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

YHO-13177, a acrylonitrile derivative, is an orally active, potent and specific inhibitor of breast cancer resistance protein (BCRP) and ABCG2 with an IC50 value of 10 nM. YHO-13177 potentiates the cytotoxicity of SN-38 in HCT116 and A549 cells that express BCRP. YHO-13177 combined with Irinotecan (HY-16562) significantly suppresses the tumor growth in an HCT116/BCRP xenograft model.

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CAS 番号 : 912287-56-0

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10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 104 在庫あり
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10 mg $140 在庫あり
25 mg $280 在庫あり
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Based on 2 publication(s) in Google Scholar

YHO-13177 関連抗体

Top Publications Citing Use of Products

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

    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.

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    製品説明

    YHO-13177, a acrylonitrile derivative, is an orally active, potent and specific inhibitor of breast cancer resistance protein (BCRP) and ABCG2 with an IC50 value of 10 nM. YHO-13177 potentiates the cytotoxicity of SN-38 in HCT116 and A549 cells that express BCRP. YHO-13177 combined with Irinotecan (HY-16562) significantly suppresses the tumor growth in an HCT116/BCRP xenograft model[1][2][3].

    Cellular Effect
    Cell Line Type Value Description References
    HCT-116 IC50
    10 nM
    Compound: 14; YHO-13177
    Cytotoxicity against human HCT-116 cells assessed as cell viability measured as mitochondrial NADH-dependent dehydrogenase activity incubated for 72 to 120 hrs
    Cytotoxicity against human HCT-116 cells assessed as cell viability measured as mitochondrial NADH-dependent dehydrogenase activity incubated for 72 to 120 hrs
    		[PMID: 37847948]
    体外実験

    YHO-13177 (0.01 to 1 μM, 96 h) reverses BCRP-mediated drug resistance and sensitivity in a concentration-dependent manner in various BCRP-transduced cancer cells[1].
    YHO-13177 (0.01 to 1 μM, 96 h) decreases the expression of BCRP protein in HCT116 and HCT116/BCRP cells, or A549 and A549/SN4 cells[1].
    YHO-13177 (0-0.1 μM, 96 h) reduces the side population cell ratio in HeLa cells in a concentration-dependent manner[2].

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

    YHO-13177 関連抗体

    Western Blot Analysis[1]

    Cell Line: HCT116 and A549 cells
    Concentration: 0.01 to 1 μM
    Incubation Time: 96 h
    Result: Apparently decreased the level of BCRP protein at more than 24 hours.
    体内実験

    YHO-13177 (19.7μM, i.v., or 27.3μM, p.o., a single dose for 25 days) is converted by YHO-13351, increases the survival time of mice inoculated with BCRP-transduced murine leukemia P388 cells and suppresses the tumor growth in an HCT116/BCRP xenograft mouse model[1].

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

    Animal Model: HCT116/BCRP xenograft mouse model[1]
    Dosage: 19.7 μM or 27.3 μM
    Administration: 19.7 μM, i.v., or 27.3 μM, p.o., a single dose for 25 days
    Result: Was maintained for at least 8 hours in plasma.
    分子量

    370.47

    分子式

    C20H22N2O3S
    CAS 番号
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 33.33 mg/mL (89.97 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 2.6993 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
    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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    一般には略語で表示されます：C1V1 = C2V2

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    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 (6.75 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.
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    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.
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    参考文献

    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.6993 mL 13.4964 mL 26.9927 mL 67.4818 mL
    5 mM 0.5399 mL 2.6993 mL 5.3985 mL 13.4964 mL
    10 mM 0.2699 mL 1.3496 mL 2.6993 mL 6.7482 mL
    15 mM 0.1800 mL 0.8998 mL 1.7995 mL 4.4988 mL
    20 mM 0.1350 mL 0.6748 mL 1.3496 mL 3.3741 mL
    25 mM 0.1080 mL 0.5399 mL 1.0797 mL 2.6993 mL
    30 mM 0.0900 mL 0.4499 mL 0.8998 mL 2.2494 mL
    40 mM 0.0675 mL 0.3374 mL 0.6748 mL 1.6870 mL
    50 mM 0.0540 mL 0.2699 mL 0.5399 mL 1.3496 mL
    60 mM 0.0450 mL 0.2249 mL 0.4499 mL 1.1247 mL
    80 mM 0.0337 mL 0.1687 mL 0.3374 mL 0.8435 mL
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    YHO-13177 Related Classifications

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    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
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    • 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:

    YHO-13177912287-56-0YHO13177YHO 13177BCRPBreast cancer resistance proteinABCG2acrylonitrile derivativeHCT116 and A549 cells tumorInhibitorinhibitorinhibit

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