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  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)

目錄號: HY-50898B 純度: 99.93%
COA 產(chǎn)品使用指南 技術(shù)支持

Lapatinib ditosylate monohydrate (GW572016 ditosylate monohydrate) 是一種 ErbB-2 和 EGFR 酪氨酸激酶結(jié)構(gòu)域的有效抑制劑，對純化的 EGFR 和 ErbB-2 的 IC50 值分別為 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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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥279
In-stock
10 mg ￥269
In-stock
25 mg ￥431
In-stock
50 mg ￥600
In-stock
100 mg ￥780
In-stock
200 mg   詢價  
500 mg   詢價  

* Please select Quantity before adding items.

Customer Review

Other Forms of Lapatinib ditosylate monohydrate:

MCE 顧客使用本產(chǎn)品發(fā)表的 70 篇科研文獻(xiàn)

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]

    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: 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: 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.

    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    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)

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A-431 IC50
    0.14 μM
    Compound: Tykerb
    Inhibition of EGFR in human A431 cells by HTRF assay
    Inhibition of EGFR in human A431 cells by HTRF assay
    		[PMID: 19815412]
    BT-474 IC50
    0.1 μM
    Compound: 1, Tykerb
    Antiproliferative activity against human BT474 cells by methylene blue staining method
    Antiproliferative activity against human BT474 cells by methylene blue staining method
    		[PMID: 21334203]
    BT-474 IC50
    100 nM
    Compound: 3, Tykerb
    Antiproliferative activity against human BT474 cells expressing ErbB2 by MEB assay
    Antiproliferative activity against human BT474 cells expressing ErbB2 by MEB assay
    		[PMID: 19111461]
    BT-474 EC50
    20 nM
    Compound: Tykerb
    Antiproliferative activity against human BT474 cells overexpressing ERBb2 after 3 days by methylene blue staining
    Antiproliferative activity against human BT474 cells overexpressing ERBb2 after 3 days by methylene blue staining
    		[PMID: 19028424]
    BT-474 IC50
    37.4 nM
    Compound: GW572016, tykerb
    Cytotoxicity against human BT474 cells after 72 hrs by SRB assay
    Cytotoxicity against human BT474 cells after 72 hrs by SRB assay
    		[PMID: 24121234]
    HN5 IC50
    120 nM
    Compound: 3, Tykerb
    Antiproliferative activity against human HN5 cells expressing EGFR by MEB assay
    Antiproliferative activity against human HN5 cells expressing EGFR by MEB assay
    		[PMID: 19111461]
    HN5 EC50
    15 nM
    Compound: Tykerb
    Antiproliferative activity against human HN5 cells overexpressing EGFR after 3 days by methylene blue staining
    Antiproliferative activity against human HN5 cells overexpressing EGFR after 3 days by methylene blue staining
    		[PMID: 19028424]
    NCI-N87 IC50
    46.2 nM
    Compound: GW572016, tykerb
    Cytotoxicity against human NCI-N87 cells after 72 hrs by SRB assay
    Cytotoxicity against human NCI-N87 cells after 72 hrs by SRB assay
    		[PMID: 24121234]
    SK-BR-3 IC50
    0.124 μM
    Compound: Tykerb
    Inhibition of HER2 in human SKBR3 cells by HTRF assay
    Inhibition of HER2 in human SKBR3 cells by HTRF assay
    		[PMID: 19815412]
    體外研究
    (In Vitro)

    Lapatinib (GW2016；0.03-10 μM；處理 6 小時；BT474 和 HN5 細(xì)胞) 可劑量依賴性抑制 EGFR 和 ErbB-2 的受體自磷酸化，同時抑制 AKT 絲氨酸 473 的磷酸化[1]。
    Lapatinib (GW2016；處理 72 小時；HN5、A-43、BT474、N87 和 CaLu-3 細(xì)胞) 可選擇性抑制人腫瘤細(xì)胞系的增殖[1]。
    Lapatinib (GW2016；1-10 μM；處理 72 小時；HN5 細(xì)胞) 導(dǎo)致 G1 期阻滯[1]。

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

    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.
    體內(nèi)研究
    (In Vivo)

    Lapatinib (GW2016；30-100 mg/kg；口服給藥；每天兩次；持續(xù) 21 天；CD-1 雌性裸鼠) 處理以 30 和 100 mg/kg 的劑量反應(yīng)方式抑制 HN5 細(xì)胞的腫瘤異種移植生長，在較高劑量下完全抑制腫瘤生長[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 號
    性狀

    固體

    顏色

    Light yellow to yellow

    中文名稱

    二甲苯磺酸拉帕替尼一水合物
    運(yùn)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(shù)據(jù)
    細(xì)胞實(shí)驗(yàn)： 

    DMSO 中的溶解度 : 50 mg/mL (53.00 mM; 超聲助溶 (<60°C); 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 1.0599 mL 5.2995 mL 10.5991 mL
    5 mM 0.2120 mL 1.0599 mL 2.1198 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲存時，請?jiān)?個月內(nèi)使用，-20°C儲存時，請?jiān)?個月內(nèi)使用。

    • 摩爾計(jì)算器

    • 稀釋計(jì)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(yàn)：

    請根據(jù)您的 實(shí)驗(yàn)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(yàn)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(yàn)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    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (2.65 mM); 懸濁液; 超聲助溶

      此方案可獲得 2.5 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。

      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(jì)算器
    請輸入動物實(shí)驗(yàn)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(yàn)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(jì)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）。

    *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(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(yàn)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: 99.93%

    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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲存時，請?jiān)?個月內(nèi)使用，-20°C儲存時，請?jiān)?個月內(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 1.0599 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
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      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：
    Lapatinib ditosylate monohydrate
    目錄號：
    HY-50898B
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