2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Autophagy Apoptosis
  3. EGFR Autophagy Ferroptosis
  4. Lapatinib ditosylate monohydrate

Lapatinib ditosylate monohydrate  (Synonyms: 二甲苯磺酸拉帕替尼一水合物; GW572016 ditosylate monohydrate; GW2016 ditosylate monohydrate)

目录号: HY-50898B 纯度: 99.78%
COA 产品使用指南

摩尔计算器

Lapatinib ditosylate monohydrate (GW572016 ditosylate monohydrate) 是一种 ErbB-2 和 EGFR 酪氨酸激酶结构域的有效抑制剂，对纯化的 EGFR 和 ErbB-2 的 IC50 值分别为 10.2 和 9.8 nM。

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Lapatinib ditosylate monohydrate Chemical Structure

Lapatinib ditosylate monohydrate Chemical Structure

CAS No. : 388082-78-8

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Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ￥660
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50 mg ￥600
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100 mg ￥780
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Customer Review

Other Forms of Lapatinib ditosylate monohydrate:

Lapatinib ditosylate monohydrate 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 63 篇科研文献

WB

    Lapatinib ditosylate monohydrate purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2018 Jun 25;37(1):123.  [Abstract]

    MCF-7 cells are treated with or without 5 μg/mL cisplatin (DDP) for 48 h after preincubated with or without Lapatinib at the indicated concentrations for 6 h, respectively. Then the levels of ER-α36, total EGFR and P-EGFR, total HER-2 and P-HER-2, total ERK and P-ERK are evaluated using western blot.

    Lapatinib ditosylate monohydrate purchased from MCE. Usage Cited in: Mol Cancer Ther. 2018 Mar;17(3):603-613.  [Abstract]

    Immunoblot analysis of U-CH1 cells treated with the indicated doses of inhibitors (Afatinib, Erlotinib and Lapatinib) for 2 h (upper panel) or 48 h (lower panel). Protein cell extracts are resolved on SDS-PAGE gel and membranes probed with the indicated antibodies. IC50s of the different inhibitors are reported.

    Lapatinib ditosylate monohydrate purchased from MCE. Usage Cited in: Cancer Chemother Pharmacol. 2018 Sep;82(3):383-394.  [Abstract]

    The expression level of EGFR and HER2 on normal esophageal epithelium cell and four esophageal squamous cancer cell lines analyzed by western blot.

    Lapatinib ditosylate monohydrate purchased from MCE. Usage Cited in: Nature. 2017 Aug 24;548(7668):471-475.  [Abstract]

    Western blot of SKBR3, BT474, MDA-MB-453, and MDA-MB-361 cells treated with DMSO, Lapatinib, or Abemaciclib for 48 h. Western blot of MDA-MB-453 cells pretreated with DMSO or Abemaciclib (500 nM) for 0, 1, or 7 days before exposure to Staurosporine (500 nM) for 4 h.

    Lapatinib ditosylate monohydrate purchased from MCE. Usage Cited in: Oncotarget. 2017 Aug 24;8(62):104894-104912.  [Abstract]

    MDA-MB-231 cells are serum-starved overnight and pre-treated with 3 μM Lapatinib or DMSO for 3 hours. After that time, cells are lysed (0hr) or stimulated with EGF for 1, 8, 24, 48, and 72 hours. Western blots of p-EGFR (Tyr1173), EGFR, p-cJun (ser63), cJun, and vinculin are shown with band densitometries beneath.

    Lapatinib ditosylate monohydrate purchased from MCE. Usage Cited in: Oncogene. 2016 Jun 9;35(23):2961-70.  [Abstract]

    The combined use of MEK162 with HER kinase inhibitor Lapatinib, almost completely abolishes MAPK signaling as evidenced by diminished phospho-Erk levels. Western blot analyses of ERK signaling in tumor transplants from mice treated as indicated. Three hours after their dose on day four of treatment, the mice are sacrificed for analysis. Vinculin is used as a loading control.

    Lapatinib ditosylate monohydrate purchased from MCE. Usage Cited in: Oncogene. 2016 Jun 9;35(23):2961-70.  [Abstract]

    Western blot analysis of p-AKT(T308), p-AKT(S473) and p-ERK in transplanted NIC+PIK3CAH1047R tumors treated as indicated. Transplants of NIC+PIK3CAH1047R primary mammary tumors are first established in immunodeficient nude mice maintained on Doxycycline. Treatment starts when tumor transplants reach 500 mm3. DOX On, on Doxycycline; DOX Off, Doxycycline withdrawal. Lapatinib, 100mg/kg/day, p.o; GDC-0941, 120mg/kg/ day, p.o. Tumo

    Lapatinib ditosylate monohydrate purchased from MCE. Usage Cited in: Tumour Biol. 2016 Nov;37(11):14831-14839.  [Abstract]

    Western blot analysis of PI3K signaling in cell lysates treated with Lapatinib (1 μM) with or without BYL719.

