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

A 419259 GMP is the GMP grade A 419259 (HY-15764), inducing cell apoptosis. GMP-grade small molecules can be used as auxiliary reagents in cell therapy. A 419259 (RK-20449) is a broad-spectrum pyrrole-pyrimidine inhibitor targeting Src, Lck, and Lyn with IC50s 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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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of A 419259:

Top Publications Citing Use of Products

1 Publications Citing Use of MCE A 419259

WB

    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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    Description

    A 419259 GMP is the GMP grade A 419259 (HY-15764), inducing cell apoptosis. GMP-grade small molecules can be used as auxiliary reagents in cell therapy. A 419259 (RK-20449) is a broad-spectrum pyrrole-pyrimidine inhibitor targeting Src, Lck, and Lyn with IC50s 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 GMP (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 GMP (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.

    Molecular Weight

    482.63

    Formula

    C29H34N6O

    CAS No.
    Appearance

    Solid

    Color

    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

    Please store the product under the recommended conditions in the Certificate of Analysis.

    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (207.20 mM; Need ultrasonic and warming; 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 10.3599 mL 20.7198 mL
    5 mM 0.4144 mL 2.0720 mL 4.1440 mL
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    Complete Stock Solution Preparation Table

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.0720 mL 10.3599 mL 20.7198 mL 51.7995 mL
    5 mM 0.4144 mL 2.0720 mL 4.1440 mL 10.3599 mL
    10 mM 0.2072 mL 1.0360 mL 2.0720 mL 5.1800 mL
    15 mM 0.1381 mL 0.6907 mL 1.3813 mL 3.4533 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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    • 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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    Inquiry Information

    Product Name:
    A 419259
    Cat. No.:
    HY-15764G
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