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

A 419259 trihydrochloride  (Synonyms: RK 20449 trihydrochloride)

Cat. No.: HY-15764A Purity: 99.21%
SDS COA Handling Instructions

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A 419259 trihydrochloride is a Src family kinases inhibitor with IC50s of 9 nM, 3 nM and 3 nM for Src, Lck and Lyn, respectively.

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

A 419259 trihydrochloride Chemical Structure

A 419259 trihydrochloride Chemical Structure

CAS No. : 1435934-25-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water
ready for reconstitution
 USD 186 In-stock
Solution
10 mM * 1 mL in Water USD 186 In-stock
Solid
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 trihydrochloride:

A 419259 trihydrochloride Related Antibodies

Top Publications Citing Use of Products

2 Publications Citing Use of MCE A 419259 trihydrochloride

WB

    A 419259 trihydrochloride 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 Fyn Blk

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    A 419259 trihydrochloride is a Src family kinases inhibitor with IC50s of 9 nM, 3 nM and 3 nM for Src, Lck and Lyn, 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 trihydrochloride (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 trihydrochloride (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 trihydrochloride Related Antibodies
    Molecular Weight

    592.00

    Formula

    C29H37Cl3N6O
    CAS No.
    Appearance

    Solid

    Color

    White to 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.[H]Cl.[H]Cl.[H]Cl
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    H2O : 50 mg/mL (84.46 mM; Need ultrasonic)

    DMSO : 1 mg/mL (1.69 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 1.6892 mL 8.4459 mL 16.8919 mL
    5 mM 0.3378 mL 1.6892 mL 3.3784 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • 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)

    C1

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    Volume (start)

    V1

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    Concentration (final)

    C2

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    In Vivo:

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  PBS

      Solubility: 100 mg/mL (168.92 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    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).
    Purity & Documentation

    Purity: 99.21%

    SDS (252 KB)

    COA (254 KB) LCMS (120 KB)

    Handling Instructions (2659 KB)
    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 (sealed storage, away from moisture). 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 / H2O 1 mM 1.6892 mL 8.4459 mL 16.8919 mL 42.2297 mL
    H2O 5 mM 0.3378 mL 1.6892 mL 3.3784 mL 8.4459 mL
    10 mM 0.1689 mL 0.8446 mL 1.6892 mL 4.2230 mL
    15 mM 0.1126 mL 0.5631 mL 1.1261 mL 2.8153 mL
    20 mM 0.0845 mL 0.4223 mL 0.8446 mL 2.1115 mL
    25 mM 0.0676 mL 0.3378 mL 0.6757 mL 1.6892 mL
    30 mM 0.0563 mL 0.2815 mL 0.5631 mL 1.4077 mL
    40 mM 0.0422 mL 0.2111 mL 0.4223 mL 1.0557 mL
    50 mM 0.0338 mL 0.1689 mL 0.3378 mL 0.8446 mL
    60 mM 0.0282 mL 0.1408 mL 0.2815 mL 0.7038 mL
    80 mM 0.0211 mL 0.1056 mL 0.2111 mL 0.5279 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    A 419259 trihydrochloride 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 419259 trihydrochloride1435934-25-0RK 20449 trihydrochlorideSrcApoptosisInhibitorinhibitorinhibit

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