2. Protein Tyrosine Kinase/RTK Apoptosis
  3. Src Apoptosis
  4. A 419259

A 419259 is a broad-spectrum pyrrolo-pyrimidine inhibitor, has high selectivity towards the Src family. A 419259 shows inhibitory effect for Src, Lck and Lyn with IC50 of 9 nM, <3 nM and <3 nM, respectively.

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

A 419259 Chemical Structure

A 419259 Chemical Structure

CAS No. : 364042-47-7

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5 mg USD 140 In-stock
10 mg USD 238 In-stock
50 mg USD 710 In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of A 419259:

A 419259 Related Antibodies

Top Publications Citing Use of Products

    A 419259 purchased from MedChemExpress. Usage Cited in: Blood. 2016 Jun 23;127(25):3237-52.  [Abstract]

    PCI-32765 binds to the ATP-binding pocketof HCK and blocks ATP binding. Results from kinase active-site inhibition assaysutilizing an ATP-BTN probe that is used to pull downactive kinases in the presence of PCI-32765, CC-292, or A419259 in lysates from BCWM.1 WM cells.

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    Lck

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    A 419259 is a broad-spectrum pyrrolo-pyrimidine inhibitor, has high selectivity towards the Src family. A 419259 shows inhibitory effect for Src, Lck and Lyn with IC50 of 9 nM, <3 nM and <3 nM, respectively[1][2].

    IC50 & Target

    IC50: 9 nM (Src), <3 nM (Lck), <3 nM (Lyn), 3 μM (Abl)[1]
    In Vitro

    "A419259 is a second-generation pyrrolopyrimidine that blocks proliferation and induces apoptosis in CML cell lines. It induces apoptosis in K-562 cells and also inhibits Meg-01 proliferation (IC50=0.1 μM)[1].
    In the absence of IL-3, A-419259 strongly inhibits DAGM/Bcr-Abl cell proliferation (IC50=0.1-0.3 μM)[1].
    A-419259 also inhibits overall SFK activity in CML cell lines and blocks Src kinase activation (IC50=0.1-0.3 μM)[1].
    A 419259 (1 μM; 16 h) inhibits endogenous SFK (c-Src and Lck) activity, thereby inhibiting Src-driven differentiation of mES cells toward primitive ectoderm-like cells[2].
    A 419259 (0.3, 1 μM; 5 days) has no effect on undifferentiated colony morphology of hES cells grown in mTeSR medium[2].
    "

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

    A 419259 Related Antibodies
    Molecular Weight

    482.62

    Formula

    C29H34N6O
    CAS No.
    Appearance

    Solid

    Color

    Off-white to light yellow

    SMILES

    NC1=C2C(N([C@H]3CC[C@H](N4CCN(C)CC4)CC3)C=C2C5=CC=C(OC6=CC=CC=C6)C=C5)=NC=N1
    Shipping

    Room temperature in continental US; may vary elsewhere.
    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 : 100 mg/mL (207.20 mM; ultrasonic and warming and heat to 60°C; 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 2.0720 mL 10.3601 mL 20.7202 mL
    5 mM 0.4144 mL 2.0720 mL 4.1440 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Concentration
    ×
    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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 (5.18 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% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.18 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 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
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    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
    References
    Kinase Assay
    [1]

    In vitro kinase assays are performed on His(6)-tagged Lck (residues 62-509) and full-length c-Abl purified from Sf-9 cells, and commercial sources of Lyn, Src and PKC. Lck, Lyn, Src and Abl activities are measured with an ELISA-based assay. Flat bottom 96-well ELISA plates are incubated with a 200 μg/mL solution of Poly(Glu,Tyr) 4 : 1 substrate in phosphate buffered saline (PBS) for 1 h at 37°C and then washed with PBS containing 0.1% Tween-20 (PBS-T). Inhibitor dilutions are added to the washed plates already containing the appropriate enzyme in kinase assay buffer (250 mM Mopso, pH 6.75, 10 mM MgCl2, 2 mM MnCl2, 2.5 mM DTT, 0.02% BSA, 2 mM Na3VO4, 5% DMSO, 5 μM ATP). After incubation at room temperature for 20 min, plates are washed three times with PBS-T and plate-bound phosphotyrosine is detected with an anti-phosphotyrosine-HRP antibody conjugate and subsequent color development with K-Blue reagents. All assays are optimized to use the least amount of enzyme necessary for a reproducible signal-to-noise ratio[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Cell Assay
    [1]

    K-562 cells are grown in RPMI 1640 supplemented with 10% fetal calf serum (FCS), and 50 g/mL Gentamycin. Meg-01 cells are cultured in Vitacell modified RPMI 1640 (ATCC), supplemented with 10% FCS and 50 μg/mL Gentamycin. The human GM-CSF-dependent myeloid leukemia cell line TF-1 is grown in RPMI 1640 supplemented with 10% FCS, 50 μg/mL Gentamycin, and 1 ng/mL of recombinant human GM-CSF. DAGM murine myeloid leukemia cells are cultured in RPMI 1640 supplemented with 10% FCS, 50 μg/mL Gentamycin, and 0.5 ng/mL recombinant IL-3. Concentrated stock solutions of PP2 (5 mM) and A-419259 (2 mM) are prepared in DMSO and stored at -20°C. Cellular proliferation is measured using the Live/Dead growth assay. This assay employs calcein-AM, a fluorogenic esterase substrate that is taken up by viable cells and hydrolyzed intracellularly, releasing a green fluorescent product. Briefly, 104 cells are plated per well in 96-well plates for each day of a 4-day time course. Various concentrations of PP2, A-419259 or vehicle control are added to the wells (five wells per concentration per day) and the plates are incubated at 37°C. At each time point, one plate is centrifuged at 1500 g for 10 min to pellet the cells. Cells are washed with phosphate buffered saline (PBS), and calcein-AM is added to each well to a final concentration of 1 μM. Plates are incubated in the dark at room temperature for 1 h. The plates are then read at 485/530 nm (excitation/emission) using a SpectraMax Gemini XS fluorescent plate reader and data are analysed with SoftMax Pro software[1].

    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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.0720 mL 10.3601 mL 20.7202 mL 51.8006 mL
    5 mM 0.4144 mL 2.0720 mL 4.1440 mL 10.3601 mL
    10 mM 0.2072 mL 1.0360 mL 2.0720 mL 5.1801 mL
    15 mM 0.1381 mL 0.6907 mL 1.3813 mL 3.4534 mL
    20 mM 0.1036 mL 0.5180 mL 1.0360 mL 2.5900 mL
    25 mM 0.0829 mL 0.4144 mL 0.8288 mL 2.0720 mL
    30 mM 0.0691 mL 0.3453 mL 0.6907 mL 1.7267 mL
    40 mM 0.0518 mL 0.2590 mL 0.5180 mL 1.2950 mL
    50 mM 0.0414 mL 0.2072 mL 0.4144 mL 1.0360 mL
    60 mM 0.0345 mL 0.1727 mL 0.3453 mL 0.8633 mL
    80 mM 0.0259 mL 0.1295 mL 0.2590 mL 0.6475 mL
    100 mM 0.0207 mL 0.1036 mL 0.2072 mL 0.5180 mL
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    A 419259 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.

    Keywords:

    A 419259364042-47-7RK-20449A419259A-419259RK20449RK 20449SrcApoptosisInhibitorinhibitorinhibit

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