2. Protein Tyrosine Kinase/RTK Autophagy
  3. Src Autophagy
  4. Saracatinib

Saracatinib  (Synonyms: 塞卡替尼; AZD0530)

目录号: HY-10234 纯度: 99.92%
COA 产品使用指南

摩尔计算器

Saracatinib (AZD0530) 是一种有效的 Src 抑制剂，抑制 c-Src，Lck，c-YES，Lyn，Fyn，Fgr 和 Blk 的 IC50 值为 2.7-11 nM，对其他酪氨酸激酶具有选择性。

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Saracatinib Chemical Structure

Saracatinib Chemical Structure

CAS No. : 379231-04-6

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥572
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1 mg ￥162
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5 mg ￥325
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10 mg ￥520
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50 mg ￥1410
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100 mg ￥2640
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500 mg   询价  

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Customer Review

Other Forms of Saracatinib:

Saracatinib 相关抗体

Top Publications Citing Use of Products

    Saracatinib purchased from MCE. Usage Cited in: Signal Transduct Target Ther. 2023 Feb 17;8(1):66.  [Abstract]

    Saracatinib (10 μM) reduces BLK-mediated FAM83A tyrosine phosphorylation in HEK293T cells.

    Saracatinib purchased from MCE. Usage Cited in: J Cell Mol Med. 2019 Apr;23(4):2399-2409.  [Abstract]

    Immunoblot analysis of p-JNK1/2 (T183/Y185) in HepG2 cells treated with saracatinib (10 μM, 12 h) and PP1 (10 μM, 2 h).

    Saracatinib purchased from MCE. Usage Cited in: Arch Biochem Biophys. 2018 May 1;645:54-60.  [Abstract]

    SK-BR-3, MCF-7, and MDA-MB-231 cells are treated with 1 μM Saracatinib for 48 h. After treatment, the Src protein expression is determined by western blot.

    查看 Src 亚型特异性产品:

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    Lck Fyn Blk

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Saracatinib (AZD0530) is a potent Src family inhibitor with IC50s of 2.7 to 11 nM for c-Src, Lck, c-YES, Lyn, Fyn, Fgr, and Blk. Saracatinib shows high selectivity over other tyrosine kinases[1].

    IC50 & Target

    IC50: 2.7 nM (Src), 30 nM (v-Abl), 66 nM (EGFR), 200 nM (c-Kit)[1]
    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A549 IC50
    0.14 μM
    Compound: 33, AZD-0530
    Inhibition of A549 cell migration by microdroplet migration assay
    Inhibition of A549 cell migration by microdroplet migration assay
    		[PMID: 17064066]
    SJRH30 IC50
    10.1 μM
    Compound: 2, NCGC00241099
    Antiproliferative activity against human Rh30 cells after 48 hrs by CellTiter-Glo luminescent assay
    Antiproliferative activity against human Rh30 cells after 48 hrs by CellTiter-Glo luminescent assay
    		[PMID: 23787099]
    Vero CC50
    > 50 μM
    Compound: 30
    Cytotoxicity against African green monkey Vero cells by MTT assay
    Cytotoxicity against African green monkey Vero cells by MTT assay
    		[PMID: 32539378]
    体外研究
    (In Vitro)

    Saracatinib (AZD0530), an orally available Src inhibitor, demonstrates potent antimigratory and anti-invasive effects in vitro, and inhibits metastasis in a murine model of bladder cancer. Antiproliferative activity of Saracatinib varies between cell lines (IC50 of 0.2-10 μM). Saracatinib potently inhibits the proliferation of Src3T3 mouse fibroblasts and demonstrates variable antiproliferative activity in a range of human cancer cell lines containing endogenous Src. Sub micromolar growth inhibition of five of the human cancer cell lines tested with Saracatinib (tumor types: colon, prostate, lung, and leukemia) is observed with IC50 values of 0.2-0.7 μM. In 3-day MTS cell proliferation assays, Saracatinib inhibits proliferation of the Bcr-Abl-driven human leukemia cell line K562 with an IC50 of 0.22 μM. In the microdroplet migration assay, Saracatinib reduces the migration of human lung cancer A549 cells in a concentration-dependent manner (IC50 0.14 μM)[1].

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

    Saracatinib 相关抗体:
    体内研究
    (In Vivo)

    Saracatinib (AZD0530) treatment potently inhibits the proliferation of subcutaneously transplanted Src3T3 fibroblasts in mice and rats in a dose-dependent manner. In both models, significant inhibition of tumor growth is seen at doses ≥6 mg/kg/day (60% inhibition in mice and 98% inhibition in rats versus animals treated with vehicle) and, at the maximum doses investigated, complete tumor growth inhibition is observed (100% inhibition at 25 mg/kg/day in mice and 10 mg/kg/day in rats)[1].

