1. Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
    Autophagy
    Apoptosis
  2. EGFR
    Autophagy
    Ferroptosis
  3. 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 USD 66 In-stock
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Customer Review

Based on 35 publication(s) in Google Scholar

Other Forms of Lapatinib ditosylate:

Top Publications Citing Use of Products

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

    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 MCE. Usage Cited in: Oncogene. 2016 Jun 9;35(23):2961-70.

    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 MCE. Usage Cited in: Tumour Biol. 2016 Nov;37(11):14831-14839.

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

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

    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 MCE. Usage Cited in: Oncotarget. 2017 Aug 24;8(62):104894-104912.

    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 MCE. Usage Cited in: Mol Cancer Ther. 2018 Mar;17(3):603-613.

    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 MCE. Usage Cited in: Cancer Chemother Pharmacol. 2018 Sep;82(3):383-394.

    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 MCE. Usage Cited in: J Exp Clin Cancer Res. 2018 Jun 25;37(1):123.

    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.
    • Biological Activity

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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].

    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].

    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.

    388082-77-7

    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, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    Solvent & Solubility
    In Vitro: 

    DMSO : 125 mg/mL (135.07 mM; Need ultrasonic)

    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
    10 mM 0.1081 mL 0.5403 mL 1.0805 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 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

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.95%

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    Keywords:

    Lapatinib ditosylateGW572016 ditosylateGW2016 ditosylateEGFRAutophagyFerroptosisEpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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    Product name:
    Lapatinib ditosylate
    Cat. No.:
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