2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Autophagy Apoptosis
  3. EGFR Autophagy Apoptosis
  4. Gefitinib

Gefitinib  (Synonyms: 吉非替尼; ZD1839)

目录号: HY-50895 纯度: 99.94%
COA 产品使用指南

摩尔计算器

Gefitinib (ZD1839) 是一种有效，选择性和口服活性的 EGFR 酪氨酸激酶抑制剂，IC50 为 33 nM。Gefitinib 选择性抑制 EGF 刺激的肿瘤细胞生长 (IC50 为 54 nM)，并阻断 EGF 刺激的肿瘤细胞中 EGFR 自磷酸化。Gefitinib 还可诱导细胞自噬 (autophagy) 和凋亡 (apoptosis)，可用于癌症相关的研究，如肺癌和乳腺癌。

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Gefitinib Chemical Structure

Gefitinib Chemical Structure

CAS No. : 184475-35-2

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥605
In-stock
100 mg ￥550
In-stock
500 mg ￥950
In-stock
1 g ￥1400
In-stock
5 g ￥2800
In-stock
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50 g   询价  

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Customer Review

Other Forms of Gefitinib:

Gefitinib 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 133 篇科研文献

WB
Cell Viability Assay

    Gefitinib purchased from MCE. Usage Cited in: Kaohsiung J Med Sci. 2023 Apr 14.  [Abstract]

    Gefitinib (0-20 μM; 24 h) significantly inhibits the viability of A549 cells.

    Gefitinib purchased from MCE. Usage Cited in: Cancer Cell. 2018 Jun 11;33(6):1061-1077.e6.  [Abstract]

    WT mice are either treated with vehicle or Gefitinib (100 mg/kg/day) starting one day prior to DEN injection (100 mg/kg). Livers are collected at 3 and 48 hr after DEN injection and subjected to IB analyses with the indicated antibodies.

    Gefitinib purchased from MCE. Usage Cited in: Theranostics. 2018 Jul 30;8(15):4262-4278.  [Abstract]

    BV2 cells are pretreated with 0.1% DMSO (Ctrl), JuA (25 µM) or JuA (25 µM) with the indicated antagonist of RTKs (Dovitinib at 1 µM, Gefitinib at 2.5 µM, SU 11248 at 2.5 µM and LDC1267 at 1 µM) for 30 min, followed by administration of Aβ42 (5 μM) for 12 h.

    Gefitinib purchased from MCE. Usage Cited in: Cell Death Dis. 2018 Feb 15;9(3):269.  [Abstract]

    WB is used to detect the effect of EGF treatment for 4 h on the expression of YAP with the inhibitors of EGFR or its downsream members, including Gefitinib, LY294002, Wortmannin, GSK2334470, BX-795, MK-2206, GSK1120212, and U0126 in the Si RhoA transfected HepG2 and SMMC7721 cells for 48 h in HepG2 and SMMC7721 cells.

    Gefitinib purchased from MCE. Usage Cited in: Oncogene. 2018 Aug;37(31):4300-4312.  [Abstract]

    Western blot analysis of E-cadherin and vimentin in HCC827 xenograft tumors treated with Gefitinib daily for 6-8 weeks until tumors regrown (resistant) or saline for 1 week (sensitive) (left panel).

    Gefitinib purchased from MCE. Usage Cited in: Oncol Rep. 2018 Oct;40(4):2242-2250.  [Abstract]

    Effects of Gefitinib(G) and SC 58635 (Cel) on ABCB1 (MDR1), FOXM1 and Bcl 2 protein levels in PC3/DR and DU145/DR cell lines. The effects of Gefitinib, SC 58635 and their combination on ABCB1 (MDR1), FOXM1 and Bcl 2 expression in the PC3/DR and DU145/DR cell lines are determined by a western blot assay.

    Gefitinib purchased from MCE. Usage Cited in: Breast Cancer Res. 2017 Aug 4;19(1):90.  [Abstract]

    The effect of Gefitinib-FTY720 treatment on CD44 expression in TNBC cell lines. HCC1806, Hs578T, and MDA-MB-468 TNBC cell lines at ~40% confluence in 12-well plates are exposed for 24 h to Gefitinib (Gef: 0.1 to 10 μM), with or without the addition of 1.5 μM FTY720.

    Gefitinib purchased from MCE. Usage Cited in: Exp Cell Res. 2017 Dec 15;361(2):246-256.  [Abstract]

    Western blot analysis for p21, p-p21, Cyclin D1. Bcl-2, Caspase 3, Cleaved Caspase 3, Caspase 9, Cleaved Caspase 9 and Bax in HCC827-GR and PC-9-GR cells treated with control, Efatutazone alone, Gefitinib alone, or Efatutazone combined with gefitinib for 48 h.

    Gefitinib purchased from MCE. Usage Cited in: Mol Med Rep. 2017 Sep;16(3):3475-3481.  [Abstract]

    Cyclin B1 and Cdk1 protein expression levels are significantly downregulated in NCI-H1975 cells treated with the combination of DHA (5 µM) and Gefitinib (10 µM).

    Gefitinib purchased from MCE. Usage Cited in: Chem Pharm Bull (Tokyo). 2017 Aug 1;65(8):768-775.  [Abstract]

    Changes in Bcl-2 protein expression in MCF-7 cells after treatment with 2CdA, BMS-354825 or Gefitinib alone or in combination for 12 h. Expression of Bcl-2 protein is analyzed by western blotting analysis.

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    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy and cell apoptosis, which can be used for cancer related research, such as Lung cancer and breast cancer [1][2][5].

