1. JAK/STAT Signaling Stem Cell/Wnt
  2. STAT
  3. BP-1-102

BP-1-102 is an orally available, small-molecule inhibitor of transcription factor Stat3, with an IC50 of 6.8 μM.

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No. CAS : 1334493-07-0

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Revisión del cliente

Based on 11 publication(s) in Google Scholar

Other Forms of BP-1-102:

Top Publications Citing Use of Products

    BP-1-102 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2020 Jul 8;18(1):104.  [Abstract]

    Immunoblotting analysis of pulmonary STAT3 and pY-STAT3 in mice 24 h after CLP with BP-1-102 (BP) administration. BP downregulates the elevated pY-STAT3 level in the mouse lung 24 h after CLP.

    Ver todos los productos específicos de isoformas STAT:

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    • Referencias

    • Revisión del cliente

    Descripciòn

    BP-1-102 is an orally available, small-molecule inhibitor of transcription factor Stat3, with an IC50 of 6.8 μM.

    IC50 & Target[1]

    STAT3

    6.8 μM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    143B IC50
    4.4 3
    Compound: 1d; BP-1-102
    Antiinvasive activity against human 143B cells assessed as reduction in cell invasion measured after 12 hrs by crystal violet staining based inverted microscopic analysis
    Antiinvasive activity against human 143B cells assessed as reduction in cell invasion measured after 12 hrs by crystal violet staining based inverted microscopic analysis
    [PMID: 35476936]
    143B IC50
    4.17 3
    Compound: 1d; BP-1-102
    Antimigratory activity against human 143B cells assessed as reduction in cell migration measured after 12 hrs by wound healing assay
    Antimigratory activity against human 143B cells assessed as reduction in cell migration measured after 12 hrs by wound healing assay
    [PMID: 35476936]
    143B IC50
    4.17 3
    Compound: 1d; BP-1-102
    Antimigratory activity against human 143B cells assessed as reduction in cell migration measured after 12 hrs by wound healing assay
    Antimigratory activity against human 143B cells assessed as reduction in cell migration measured after 12 hrs by wound healing assay
    [PMID: 35476936]
    143B IC50
    4.4 3
    Compound: 1d; BP-1-102
    Antiinvasive activity against human 143B cells assessed as reduction in cell invasion measured after 12 hrs by crystal violet staining based inverted microscopic analysis
    Antiinvasive activity against human 143B cells assessed as reduction in cell invasion measured after 12 hrs by crystal violet staining based inverted microscopic analysis
    [PMID: 35476936]
    143B IC50
    4.4 3
    Compound: 1d; BP-1-102
    Antiinvasive activity against human 143B cells assessed as reduction in cell invasion measured after 12 hrs by crystal violet staining based inverted microscopic analysis
    Antiinvasive activity against human 143B cells assessed as reduction in cell invasion measured after 12 hrs by crystal violet staining based inverted microscopic analysis
    [PMID: 35476936]
    143B IC50
    4.17 3
    Compound: 1d; BP-1-102
    Antimigratory activity against human 143B cells assessed as reduction in cell migration measured after 12 hrs by wound healing assay
    Antimigratory activity against human 143B cells assessed as reduction in cell migration measured after 12 hrs by wound healing assay
    [PMID: 35476936]
    143B IC50
    5.87 3
    Compound: 1d; BP-1-102
    Antiproliferative activity against human 143B cells assessed as inhibition of cell growth incubated for 48 hrs by cell titer based MTS assay
    Antiproliferative activity against human 143B cells assessed as inhibition of cell growth incubated for 48 hrs by cell titer based MTS assay
    [PMID: 35476936]
    143B IC50
    5.87 3
    Compound: 1d; BP-1-102
    Antiproliferative activity against human 143B cells assessed as inhibition of cell growth incubated for 48 hrs by cell titer based MTS assay
    Antiproliferative activity against human 143B cells assessed as inhibition of cell growth incubated for 48 hrs by cell titer based MTS assay
    [PMID: 35476936]
    143B IC50
    5.87 3
    Compound: 1d; BP-1-102
    Antiproliferative activity against human 143B cells assessed as inhibition of cell growth incubated for 48 hrs by cell titer based MTS assay
    Antiproliferative activity against human 143B cells assessed as inhibition of cell growth incubated for 48 hrs by cell titer based MTS assay
    [PMID: 35476936]
    A549 IC50
    5 3
    Compound: 3; SH4-54
    Antiproliferative activity against human A549 cells
