1. Protein Tyrosine Kinase/RTK Apoptosis
  2. Bcr-Abl Src Apoptosis
  3. Bafetinib

Bafetinib  (Synonyms: INNO-406; NS-187)

Cat. No.: HY-50868 Purity: 99.77%
COA Handling Instructions

Bafetinib is an orally active Lyn/Bcr-Abl tyrosine kinase inhibitor. Bafetinib enhances the activity of several pro-apoptotic Bcl-2 homology (BH) 3-pure proteins (Bim, Bad, Bmf, and Bik) through intrinsic apoptotic pathways regulated by the Bcl-2 family, and induces apoptosis of Ph+ leukemia cells. Bafetinib has antitumor activity.

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

Bafetinib Chemical Structure

Bafetinib Chemical Structure

CAS No. : 859212-16-1

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 114 In-stock
Solution
10 mM * 1 mL in DMSO USD 114 In-stock
Solid
5 mg USD 90 In-stock
10 mg USD 130 In-stock
50 mg USD 250 In-stock
100 mg USD 450 In-stock
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Customer Review

Based on 10 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Bafetinib purchased from MedChemExpress. Usage Cited in: J Cancer. 2019 Jan 29;10(5):1197-1208.  [Abstract]

    Western blot shows the effects of Bafetinib on expression of Akt, p-Akt, Cyclin D1, cleaved-Caspase3, Caspase9, Bcl-2, LC3II/I, P62 and Lyn.

    View All Src Isoform Specific Products:

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Bafetinib is an orally active Lyn/Bcr-Abl tyrosine kinase inhibitor. Bafetinib enhances the activity of several pro-apoptotic Bcl-2 homology (BH) 3-pure proteins (Bim, Bad, Bmf, and Bik) through intrinsic apoptotic pathways regulated by the Bcl-2 family, and induces apoptosis of Ph+ leukemia cells. Bafetinib has antitumor activity[1][2][3].

    In Vitro

    Bafetinib (0.625, 1.25, 2.5 μM,24 h) inhibits the transcription of PD-L1 in lung cancer cell H292 by c-Myc[1].

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

    Western Blot Analysis[1]

    Cell Line: H292
    Concentration: 0.625, 1.25, 2.5 μM
    Incubation Time: 24 h
    Result: Inhibited the expression of PD-L1 and c-Myc.
    In Vivo

    Bafetinib (30 mg/kg/day, orally, for 10 consecutive days) inhibits the expression of PD-L1 in mouse lung cancer[1].
    Bafetinib (10 mg/kg, gavage, single dose) alleviates pain in mice by inhibiting PAR2-induced TRPV4 channel activation[2].

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

    Animal Model: Murine inflammatory pain model[2]
    Dosage: 10 mg/kg
    Administration: i.g.
    Result: Inhibited PAR2-induced mechanical hyperalgesia.
    Clinical Trial
    Molecular Weight

    576.62

    Formula

    C30H31F3N8O

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C(C1=CC=C(C(C(F)(F)F)=C1)CN2C[C@@H](N(C)C)CC2)NC3=CC=C(C)C(NC4=NC=CC(C5=CN=CN=C5)=N4)=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 : 100 mg/mL (173.42 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 1.7342 mL 8.6712 mL 17.3424 mL
    5 mM 0.3468 mL 1.7342 mL 3.4685 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

    • Dilution Calculator

    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)

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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 (4.34 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 (4.34 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
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

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    Dosing volume
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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    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: 99.77%

    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 1.7342 mL 8.6712 mL 17.3424 mL 43.3561 mL
    5 mM 0.3468 mL 1.7342 mL 3.4685 mL 8.6712 mL
    10 mM 0.1734 mL 0.8671 mL 1.7342 mL 4.3356 mL
    15 mM 0.1156 mL 0.5781 mL 1.1562 mL 2.8904 mL
    20 mM 0.0867 mL 0.4336 mL 0.8671 mL 2.1678 mL
    25 mM 0.0694 mL 0.3468 mL 0.6937 mL 1.7342 mL
    30 mM 0.0578 mL 0.2890 mL 0.5781 mL 1.4452 mL
    40 mM 0.0434 mL 0.2168 mL 0.4336 mL 1.0839 mL
    50 mM 0.0347 mL 0.1734 mL 0.3468 mL 0.8671 mL
    60 mM 0.0289 mL 0.1445 mL 0.2890 mL 0.7226 mL
    80 mM 0.0217 mL 0.1084 mL 0.2168 mL 0.5420 mL
    100 mM 0.0173 mL 0.0867 mL 0.1734 mL 0.4336 mL
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    Bafetinib 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:
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