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

Saracatinib  (Synonyms: 塞卡替尼; AZD0530)

目錄號: HY-10234 純度: 99.92%
COA 產(chǎn)品使用指南

Saracatinib (AZD0530) 是一種有效的 Src 抑制劑，抑制 c-Src，Lck，c-YES，Lyn，Fyn，Fgr 和 Blk 的 IC50 值為 2.7-11 nM，對其他酪氨酸激酶具有選擇性。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報，我們不為任何個人用途提供產(chǎn)品和服務(wù)

Saracatinib Chemical Structure

Saracatinib Chemical Structure

CAS No. : 379231-04-6

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥572
In-stock
1 mg ￥162
In-stock
5 mg ￥325
In-stock
10 mg ￥520
In-stock
50 mg ￥1410
In-stock
100 mg ￥2640
In-stock
200 mg   詢價  
500 mg   詢價  

* Please select Quantity before adding items.

Customer Review

Other Forms of Saracatinib:

MCE 顧客使用本產(chǎn)品發(fā)表的 29 篇科研文獻(xiàn)

WB

    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 亞型特異性產(chǎn)品:

    • 生物活性

    • 實(shí)驗參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    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]
    細(xì)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]
    體外研究
    (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.
    體內(nèi)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 號
    性狀

    固體

    顏色

    White to light yellow

    中文名稱

    塞卡替尼
    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗： 

    DMSO 中的溶解度 : 50 mg/mL (92.25 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

    配制儲備液
    濃度 溶劑體積 質(zhì)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
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

    • 摩爾計算器

    • 稀釋計算器

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

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動物實(shí)驗：

    請根據(jù)您的 實(shí)驗動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
    ——為保證實(shí)驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

      此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
    • 方案 二

      請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

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

      此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

      2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
    動物溶解方案計算器
    請輸入動物實(shí)驗的基本信息：

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    只
    由于實(shí)驗過程有損耗，建議您多配一只動物的量
    請輸入您的動物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
    計算結(jié)果
    工作液所需濃度 : mg/mL
    儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
    您所需的儲備液濃度超過該產(chǎn)品的實(shí)測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
    動物實(shí)驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
    連續(xù)給藥周期超過半月以上，請謹(jǐn)慎選擇該方案。
    請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料

    純度: 99.92%

    參考文獻(xiàn)
    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.
    參考文獻(xiàn)

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)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
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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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    產(chǎn)品名稱：
    Saracatinib
    目錄號：
    HY-10234
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