    Antiproliferative activity against human A549 cells
    [PMID: 34000483]
    A549 IC50
    5 3
    Compound: 3; SH4-54
    Antiproliferative activity against human A549 cells
    Antiproliferative activity against human A549 cells
    [PMID: 34000483]
    DU-145 EC50
    22.7 3
    Compound: 17o
    Cytotoxicity against human DU145 cells after 72 hrs by MTS assay
    Cytotoxicity against human DU145 cells after 72 hrs by MTS assay
    [PMID: 21788134]
    DU-145 EC50
    22.7 3
    Compound: 17o
    Cytotoxicity against human DU145 cells after 72 hrs by MTS assay
    Cytotoxicity against human DU145 cells after 72 hrs by MTS assay
    [PMID: 21788134]
    DU-145 EC50
    22.7 3
    Compound: 17o
    Cytotoxicity against human DU145 cells after 72 hrs by MTS assay
    Cytotoxicity against human DU145 cells after 72 hrs by MTS assay
    [PMID: 21788134]
    DU-145 IC50
    23 3
    Compound: 9, BP-1-102
    Cytotoxicity against human DU145 cells assessed as cell viability after 72 hrs by MTS assay
    Cytotoxicity against human DU145 cells assessed as cell viability after 72 hrs by MTS assay
    [PMID: 23968501]
    DU-145 IC50
    23 3
    Compound: 9, BP-1-102
    Cytotoxicity against human DU145 cells assessed as cell viability after 72 hrs by MTS assay
    Cytotoxicity against human DU145 cells assessed as cell viability after 72 hrs by MTS assay
    [PMID: 23968501]
    DU-145 IC50
    23 3
    Compound: 9, BP-1-102
    Cytotoxicity against human DU145 cells assessed as cell viability after 72 hrs by MTS assay
    Cytotoxicity against human DU145 cells assessed as cell viability after 72 hrs by MTS assay
    [PMID: 23968501]
    HCT-116 IC50
    15.05 3
    Compound: BP-1-102; 36
    Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay
    Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay
    [PMID: 29674294]
    HCT-116 IC50
    15.05 3
    Compound: BP-1-102; 36
    Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay
    Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay
    [PMID: 29674294]
    HCT-116 IC50
    15.05 3
    Compound: BP-1-102; 36
    Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay
    Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay
    [PMID: 29674294]
    HOS IC50
    6.44 3
    Compound: 1d; BP-1-102
    Antiproliferative activity against human HOS cells assessed as inhibition of cell growth incubated for 48 hrs by cell titer based MTS assay
    Antiproliferative activity against human HOS cells assessed as inhibition of cell growth incubated for 48 hrs by cell titer based MTS assay
    [PMID: 35476936]
    HOS IC50
    6.44 3
    Compound: 1d; BP-1-102
    Antiproliferative activity against human HOS cells assessed as inhibition of cell growth incubated for 48 hrs by cell titer based MTS assay
    Antiproliferative activity against human HOS cells assessed as inhibition of cell growth incubated for 48 hrs by cell titer based MTS assay
    [PMID: 35476936]
    JJN-3 EC50
    16.7 3
    Compound: 17o
    Cytotoxicity against human JJN-3 cells after 72 hrs by MTS assay
    Cytotoxicity against human JJN-3 cells after 72 hrs by MTS assay
    [PMID: 21788134]
    HOS IC50
    6.44 3
    Compound: 1d; BP-1-102
    Antiproliferative activity against human HOS cells assessed as inhibition of cell growth incubated for 48 hrs by cell titer based MTS assay
    Antiproliferative activity against human HOS cells assessed as inhibition of cell growth incubated for 48 hrs by cell titer based MTS assay
    [PMID: 35476936]
    JJN-3 EC50
    16.7 3
    Compound: 17o
    Cytotoxicity against human JJN-3 cells after 72 hrs by MTS assay
    Cytotoxicity against human JJN-3 cells after 72 hrs by MTS assay
    [PMID: 21788134]
    MDA-MB-231 IC50
    6.8 3
    Compound: 14; BP-1-102
    Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay
    [PMID: 28245116]
    JJN-3 EC50
    16.7 3
    Compound: 17o
    Cytotoxicity against human JJN-3 cells after 72 hrs by MTS assay
    Cytotoxicity against human JJN-3 cells after 72 hrs by MTS assay
    [PMID: 21788134]
    MDA-MB-231 IC50
    2 3
    Compound: 3; SH4-54
    Antiproliferative activity against human MDA-MB-231 cells
    Antiproliferative activity against human MDA-MB-231 cells
    [PMID: 34000483]
    MDA-MB-231 IC50
    2 3
    Compound: 3; SH4-54
    Antiproliferative activity against human MDA-MB-231 cells
    Antiproliferative activity against human MDA-MB-231 cells
    [PMID: 34000483]
    MDA-MB-468 EC50
    10.9 3
    Compound: 17o
    Cytotoxicity against human MDA468 cells after 72 hrs by MTS assay
