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PTC-209 

Cat. No.: HY-15888 Purity: 99.85%
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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.

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

PTC-209 Chemical Structure

PTC-209 Chemical Structure

CAS No. : 315704-66-6

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Solid + Solvent
10 mM * 1 mL in DMSO
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Solid
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10 mg USD 154 In-stock
50 mg USD 594 In-stock
100 mg USD 979 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

    Appearance

    Solid

    Formula

    C17H13Br2N5OS

    CAS No.
    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)

    *"≥" 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
    10 mM 0.2019 mL 1.0097 mL 2.0194 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    *All of the co-solvents are available by MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.85%

    References
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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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