1. Membrane Transporter/Ion Channel
  2. BCRP
  3. YHO-13177

YHO-13177 

Cat. No.: HY-12757 Purity: 98.72%
Handling Instructions

YHO-13177 is a potent and specific inhibitor of BCRP; potentiated the cytotoxicity of SN-38 in cancer cells and no effect on P-glycoprotein–mediated paclitaxel resistance in MDR1-transduced human leukemia K562 cells.

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

YHO-13177 Chemical Structure

YHO-13177 Chemical Structure

CAS No. : 912287-56-0

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 110 In-stock
Estimated Time of Arrival: December 31
5 mg USD 100 In-stock
Estimated Time of Arrival: December 31
10 mg USD 150 In-stock
Estimated Time of Arrival: December 31
50 mg USD 450 In-stock
Estimated Time of Arrival: December 31
100 mg USD 750 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Top Publications Citing Use of Products

    YHO-13177 purchased from MCE. Usage Cited in: Drug Deliv. 2017 Nov;24(1):1453-1459.

    Fluorescent substrates accumulate in the organoids. The organoids are incubated in Hoechst 33342 with or without YHO-13177 or Ko143 for 20, 60 and 100 minutes, respectively. Ko143 and YHO-13177 notably decrease the fluorescence intensity of Hoechst 33342 in the organoids.
    • Biological Activity

    • Technical Information

    • Purity & Documentation

    • References

    Description

    YHO-13177 is a potent and specific inhibitor of BCRP; potentiated the cytotoxicity of SN-38 in cancer cells and no effect on P-glycoprotein–mediated paclitaxel resistance in MDR1-transduced human leukemia K562 cells. IC50 value: Target: BCRP inhibitor in vitro: YHO-13177 potentiated the cytotoxicity of SN-38, mitoxantrone, and topotecan in both BCRP-transduced human colon cancer HCT116 (HCT116/BCRP) cells and SN-38–resistant human lung cancer A549 (A549/SN4) cells that express BCRP, but had little effect in the parental cells. In addition, YHO-13177 potentiated the cytotoxicity of SN-38 in human lung cancer NCI-H460 and NCI-H23, myeloma RPMI-8226, and pancreatic cancer AsPC-1 cells that intrinsically expressed BCRP. In contrast, it had no effect on P-glycoprotein–mediated paclitaxel resistance in MDR1-transduced human leukemia K562 cells and multidrug resistance-related protein 1–mediated doxorubicin resistance in MRP1-transfected human epidermoid cancer KB-3-1 cells. YHO-13177 increased the intracellular accumulation of Hoechst 33342, a substrate of BCRP, at 30 minutes and partially suppressed the expression of BCRP protein at more than 24 hours after its treatment in both HCT116/BCRP and A549/SN4 cells [1]. in vivo: In mice, YHO-13351 was rapidly converted into YHO-13177 after its oral or intravenous administration. Coadministration of irinotecan with YHO-13351 significantly increased the survival time of mice inoculated with BCRP-transduced murine leukemia P388 cells and suppressed the tumor growth in an HCT116/BCRP xenograft model, whereas irinotecan alone had little effect in these tumor models [1].

    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 (89.97 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.6993 mL 13.4964 mL 26.9927 mL
    5 mM 0.5399 mL 2.6993 mL 5.3985 mL
    10 mM 0.2699 mL 1.3496 mL 2.6993 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 (6.75 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Molecular Weight

    370.47

    Formula

    C₂₀H₂₂N₂O₃S

    CAS No.

    912287-56-0

    SMILES

    N#C/C(C1=CC=C(OC)C(OC)=C1)=C\C2=CC=C(N3CCC(O)CC3)S2

    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 98.72%

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    Product Name:
    YHO-13177
    Cat. No.:
    HY-12757
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    YHO-13177

    Cat. No.: HY-12757