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

    542.03

    Formula

    C27H32ClN5O5
    CAS 号
    性状

    固体

    颜色

    White to light yellow

    中文名称

    塞卡替尼
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : 50 mg/mL (92.25 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 1.8449 mL 9.2246 mL 18.4492 mL
    5 mM 0.3690 mL 1.8449 mL 3.6898 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    • 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

    动物实验：

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
    ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
    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： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (4.61 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

      生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (4.61 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

      2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
    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

    只
    由于实验过程有损耗，建议您多配一只动物的量
    请输入您的动物体内配方组成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
    您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
    连续给药周期超过半月以上，请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.92%

    COA (288 KB) HNMR (301 KB) LCMS (99 KB) 元素分析报告 (211 KB)

    产品使用指南 (1538 KB)
    参考文献
    Kinase Assay
    [1]

    Investigation of the reversibility and the mechanism of Saracatinib inhibition is conducted using a full-length activated human Src in a continuous, coupled assay. ATP and peptide substrate (Src II peptide) concentrations are varied in turn (ATP 40-1280 μM; Src II peptide 100-800 μM), in conjunction with Saracatinib (0-30 nM), at saturating concentrations of the non-varied substrate (ATP 1.6 mM; Src II peptide 1.0 mM). The binding affinity of Saracatinib for inactivated Src (phosphorylated at tyrosine 527, not tyrosine 416) is measured using a BIAcore inhibition-in-solution assay. The assay followed competition binding between Saracatinib and an immobilized ureidoquinazoline for binding to Src. Data analysis is performed by unweighted nonlinear regression using GraFit, version 5 and an F-test is used to identify the most suitable equation[1].

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

    Cell proliferation is assessed using a colorimetric 5-bromo-2′-deoxyuridine (BrdU) Cell Proliferation ELISA kit. Briefly, cells are plated onto 96-well plates (1.5×104 cells/well), the following day 0.039-20 μM Saracatinib in DMSO (at a final concentration of 0.5%) is added and the cells are incubated for 24 h. The cells are pulse labeled with BrdU for 2 h and fixed. Cellular DNA is then denatured with the provided solution and incubated with antiBrdU peroxidase for 90 min. Following three washes with phosphate-buffered saline, tetramethylbenzidine substrate solution is added and the plates are incubated on a plate shaker for 10-30 min until the positive control absorbance at 690 nm is approximately 1.5 absorbance units[1].

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

    Mice and Rats[1]
    Female athymic mice (nu/nu) and rats (RH-rnu/rnu) are used. Animals are treated once daily by oral gavage with either vehicle alone or Saracatinib 6.25-50 mg/kg for 10-91 days. Tumor growth inhibition is calculated. For pharmacokinetic and pharmacodynamic analysis animals are humanely sacrificed and samples (plasma and tumor) are collected. Tumor samples are homogenized with 5 volumes of water and extracted with chloroform. Plasma and tumor samples are analyzed for Saracatinib concentration using high-performance liquid chromatography with tandem mass spectrometric detection after solid-phase extraction.

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

    Saracatinib 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.8449 mL 9.2246 mL 18.4492 mL 46.1229 mL
    5 mM 0.3690 mL 1.8449 mL 3.6898 mL 9.2246 mL
    10 mM 0.1845 mL 0.9225 mL 1.8449 mL 4.6123 mL
    15 mM 0.1230 mL 0.6150 mL 1.2299 mL 3.0749 mL
    20 mM 0.0922 mL 0.4612 mL 0.9225 mL 2.3061 mL
    25 mM 0.0738 mL 0.3690 mL 0.7380 mL 1.8449 mL
    30 mM 0.0615 mL 0.3075 mL 0.6150 mL 1.5374 mL
    40 mM 0.0461 mL 0.2306 mL 0.4612 mL 1.1531 mL
    50 mM 0.0369 mL 0.1845 mL 0.3690 mL 0.9225 mL
    60 mM 0.0307 mL 0.1537 mL 0.3075 mL 0.7687 mL
    80 mM 0.0231 mL 0.1153 mL 0.2306 mL 0.5765 mL
    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:

    Saracatinib379231-04-6AZD0530塞卡替尼AZD 0530AZD-0530SrcAutophagyInhibitorinhibitorinhibit

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