    Cytotoxicity against human MDA468 cells after 72 hrs by MTS assay
    [PMID: 21788134]
    MDA-MB-231 IC50
    6.8 3
    Compound: 14; BP-1-102
    Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay
    [PMID: 28245116]
    MDA-MB-468 IC50
    11 3
    Compound: 9, BP-1-102
    Cytotoxicity against human MDA468 cells assessed as cell viability after 72 hrs by MTS assay
    Cytotoxicity against human MDA468 cells assessed as cell viability after 72 hrs by MTS assay
    [PMID: 23968501]
    MDA-MB-231 IC50
    6.8 3
    Compound: 14; BP-1-102
    Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay
    [PMID: 28245116]
    MDA-MB-468 EC50
    10.9 3
    Compound: 17o
    Cytotoxicity against human MDA468 cells after 72 hrs by MTS assay
    Cytotoxicity against human MDA468 cells after 72 hrs by MTS assay
    [PMID: 21788134]
    MDA-MB-468 EC50
    10.9 3
    Compound: 17o
    Cytotoxicity against human MDA468 cells after 72 hrs by MTS assay
    Cytotoxicity against human MDA468 cells after 72 hrs by MTS assay
    [PMID: 21788134]
    MG-63 IC50
    12.66 3
    Compound: 1d; BP-1-102
    Antiproliferative activity against human MG-63 cells assessed as inhibition of cell growth incubated for 48 hrs by cell titer based MTS assay
    Antiproliferative activity against human MG-63 cells assessed as inhibition of cell growth incubated for 48 hrs by cell titer based MTS assay
    [PMID: 35476936]
    MDA-MB-468 IC50
    11 3
    Compound: 9, BP-1-102
    Cytotoxicity against human MDA468 cells assessed as cell viability after 72 hrs by MTS assay
    Cytotoxicity against human MDA468 cells assessed as cell viability after 72 hrs by MTS assay
    [PMID: 23968501]
    MDA-MB-468 IC50
    11 3
    Compound: 9, BP-1-102
    Cytotoxicity against human MDA468 cells assessed as cell viability after 72 hrs by MTS assay
    Cytotoxicity against human MDA468 cells assessed as cell viability after 72 hrs by MTS assay
    [PMID: 23968501]
    OCI-AML2 IC50
    10 3
    Compound: 9, BP-1-102
    Cytotoxicity against human OCI-AML2 cells assessed as cell viability after 72 hrs by MTS assay
    Cytotoxicity against human OCI-AML2 cells assessed as cell viability after 72 hrs by MTS assay
    [PMID: 23968501]
    MG-63 IC50
    12.66 3
    Compound: 1d; BP-1-102
    Antiproliferative activity against human MG-63 cells assessed as inhibition of cell growth incubated for 48 hrs by cell titer based MTS assay
    Antiproliferative activity against human MG-63 cells assessed as inhibition of cell growth incubated for 48 hrs by cell titer based MTS assay
    [PMID: 35476936]
    MG-63 IC50
    12.66 3
    Compound: 1d; BP-1-102
    Antiproliferative activity against human MG-63 cells assessed as inhibition of cell growth incubated for 48 hrs by cell titer based MTS assay
    Antiproliferative activity against human MG-63 cells assessed as inhibition of cell growth incubated for 48 hrs by cell titer based MTS assay
    [PMID: 35476936]
    U2OS IC50
    8.3 3
    Compound: 14; BP-1-102
    Antiproliferative activity against human U2OS cells after 24 hrs by MTT assay
    Antiproliferative activity against human U2OS cells after 24 hrs by MTT assay
    [PMID: 28245116]
    MGC-803 IC50
    5.6 3
    Compound: 3; SH4-54
    Antiproliferative activity against human MGC-803 cells
    Antiproliferative activity against human MGC-803 cells
    [PMID: 34000483]
    MGC-803 IC50
    5.6 3
    Compound: 3; SH4-54
    Antiproliferative activity against human MGC-803 cells
    Antiproliferative activity against human MGC-803 cells
    [PMID: 34000483]
    OCI-AML2 IC50
    10 3
    Compound: 9, BP-1-102
    Cytotoxicity against human OCI-AML2 cells assessed as cell viability after 72 hrs by MTS assay
    Cytotoxicity against human OCI-AML2 cells assessed as cell viability after 72 hrs by MTS assay
    [PMID: 23968501]
    OCI-AML2 IC50
    10 3
    Compound: 9, BP-1-102
    Cytotoxicity against human OCI-AML2 cells assessed as cell viability after 72 hrs by MTS assay
    Cytotoxicity against human OCI-AML2 cells assessed as cell viability after 72 hrs by MTS assay
    [PMID: 23968501]
    U2OS IC50
    8.3 3
    Compound: 14; BP-1-102
    Antiproliferative activity against human U2OS cells after 24 hrs by MTT assay
    Antiproliferative activity against human U2OS cells after 24 hrs by MTT assay
    [PMID: 28245116]
    U2OS IC50
    8.3 3
    Compound: 14; BP-1-102
    Antiproliferative activity against human U2OS cells after 24 hrs by MTT assay
    Antiproliferative activity against human U2OS cells after 24 hrs by MTT assay
    [PMID: 28245116]
    In Vitro