    查看 EGFR 亚型特异性产品:

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    EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Lapatinib ditosylate monohydrate (GW572016 ditosylate monohydrate) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively[1].

    IC50 & Target[1]

    EGFR

    10.8 nM (IC50)

    ErbB2

    9.2 nM (IC50)

    体外研究
    (In Vitro)

    Lapatinib (GW2016; 0.03-10 µM; 6 hours; BT474 and HN5 cells) treatment inhibits receptor autophosphorylation of EGFR and ErbB-2 in a dose-responsive manner. Phosphorylation of serine 473 of AKT was inhibited by GW2016 in a dose-dependent manner[1].
    Lapatinib (GW2016; 72 hours; HN5, A-43, BT474, N87, and CaLu-3 cells) treatment has a selective inhibition of the proliferation of human tumor cell lines[1].
    Lapatinib (GW2016; 1-10 µM; 72 hours; HN5 cells) treatment results in induces G1 arrest[1].

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

    Lapatinib ditosylate monohydrate 相关抗体:

    Western Blot Analysis[1]

    Cell Line: BT474 and HN5 cells
    Concentration: 0.03 µM, 0.1 µM, 0.3 µM, 1 µM, 3 µM, or 10 µM
    Incubation Time: 6 hours
    Result: Inhibited receptor autophosphorylation of EGFR and ErbB-2 in a dose-responsive manner. Phosphorylation of serine 473 of AKT was also inhibited in a dose-dependent manner.

    Cell Proliferation Assay[1]

    Cell Line: HN5, A-43, BT474, N87, and CaLu-3 cells
    Concentration:
    Incubation Time: 72 hours
    Result: Inhibited the growth of tumor cells overexpressing EGFR or ErbB-2.

    Cell Cycle Analysis[1]

    Cell Line: HN5 cells
    Concentration: 1 µM, or 10 µM
    Incubation Time: 72 hours
    Result: Resulted in induction of G1 arrest.
    体内研究
    (In Vivo)

    Lapatinib (GW2016; 30-100 mg/kg; oral administration; twice daily; for 21 days; CD-1 nude female mice) treatment inhibits tumor xenograft growth of the HN5 cells in a dose-responsive manner at 30 and 100 mg/kg, with complete inhibition of tumor growth at the higher dose[1].

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

    Animal Model: CD-1 nude female mice (4-6 weeks old) with HN5 cells[1]
    Dosage: 30 mg/kg, 100 mg/kg
    Administration: Oral administration; twice daily; for 21 days
    Result: Inhibited tumor xenograft growth of the HN5 cells in a dose-responsive manner.
    Clinical Trial
    分子量

    943.48

    Formula

    C43H44ClFN4O11S3
    CAS 号
    性状

    固体

    颜色

    Light yellow to yellow

    中文名称

    二甲苯磺酸拉帕替尼一水合物
    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: 

    DMSO 中的溶解度 : 50 mg/mL (53.00 mM; 超声助溶 (<60°C); 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 1.0599 mL 5.2995 mL 10.5991 mL
    5 mM 0.2120 mL 1.0599 mL 2.1198 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。

    • 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:

    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% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (2.65 mM); 悬浊液; 超声助溶

      此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。

      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。

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

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

    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: 99.78%

    COA (268 KB) HNMR (131 KB) LCMS (268 KB)

    产品使用指南 (1538 KB)
    参考文献

    Lapatinib ditosylate monohydrate 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 1 mM 1.0599 mL 5.2995 mL 10.5991 mL 26.4976 mL
    5 mM 0.2120 mL 1.0599 mL 2.1198 mL 5.2995 mL
    10 mM 0.1060 mL 0.5300 mL 1.0599 mL 2.6498 mL
    15 mM 0.0707 mL 0.3533 mL 0.7066 mL 1.7665 mL
    20 mM 0.0530 mL 0.2650 mL 0.5300 mL 1.3249 mL
    25 mM 0.0424 mL 0.2120 mL 0.4240 mL 1.0599 mL
    30 mM 0.0353 mL 0.1767 mL 0.3533 mL 0.8833 mL
    40 mM 0.0265 mL 0.1325 mL 0.2650 mL 0.6624 mL
    50 mM 0.0212 mL 0.1060 mL 0.2120 mL 0.5300 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:

    Lapatinib ditosylate388082-78-8GW572016 ditosylateGW2016 ditosylate二甲苯磺酸拉帕替尼一水合物EGFRAutophagyFerroptosisEpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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