cell lines tested[2].
    PTC-209 (1-2.5 μM) inhibits STAT3 phosphorylation in A549 lung cancer cells and MDA-MB-231 breast cancer cells[2].

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

    Cell Viability Assay[2]

    Cell Line: Lung (LNM35, A549 cells), breast (MDA-MB-231 and T47D cells), and colon (HT-29, HCT-116, and HCT8/S11 cells)
    Concentration: 0.01-10 µM
    Incubation Time: 24, 48, and 72 hour
    Result: Induced a concentration- and time-dependent decrease in the cellular viability of all cell lines tested.
    In Vivo

    PTC-209 (60 mg/kg body weight; subcutaneously; once a day for 11 days) significantly reduces tumor volume[1].

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

    Animal Model: Nude mice (male, aged 8-10 weeks, HCT1116 cell-derived tumor)[1]
    Dosage: 60 mg/kg body weight
    Administration: Subcutaneously; once a day for 11 days
    Result: Significantly reduced tumor volume
    Molecular Weight

    495.19

    Formula

    C17H13Br2N5OS

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to green yellow

    SMILES

    CC1=C(C2=CSC(NC3=C(Br)C=C(OC)C=C3Br)=N2)N4C=CC=NC4=N1

    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 : ≥ 32 mg/mL (64.62 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 2.0194 mL 10.0971 mL 20.1943 mL
    5 mM 0.4039 mL 2.0194 mL 4.0389 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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    Volume
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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

    ×
    Volume (start)

    V1

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    Concentration (final)

    C2

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    Volume (final)

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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 (5.05 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      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.
    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

    Purity: 99.85%

    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 2.0194 mL 10.0971 mL 20.1943 mL 50.4857 mL
    5 mM 0.4039 mL 2.0194 mL 4.0389 mL 10.0971 mL
    10 mM 0.2019 mL 1.0097 mL 2.0194 mL 5.0486 mL
    15 mM 0.1346 mL 0.6731 mL 1.3463 mL 3.3657 mL
    20 mM 0.1010 mL 0.5049 mL 1.0097 mL 2.5243 mL
    25 mM 0.0808 mL 0.4039 mL 0.8078 mL 2.0194 mL
    30 mM 0.0673 mL 0.3366 mL 0.6731 mL 1.6829 mL
    40 mM 0.0505 mL 0.2524 mL 0.5049 mL 1.2621 mL
    50 mM 0.0404 mL 0.2019 mL 0.4039 mL 1.0097 mL
    60 mM 0.0337 mL 0.1683 mL 0.3366 mL 0.8414 mL
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    PTC-209 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.

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    Product Name:
    PTC-209
    Cat. No.:
    HY-15888
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