    IC50 & Target[1]

    EGFR

     

    体外研究
    (In Vitro)

    Gefitinib (0.01-0.1  μM, 72 h) results in increased phosphotyrosine load of the receptor, increased signalling to ERK and stimulation of proliferation and anchorage-independent growth[2].
    Gefitinib (1-2 μM, 72 h) significantly decreases EGFRvIII phosphotyrosine load, EGFRvIII-mediated proliferation and anchorage-independent growth[2].
    Gefitinib (0.62 μM, 24-72 h) inhibits IL-13-induced M2-like polarization of RAW 264.7 cells through the STAT6-dependent signaling pathway[3].
    Gefitinib (0.62 μM, 72 h) inhibits M2-like macrophage-promoted invasion and migration[3].
    Gefitinib (0-10 μM, 72 h) induces apoptosis (induction of BIM protein) in NSCLC Cell Lines (H3255 and HCC827 cells)[4].
    Gefitinib (100 nM, 24 h) suppresses macropinocytosis and increases the cellular uptake of extracellular vesicles( EVs) in HCC827 and A549 cells[6].
    Gefitinib (1.5-60 μM, 48 h) increases inhibition of proliferation in H358R and A549R cells (Cisplatin-resistant wtEGFR NSCLC cell lines)[7].

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

    Gefitinib 相关抗体:

    Western Blot Analysis[2]

    Cell Line: NR6wtEGFR, NR6W and NR6M
    Concentration: 1, 10, 100 μM
    Incubation Time: 5 h
    Result: Inhibited EGFR tyrosine phosphorylations.

    Cell Migration Assay [3]

    Cell Line: LLCs cell
    Concentration: 0.62 μM
    Incubation Time: 72 h
    Result: Abrogated M2-like macrophage promoted invasion and migration of LLCs.
    体内研究
    (In Vivo)

    Gefitinib (Oral administration, 75 mg/kg/d, 21 days) inhibits the M2-like polarization of macrophages in LLC mice metastasis model[3].
    Gefitinib (Oral administration, 75 mg/kg for the initial week, daily for 5 consecutive days per week) eliminates phosphorylation of HER2 and HER3 and signaling through MAPK and Akt in lobular hyperplasias and carcinomas, increases MAPK activity and cytokine production in splenocytes and lymph nodes[5]. Gefitinib (Oral gavage, 150 mg/kg, daily) enhances the anti-tumor effect of Cisplatin in H358R xenograft[7].

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

    Animal Model: LLC mice metastasis model[3]
    Dosage: 75 mg/kg/d, for 21 days.
    Administration: Oral administration
    Result: Reduced the number of lung metastasis nodules, down-regulated the expression of M2 marker genes and the percentages CD206+ and CD68+ macrophages in tumor tissues.
    Animal Model: BALB-NeuT transgenic mouse model[5]
    Dosage: 75 mg/kg for the initial week, and increased by 15 mg/kg every other week, daily for 5 consecutive days per week, followed by 2 days without treatment and repeated for 8–9 weeks.
    Administration: Oral administration
    Result: Reduced tumor multiplicity from 9.6 to 0.58 (83%), and reduced the number and size of lobules and lobular nodules in treated mice.
    Clinical Trial
    分子量

    446.90

    Formula

    C22H24ClFN4O3
    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    吉非替尼；吉菲替尼
    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 : 100 mg/mL (223.76 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 2.2376 mL 11.1882 mL 22.3764 mL
    5 mM 0.4475 mL 2.2376 mL 4.4753 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    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (5.59 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，此方案实验周期在半个月以上的动物实验酌情使用。

      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玉米油中，混合均匀。

    • 方案 二

      请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (4.65 mM); 澄清溶液

      此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 20.8 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。

    以下溶解方案，请直接配制工作液。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： Corn Oil

      Solubility: 5 mg/mL (11.19 mM); 悬浊液; 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

    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: 99.94%

    COA (288 KB) LCMS (102 KB) 元素分析报告 (211 KB)

    产品使用指南 (1538 KB)
    参考文献

    Gefitinib 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 2.2376 mL 11.1882 mL 22.3764 mL 55.9409 mL
    5 mM 0.4475 mL 2.2376 mL 4.4753 mL 11.1882 mL
    10 mM 0.2238 mL 1.1188 mL 2.2376 mL 5.5941 mL
    15 mM 0.1492 mL 0.7459 mL 1.4918 mL 3.7294 mL
    20 mM 0.1119 mL 0.5594 mL 1.1188 mL 2.7970 mL
    25 mM 0.0895 mL 0.4475 mL 0.8951 mL 2.2376 mL
    30 mM 0.0746 mL 0.3729 mL 0.7459 mL 1.8647 mL
    40 mM 0.0559 mL 0.2797 mL 0.5594 mL 1.3985 mL
    50 mM 0.0448 mL 0.2238 mL 0.4475 mL 1.1188 mL
    60 mM 0.0373 mL 0.1865 mL 0.3729 mL 0.9323 mL
    80 mM 0.0280 mL 0.1399 mL 0.2797 mL 0.6993 mL
    100 mM 0.0224 mL 0.1119 mL 0.2238 mL 0.5594 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:

    Gefitinib184475-35-2ZD1839吉非替尼吉菲替尼ZD 1839ZD-1839EGFRAutophagyApoptosisEpidermal growth factor receptorErbB-1HER1EGFR tyrosine kinaseantitumourphosphorylationTAMstumor metastasislung cancerNSCLCsbreast cancerInhibitorinhibitorinhibit

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