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

Lapatinib ditosylate  (Synonyms: GW572016 ditosylate; GW2016 ditosylate)

Cat. No.: HY-50898A Purity: 99.95%
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Lapatinib ditosylate (GW572016 ditosylate) 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.

For research use only. We do not sell to patients.

Lapatinib ditosylate Chemical Structure

Lapatinib ditosylate Chemical Structure

CAS No. : 388082-77-7

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10 mM * 1 mL in DMSO
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Based on 71 publication(s) in Google Scholar

Other Forms of Lapatinib ditosylate:

Lapatinib ditosylate Related Antibodies

Top Publications Citing Use of Products

63 Publications Citing Use of MCE Lapatinib ditosylate

WB

    Lapatinib ditosylate purchased from MedChemExpress. 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 purchased from MedChemExpress. 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 purchased from MedChemExpress. 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 purchased from MedChemExpress. 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 purchased from MedChemExpress. 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 purchased from MedChemExpress. 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 purchased from MedChemExpress. 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 purchased from MedChemExpress. 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.

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    Description

    Lapatinib ditosylate (GW572016 ditosylate) 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, Cell Free Assay)

    ErbB2

    9.2 nM (IC50, Cell Free Assay)

    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].

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

    Lapatinib ditosylate Related Antibodies

    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.
    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].

    MedChemExpress (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
    Molecular Weight

    925.46

    Formula

    C43H42ClFN4O10S3
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=S(CCNCC1=CC=C(C2=CC=C3C(C(NC4=CC(Cl)=C(C=C4)OCC5=CC(F)=CC=C5)=NC=N3)=C2)O1)(C)=O.O=S(C6=CC=C(C)C=C6)(O)=O.O=S(C7=CC=C(C)C=C7)(O)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture and light

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

    Solvent & Solubility
    In Vitro: 

    DMSO : 125 mg/mL (135.07 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.0805 mL 5.4027 mL 10.8054 mL
    5 mM 0.2161 mL 1.0805 mL 2.1611 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture and light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    C2

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    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.33 mg/mL (2.52 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.33 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (23.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.33 mg/mL (2.52 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.33 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (23.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.95%

    COA (255 KB) HNMR (216 KB) LCMS (120 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture and light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.0805 mL 5.4027 mL 10.8054 mL 27.0136 mL
    5 mM 0.2161 mL 1.0805 mL 2.1611 mL 5.4027 mL
    10 mM 0.1081 mL 0.5403 mL 1.0805 mL 2.7014 mL
    15 mM 0.0720 mL 0.3602 mL 0.7204 mL 1.8009 mL
    20 mM 0.0540 mL 0.2701 mL 0.5403 mL 1.3507 mL
    25 mM 0.0432 mL 0.2161 mL 0.4322 mL 1.0805 mL
    30 mM 0.0360 mL 0.1801 mL 0.3602 mL 0.9005 mL
    40 mM 0.0270 mL 0.1351 mL 0.2701 mL 0.6753 mL
    50 mM 0.0216 mL 0.1081 mL 0.2161 mL 0.5403 mL
    60 mM 0.0180 mL 0.0900 mL 0.1801 mL 0.4502 mL
    80 mM 0.0135 mL 0.0675 mL 0.1351 mL 0.3377 mL
    100 mM 0.0108 mL 0.0540 mL 0.1081 mL 0.2701 mL
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    Lapatinib ditosylate Related Classifications

    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 ditosylate388082-77-7GW572016 ditosylateGW2016 ditosylateEGFRAutophagyFerroptosisEpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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