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

A 419259 trihydrochloride  (Synonyms: RK 20449 trihydrochloride)

目录号: HY-15764A 纯度: 99.21%
COA 产品使用指南

A 419259 trihydrochloride 是 Src 家族激酶抑制剂,对 SrcLckLynIC50 分别为 9 nM,3 nM,3 nM。A 419259 trihydrochloride 可诱导细胞凋亡 (apoptosis)。

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A 419259 trihydrochloride Chemical Structure

A 419259 trihydrochloride Chemical Structure

CAS No. : 1435934-25-0

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规格 价格 是否有货 数量
10 mM * 1 mL in Water ¥1693
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1 mg ¥590
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5 mg ¥1300
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10 mg ¥1814
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50 mg ¥6300
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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 2 篇科研文献

WB

    A 419259 trihydrochloride purchased from MCE. 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.

    查看 Src 亚型特异性产品:

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    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]

    体外研究
    (In Vitro)

    "A419259 是第二代吡咯并嘧啶,可阻断 CML 细胞系的增殖并诱导细胞凋亡。它 诱导 K-562 细胞凋亡,还抑制 Meg-01 增殖 (IC50=0.1 μM)[1]
    在没有 IL-3 的情况下,A-419259 会强烈抑制 DAGM/Bcr-Abl 细胞增殖 (IC50=0.1-0.3 μM)[1]
    A-419259 还抑制 CML 细胞系中的整体 SFK 活性,可阻断Src 激酶激活 (IC50=0.1-0.3 μM)[1]
    A 419259 trihydrochloride (1 μM;16 h) 抑制内源 SFK (c-Src 和 Lck) 活性,从而抑制 Src 的驱动 mES 细胞向原始外胚层样细胞分化[2]
    A 419259 trihydrochloride (0.3, 1 μM;5 天) 对 mTeSR 培养基中生长的 hES 细胞的未分化集落形态没有影响[2]
    "

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

    分子量

    592.00

    Formula

    C29H37Cl3N6O

    CAS 号
    性状

    固体

    颜色

    White to yellow

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, sealed storage, away from moisture

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

    溶解性数据
    In Vitro: 

    H2O 中的溶解度 : 50 mg/mL (84.46 mM; 超声助溶)

    DMSO 中的溶解度 : 1 mg/mL (1.69 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 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
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    • 摩尔计算器

    • 稀释计算器

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

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    In Vivo:

    以下溶解方案,请直接配置工作液。建议现用现配,在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比; 如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶。

    • 方案 一

      请依序添加每种溶剂: PBS

      Solubility: 100 mg/mL (168.92 mM); 澄清溶液; 超声助溶

    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
    您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
    纯度 & 产品资料

    纯度: 99.21%

    参考文献
    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.

    参考文献

    A 419259 trihydrochloride 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 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

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

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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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    产品名称:
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    目录号:
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