1. JAK/STAT Signaling Stem Cell/Wnt
  2. STAT
  3. Napabucasin

Napabucasin (BBI608) is a STAT3 inhibitor which blocks stem cell activity in cancer cells.

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

Napabucasin Chemical Structure

Napabucasin Chemical Structure

CAS No. : 83280-65-3

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Customer Review

Based on 21 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Napabucasin purchased from MedChemExpress. Usage Cited in: Cancer Med. 2016 Jun;5(6):1251-8.  [Abstract]

    Representative images of colony formation assay in PCa cell lines (PC-3 and 22RV1) and histological analysis of the colony number show that the colony formation of PCa cell lines are dramatically decreased after treated with 1 μM Napabucasin for 24 h.

    View All STAT Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Napabucasin (BBI608) is a STAT3 inhibitor which blocks stem cell activity in cancer cells.

    IC50 & Target[1]

    STAT3

     

    Cellular Effect
    Cell Line Type Value Description References
    A549 IC50
    0.12 μM
    Compound: 6; BBI608
    Cytotoxicity against human A549 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay
    Cytotoxicity against human A549 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay
    [PMID: 32044231]
    A549 IC50
    0.74 μM
    Compound: Nap; BBI608
    Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay
    [PMID: 28558333]
    A549 IC50
    6.69 μM
    Compound: BBI608
    Antiproliferative activity against human A549 cells assessed as reduction in cell viability measured after 48 hrs MTT assay
    Antiproliferative activity against human A549 cells assessed as reduction in cell viability measured after 48 hrs MTT assay
    [PMID: 32631508]
    AGS IC50
    437 nM
    Compound: BBI608
    Antiproliferative activity against human AGS cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
    Antiproliferative activity against human AGS cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
    [PMID: 36103247]
    BXPC-3 IC50
    1.3 μM
    Compound: NP
    Antiproliferative activity against human BxPC-3 cells harboring ZFP91siRNA assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    Antiproliferative activity against human BxPC-3 cells harboring ZFP91siRNA assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    [PMID: 33506674]
    BXPC-3 IC50
    1.4 μM
    Compound: NP
    Antiproliferative activity against human BxPC-3 cells assessed as reduction in cell viability incubated for 3 days by MTT assay
    Antiproliferative activity against human BxPC-3 cells assessed as reduction in cell viability incubated for 3 days by MTT assay
    [PMID: 33506674]
    BXPC-3 IC50
    1.8 μM
    Compound: NP
    Antiproliferative activity against ZFP91 knockdown human BxPC-3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    Antiproliferative activity against ZFP91 knockdown human BxPC-3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    [PMID: 33506674]
    BXPC-3 IC50
    1962 nM
    Compound: 1c; BBI608
    Inhibition of ATP production in human BXPC-3 cells incubated for 20 to 24 hrs by ATP assay kit method
    Inhibition of ATP production in human BXPC-3 cells incubated for 20 to 24 hrs by ATP assay kit method
    [PMID: 36282975]
    BXPC-3 IC50
    5306 nM
    Compound: 1c; BBI608
    Anti-proliferative activity against human BXPC-3 cells assessed as cell growth inhibition incubated for 72 hrs by MTS assay
    Anti-proliferative activity against human BXPC-3 cells assessed as cell growth inhibition incubated for 72 hrs by MTS assay
    [PMID: 36282975]
    Capan-2 IC50
    1586 nM
    Compound: 1c; BBI608
    Anti-proliferative activity against human Capan-2 cells assessed as cell growth inhibition incubated for 72 hrs by MTS assay
    Anti-proliferative activity against human Capan-2 cells assessed as cell growth inhibition incubated for 72 hrs by MTS assay
    [PMID: 36282975]
    CT26 IC50
    2.5 μM
    Compound: Napabucasin
    Antiproliferative activity against mouse CT26 cells after 72 hrs by MTT assay
    Antiproliferative activity against mouse CT26 cells after 72 hrs by MTT assay
    [PMID: 30472602]
    DU-145 IC50
    23.04 nM
    Compound: 3
    Anticancer activity against human DU145 cells after 72 hrs by XTT assay
    Anticancer activity against human DU145 cells after 72 hrs by XTT assay
    [PMID: 18829316]
    HaCaT IC50