    BP-1-102 binds Stat3 with an affinity KD of 504 nM. BP-1-102 inhibits Stat3 DNA-binding activity in vitro, with an IC50 value of 6.8±0.8 μM. It blocks Stat3-phospho-tyrosine peptide interactions and Stat3 activation at 4-6.8 μM, and selectively inhibits growth, survival, migration, and invasion of Stat3-dependent tumor cells. BP-1-102-mediated inhibition of aberrantly active Stat3 in tumor cells suppresses the expression of c-Myc, Cyclin D1, Bcl-xL, Survivin, VEGF, and Krüppel-like factor 8[1].

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

    In Vivo

    Mice therapeutically given BP-1-102, an orally bioavailable compound targeting STAT3/NF-kB activation and cross-talk, exhibit reduced colon tumorigenesis and diminished expression of STAT3/NF-kB-activating cytokines in the neoplastic areas[2]. BP-1-102 is orally bioavailable and that the agent accumulates in tumor tissues at levels sufficient to inhibit aberrantly active Stat3 functions and inhibit tumor growth[1].

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

    Peso molecular

    626.59

    Fòrmula

    C29H27F5N2O6S

    No. CAS
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(O)C1=CC=C(N(CC2=CC=C(C3CCCCC3)C=C2)C(CN(C)S(=O)(C4=C(F)C(F)=C(F)C(F)=C4F)=O)=O)C=C1O

    Envío

    Room temperature in continental US; may vary elsewhere.

    Almacenamiento
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvente y solubilidad
    In Vitro: 

    DMSO : ≥ 33 mg/mL (52.67 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 1.5959 mL 7.9797 mL 15.9594 mL
    5 mM 0.3192 mL 1.5959 mL 3.1919 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.

    • Calculadora de molaridad

    • Calculadora de dilución

    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)

    C1

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    Volume (start)

    V1

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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 (3.99 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% Corn Oil

      Solubility: ≥ 2.5 mg/mL (3.99 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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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.
    Pureza y Documentación
    Referencias
    Ensayo celular
    [1]

    Proliferating cells in 6- or 96-well plates are treated once with 0-30 μM BP-1-102 for 24 h or with 10 μM BP-1-102 for up to 96 h. Viable cells are counted by trypan blue exclusion/phase-contrast microscopy or assessed by a cell proliferation kit[1].

    MCE no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.

    Administraciòn de animales
    [1]

    Mice: Athymic nude mice with established tumors are grouped and then given BP-1-102 (in 0.05% DMSO in water) at 1 or 3mg/kg (i.v.) every 2 or every 3 d or 3 mg/kg (oral gavage, 100 μL) every day for 15 or 20 d. Animals are monitored every day, and tumor sizes are measured with calipers and body weights are taken every 2 or 3 d. For each treatment group, the tumor volumes for each set of measurements are statistically analyzed in comparison with the control group using a paired T test[1].

    MCE no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.

    Referencias

    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 1.5959 mL 7.9797 mL 15.9594 mL 39.8985 mL
    5 mM 0.3192 mL 1.5959 mL 3.1919 mL 7.9797 mL
    10 mM 0.1596 mL 0.7980 mL 1.5959 mL 3.9898 mL
    15 mM 0.1064 mL 0.5320 mL 1.0640 mL 2.6599 mL
    20 mM 0.0798 mL 0.3990 mL 0.7980 mL 1.9949 mL
    25 mM 0.0638 mL 0.3192 mL 0.6384 mL 1.5959 mL
    30 mM 0.0532 mL 0.2660 mL 0.5320 mL 1.3299 mL
    40 mM 0.0399 mL 0.1995 mL 0.3990 mL 0.9975 mL
    50 mM 0.0319 mL 0.1596 mL 0.3192 mL 0.7980 mL
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    Nombre del producto:
    BP-1-102
    Cat. No.:
    HY-100493
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    MCE Japan Authorized Agent: