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  2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. Icotinib Hydrochloride

Icotinib Hydrochloride  (Synonyms: 鹽酸埃克替尼; BPI-2009H)

目錄號: HY-15164 純度: 99.81%
COA 產品使用指南

Icotinib Hydrochloride (BPI-2009)是有效，選擇性的 EGFR 抑制劑，IC50 值為5 nM；也抑制突變型EGFRL858R，EGFRL858R/T790M，EGFRT790M 和 EGFRL861Q。Icotinib (Hydrochloride) 是一種點擊化學試劑。它含有 Alkyne 基團，可以和含有 Azide 基團的分子發(fā)生銅催化的疊氮-炔環(huán)加成反應 (CuAAc)。

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Icotinib Hydrochloride Chemical Structure

Icotinib Hydrochloride Chemical Structure

CAS No. : 1204313-51-8

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規(guī)格 價格 是否有貨 數量
10 mM * 1 mL in DMSO ￥2188
In-stock
5 mg ￥1600
In-stock
10 mg ￥2400
In-stock
50 mg ￥6000
In-stock
100 mg   詢價  
200 mg   詢價  

* Please select Quantity before adding items.

Customer Review

Other Forms of Icotinib Hydrochloride:

    Icotinib Hydrochloride purchased from MCE. Usage Cited in: Eur J Pharmacol. 2019 May 5;850:141-149.  [Abstract]

    Immunoblotting for LC3 and p62 using lysates from cells treated with 1 μM icotinib in the presence or absence of CQ for 24 h.

    Icotinib Hydrochloride purchased from MCE. Usage Cited in: Eur J Pharmacol. 2019 May 5;850:141-149.  [Abstract]

    LC3 II levels are evaluated by immunoblotting using lysates from cells treated with 1 μM icotinib (parental cells) or 20 μM icotinib (resistant cells) for 24 h.

    • 生物活性

    • 實驗參考方法

    • 純度 & 產品資料

    • 參考文獻

    生物活性

    Icotinib Hydrochloride (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFRL858R, EGFRL858R/T790M, EGFRT790M and EGFRL861Q. Icotinib (Hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

    IC50 & Target[1]

    EGFR

    5 nM (IC50)

    EGFRL861Q

     

    EGFRL858R/T790M

     

    EGFRL858R

     

    EGFRT790M

     

    體外研究
    (In Vitro)

    Incubation with Iconitib at 0.5 μM results in kinase activity inhibition of 91%, 99%, 96%, 61% and 61%, respectively. Iconitib inhibits the proliferation of A431 and BGC-823 A549, H460 and KB cell lines with IC50s of 1, 4.06, 12.16, 16.08, 40.71 μM. When profiled with 88 kinases, Icotinib only shows meaningful inhibitory activity to EGFR and its mutants. Icotinib blocks EGFR-mediated intracellular tyrosine phosphorylation (IC50=45 nM) in the human epidermoid carcinoma A431 cell line and inhibits tumor cell proliferation[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    體內研究
    (In Vivo)

    Icotinib exhibits potent dose-dependent antitumor effects in nude mice carrying a variety of human tumor-derived xenografts. The drug is well tolerated at doses up to 120 mg/kg/day in mice without mortality or significant body weight loss during the treatment. Icotinib inhibits tumor growth at a rate of 25.2%, 45.6% and 51.5% in the A431 cell line groups; 3.4%, 25.9% and 31.0% in the A549 cell line groups; 49.4%, 52.6% and 67.4% in the H460 cell line groups, and 30.3%, 36.4% and 46.5% in the HCT8 cell line groups, at 30, 60 and 120 mg/kg/dose, respectively[1].

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

    427.88

    Formula

    C22H22ClN3O4
    CAS 號
    性狀

    固體

    顏色

    White to off-white

    中文名稱

    鹽酸埃克替尼
    運輸條件

    Room temperature in continental US; may vary elsewhere.
    儲存方式

    4°C, sealed storage, away from moisture

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

    溶解性數據
    細胞實驗： 

    DMSO 中的溶解度 : 25 mg/mL (58.43 mM; 超聲助溶; 吸濕的 DMSO 對產品的溶解度有顯著影響，請使用新開封的 DMSO)

    H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

    配制儲備液
    濃度 溶劑體積 質量 1 mg 5 mg 10 mg
    1 mM 2.3371 mL 11.6855 mL 23.3710 mL
    5 mM 0.4674 mL 2.3371 mL 4.6742 mL
    查看完整儲備液配制表

    * 請根據產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，避免反復凍融造成的產品失效。
    儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲存時，請在6個月內使用，-20°C儲存時，請在1個月內使用。

    • 摩爾計算器

    • 稀釋計算器

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

    質量
    =
    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

    動物實驗：

    請根據您的 實驗動物和給藥方式 選擇適當的溶解方案。

    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：
    ——為保證實驗結果的可靠性，澄清的儲備液可以根據儲存條件，適當保存；體內實驗的工作液，建議您現用現配，當天使用；
    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沉淀、析出現象，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 (5.84 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 (5.84 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。

      20% SBE-β-CD in Saline 的配制（4°C，儲存一周）：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

    動物數量

    只
    由于實驗過程有損耗，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 網站選購。 ，Tween 80，均可在 MCE 網站選購。
    計算結果
    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）。

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

    您所需的儲備液濃度超過該產品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術支持聯系。
    動物實驗體內工作液的配制方法 : 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 & 產品資料

    純度: 99.81%

    參考文獻
    Kinase Assay
    [1]

    In the in vitro kinase assays, 2.4 ng/μL EGFR protein is mixed with 32 ng/μL Crk in 25 μL kinase reaction buffer containing 1 μM cold ATP and 1 μCi32P-γ-ATP. The mix is incubated with Icotinib at 0, 0.5, 2.5, 12.5 or 62.5 nM on ice for 10 min followed by incubation at 30°C for 20 min. After quenching with SDS sample buffer at 100°C for 4 min, the protein mix is resolved by electrophoresis in a 10% SDS-PAGE gel. The dried gel is then exposed to detect radioactivity. Quantification is performed by software[1].

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

    Cells (1000/well) are seeded into 96-well plates in RPMI-1640 medium containing 10% FBS and grown in a 5% CO2 incubator at 37°C. After 24 h, cells are treated with Icotinib at 0, 0.78, 1.56, 3.125, 6.25, 12.5 or 25 μM for 96 h. Cell proliferation is calculated by subtracting the mean absorbance value on day 0 from the mean absorbance value on day 4[1].

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

    Mice: The effect of three doses of Icotinib (30, 60, and 120 mg/kg/dose p.o. qd) on antitumor activity and survival is determined in mice bearing A431, A549, H460 and HCT8 tumor xenografts. Taxol (30 mg/kg/dose i.p. once a week) is employed in these experiments as a positive control group[1].

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

    完整儲備液配制表

    * 請根據產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，避免反復凍融造成的產品失效。
    儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲存時，請在6個月內使用，-20°C儲存時，請在1個月內使用。

    可選溶劑 濃度 溶劑體積 質量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.3371 mL 11.6855 mL 23.3710 mL 58.4276 mL
    5 mM 0.4674 mL 2.3371 mL 4.6742 mL 11.6855 mL
    10 mM 0.2337 mL 1.1686 mL 2.3371 mL 5.8428 mL
    15 mM 0.1558 mL 0.7790 mL 1.5581 mL 3.8952 mL
    20 mM 0.1169 mL 0.5843 mL 1.1686 mL 2.9214 mL
    25 mM 0.0935 mL 0.4674 mL 0.9348 mL 2.3371 mL
    30 mM 0.0779 mL 0.3895 mL 0.7790 mL 1.9476 mL
    40 mM 0.0584 mL 0.2921 mL 0.5843 mL 1.4607 mL
    50 mM 0.0467 mL 0.2337 mL 0.4674 mL 1.1686 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.

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    產品名稱：
    Icotinib Hydrochloride
    目錄號：
    HY-15164
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