    0.5 μM
    Compound: 4a
    Antihyperproliferative activity against human HaCaT cells after 48 hrs by phase contrast microscopy
    Antihyperproliferative activity against human HaCaT cells after 48 hrs by phase contrast microscopy
    [PMID: 22845014]
    HCT-116 IC50
    0.3 μM
    Compound: 87; BBI608
    Antiproliferative activity against human HCT-116 cells assessed as reduction in cell proliferation incubated for 72 hrs by CellTiter-Glo assay
    Antiproliferative activity against human HCT-116 cells assessed as reduction in cell proliferation incubated for 72 hrs by CellTiter-Glo assay
    [PMID: 33445154]
    HEK293 IC50
    10.4 μM
    Compound: NP
    Antiproliferative activity against human HEK293 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
    Antiproliferative activity against human HEK293 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
    [PMID: 33506674]
    HepG2 IC50
    0.66 μM
    Compound: Nap; BBI608
    Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay
    [PMID: 28558333]
    HepG2 IC50
    0.84 μM
    Compound: BBI608
    Antiproliferative activity against human HepG2 cells overexpressed STAT3 assessed as reduction in cell growth incubated for 48 hrs by CCK-8 assay
    Antiproliferative activity against human HepG2 cells overexpressed STAT3 assessed as reduction in cell growth incubated for 48 hrs by CCK-8 assay
    [PMID: 32603980]
    HepG2 IC50
    10.2 μM
    Compound: BBI 608
    Antiproliferative activity against human HepG2 cells after 48 hrs by CCK-8 assay
    Antiproliferative activity against human HepG2 cells after 48 hrs by CCK-8 assay
    [PMID: 29604543]
    HepG2 IC50
    6.6 μM
    Compound: Napabucasin
    Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay
    Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay
    [PMID: 30472602]
    HT-29 IC50
    0.14 μM
    Compound: BBI608
    Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability measured after 48 hrs MTT assay
    Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability measured after 48 hrs MTT assay
    [PMID: 32631508]
    HT-29 IC50
    1.6 μM
    Compound: Napabucasin
    Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay
    Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay
    [PMID: 30472602]
    HUVEC IC50
    41.28 μM
    Compound: BBI608
    Antiproliferative activity against human HUVEC cells assessed as inhibition of cell growth in measured after 72 hrs by MTT assay
    Antiproliferative activity against human HUVEC cells assessed as inhibition of cell growth in measured after 72 hrs by MTT assay
    [PMID: 34435487]
    K562 IC50
    1 μM
    Compound: 6
    Antiproliferative activity against human K562 cells measured after 48 hrs by MTT assay
    Antiproliferative activity against human K562 cells measured after 48 hrs by MTT assay
    [PMID: 30003778]
    L02 IC50
    18.7 μM
    Compound: BBI 608
    Antiproliferative activity against human L02 cells after 48 hrs by CCK-8 assay
    Antiproliferative activity against human L02 cells after 48 hrs by CCK-8 assay
    [PMID: 29604543]
    MCF-10A IC50
    0.54 μM
    Compound: BBI608
    Cytotoxicity against human MCF10A cells assessed as reduction in cell viability measured after 48 hrs MTT assay
    Cytotoxicity against human MCF10A cells assessed as reduction in cell viability measured after 48 hrs MTT assay
    [PMID: 32631508]
    MCF7 IC50
    < 1 μM
    Compound: 6; BBI608
    Inhibition of IL-6 induced STAT3 phosphorylation at Tyr705 residue in human MCF7 cells preincubated for 1 hr followed by IL-6 stimulation and measured after 1 hr by Western blot analysis
    Inhibition of IL-6 induced STAT3 phosphorylation at Tyr705 residue in human MCF7 cells preincubated for 1 hr followed by IL-6 stimulation and measured after 1 hr by Western blot analysis
    [PMID: 32044231]
    MCF7 IC50
    0.24 μM
    Compound: 6; BBI608
    Cytotoxicity against human MCF7 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay
    Cytotoxicity against human MCF7 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay
    [PMID: 32044231]
    MCF7 IC50
    0.63 μM
    Compound: BBI608
    Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured after 48 hrs MTT assay
    Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured after 48 hrs MTT assay
    [PMID: 32631508]
    MCF7 EC50
    1.49 μM
    Compound: BBI-608
    Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by CyQuant assay
    Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by CyQuant assay
    [PMID: 33352047]
    MCF7 IC50
    11.42 μM
    Compound: BBI608
    Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
    [PMID: 34435487]
    MDA-MB-231 IC50
    0.25 μM
    Compound: 6; BBI608
    Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay
    Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay
    [PMID: 32044231]
    MDA-MB-231 IC50
    0.34 μM
    Compound: Nap; BBI608
    Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay
    [PMID: 28558333]
    MDA-MB-231 IC50
    0.7 μM
    Compound: BBI608
    Antiproliferative activity against human MDA-MB-231 cells overexpressing STAT3 assessed as reduction in cell growth incubated for 48 hrs by CCK-8 assay
    Antiproliferative activity against human MDA-MB-231 cells overexpressing STAT3 assessed as reduction in cell growth incubated for 48 hrs by CCK-8 assay
    [PMID: 32603980]
    MDA-MB-231 IC50
    1.29 μM
    Compound: BBI608
    Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 48 hrs MTT assay
    Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 48 hrs MTT assay
    [PMID: 32631508]
    MDA-MB-231 EC50
    1.8 μM
    Compound: BBI-608
    Antiproliferative activity against human MDA-MB-231 cells harbouring STAT3 assessed as reduction in cell viability at upto 10 uM incubated for 72 hrs by CyQuant assay
    Antiproliferative activity against human MDA-MB-231 cells harbouring STAT3 assessed as reduction in cell viability at upto 10 uM incubated for 72 hrs by CyQuant assay
    [PMID: 33352047]
    MDA-MB-231 IC50
    10.97 μM
    Compound: BBI608
    Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
    [PMID: 34435487]
    MDA-MB-231 IC50
    2.1 μM
    Compound: 6
    Antiproliferative activity against human MDA-MB-231 cells measured after 48 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells measured after 48 hrs by MTT assay
    [PMID: 30003778]
    MDA-MB-231 IC50
    9.68 μM
    Compound: BBI608
    Antiproliferative activity against human drug tolerant MDA-MB-231/lapatinib cells assessed as inhibition of cell growth in measured after 72 hrs by MTT assay
    Antiproliferative activity against human drug tolerant MDA-MB-231/lapatinib cells assessed as inhibition of cell growth in measured after 72 hrs by MTT assay
    [PMID: 34435487]
    MDA-MB-468 IC50
    1.14 μM
    Compound: 1; BBI608
    Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell growth measured after 48 hrs by CCK8 assay
    Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell growth measured after 48 hrs by CCK8 assay
    [PMID: 33126089]
    MDA-MB-468 IC50
    1.14 μM
    Compound: BBI608
    Antiproliferative activity against human MDA-MB-468 cells overexpressing STAT3 assessed as reduction in cell growth incubated for 48 hrs by CCK-8 assay
    Antiproliferative activity against human MDA-MB-468 cells overexpressing STAT3 assessed as reduction in cell growth incubated for 48 hrs by CCK-8 assay
    [PMID: 32603980]
    MGC-803 IC50
    871.8 nM
    Compound: BBI608
    Antiproliferative activity against human MGC-803 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
    Antiproliferative activity against human MGC-803 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
    [PMID: 36103247]
    MIA PaCa-2 IC50
    1.2 μM
    Compound: NP
    Antiproliferative activity against human MIA PaCa-2 cells assessed as reduction in cell viability incubated for 3 days by MTT assay
    Antiproliferative activity against human MIA PaCa-2 cells assessed as reduction in cell viability incubated for 3 days by MTT assay
    [PMID: 33506674]
    MKN-45 IC50
    3943 nM
    Compound: BBI608
    Antiproliferative activity against human MKN-45 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
    Antiproliferative activity against human MKN-45 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
    [PMID: 36103247]
    PC-3 IC50
    5.25 μM
    Compound: Napabucasin
    Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay
    Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay
    [PMID: 30472602]
    U-251 IC50
    2.6 μM
    Compound: Napabucasin
    Antiproliferative activity against human U251 cells after 72 hrs by MTT assay
    Antiproliferative activity against human U251 cells after 72 hrs by MTT assay
    [PMID: 30472602]
    In Vitro

    Napabucasin inhibits the expressions of stemness markers and kill stemness-high cancer cells isolated from several kinds of tumors except PCa. Napabucasin not only inhibits cell proliferation, cell motility, cell survival, colony formation ability, and tumorigenic potential of PCa cells, and increases cell apoptosis and sensitivity to docetaxel, but also effectively blocks sphere formation of PrCSCs and kill them as well as inhibits stemness gene expression. Napabucasin inhibits cell proliferation in PC-3 cells and 22RV1 cells at 48, 72, 96, and 120 h (P<0.05). Cell motility and colony formation ability are closely correlated with the process of tumor metastasis. Napabucasin significantly decreases colony formation and cell motility ability of PCa cell lines in vitro (P<0.05). The proliferation of PC-3 and 22RV1 cells treated with 1 μM Napabucasin are significantly decreased from day 2 to 5 compared with the control group (P<0.05)[1].

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

    In Vivo

    Napabucasin (40 mg/kg) or Docetaxel significantly reduces xenograft tumor growth and tumor volume (TV) compared with PBS (P<0.05). Notably, while no differences are observed between the Napabucasin and the docetaxel groups in PC-3 mouse xenograft models, the TV in Napabucasin group is even lower than docetaxel group in 22RV1 mouse xenograft models (P<0.05). Additionally, Napabucasin or docetaxel also significantly reduces tumor weight compared with PBS (P<0.05)[1].

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

    Clinical Trial
    Molecular Weight

    240.21

    Formula

    C14H8O4

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to green yellow

    SMILES

    O=C(C1=C2OC(C(C)=O)=C1)C3=C(C2=O)C=CC=C3

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 4.44 mg/mL (18.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 4.1630 mL 20.8151 mL 41.6302 mL
    5 mM 0.8326 mL 4.1630 mL 8.3260 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.

    • Molarity Calculator

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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: 0.5 mg/mL (2.08 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 0.5 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 (5.0 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% (20% SBE-β-CD in Saline)

      Solubility: 0.5 mg/mL (2.08 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 0.5 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 (5.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    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.
    Purity & Documentation

    Purity: 99.94%

    References
    Cell Assay
    [1]

    The antiproliferative activity of Napabucasin against the PCa cell lines PC-3 and 22RV1 is examined. For cell proliferation assay, the PCa cell lines (22RV1 and PC-3) are seeded in 96-well plates at 2×103 cells/well in a final volume of 100 μL and incubated overnight. The proliferation of PC-3 and 22RV1 cells treated with 1 μM Napabucasin. The viability of cells is determined with CellTiter 96 non-radioactive cell proliferation assay (MTS). For colony formation assay, cells are placed in a six-well plate and maintained in RPMI-1640 supplemented with 10% FBS for 2 weeks. The colonies are fixed with 4% paraformaldehyde, stained with 0.1% crystal violet and counted[1].

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

    Animal Administration
    [1]

    Mice[1]
    A total of 1×106 PC-3 cells or 8×106 22RV1 cells in 100 μL of PBS are injected subcutaneously into dorsal flanks of an immunodeficient nude mouse. The animals are treated i.p. with Napabucasin (40 mg/kg), Docetaxel (10 mg/kg), or PBS q3d once the tumors have reached 50 mm3. The tumor volume (TV) is calculated every 4 days according to the following standard formula: TV (mm3)=length×width2×0.5.

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

    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, 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 4.1630 mL 20.8151 mL 41.6302 mL 104.0756 mL
    5 mM 0.8326 mL 4.1630 mL 8.3260 mL 20.8151 mL
    10 mM 0.4163 mL 2.0815 mL 4.1630 mL 10.4076 mL
    15 mM 0.2775 mL 1.3877 mL 2.7753 mL 6.9384 mL
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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.

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    Product Name:
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    Cat. No.:
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