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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. 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.
ErbB-2 and EGFR dual tyrosine kinases are growth promoting factors that are over expressed in some breast cancer cell lines. Lapatinib inhibits the growth of both EGFR- and ErbB-2-overexpressing cells, whereas OSI-774 and Iressa which are EGFR selective inhibitors preferentially inhibit the growth of the EGFR-overexpressing cell lines. Research studies have reported that Lapatinib Ditosylate can inhibit breast cancer cell proliferation.
Cell Death Dis. 2021 Feb 15;12(2):179.
Targeting transcription of MCL-1 sensitizes HER2-amplified breast cancers to HER2 inhibitors
Lapatinib ditosylate monohydrate purchased from AbMole
Proc Natl Acad Sci U S A. 2018 Feb 23.
Coamplification of miR-4728 protects HER2-amplified breast cancers from targeted therapy
Lapatinib ditosylate monohydrate purchased from AbMole
J Pharm Pharm Sci. 2016 Feb;404-407.
Phase dependent discrepancy in murine vaginal micro-environment: A correlative analysis of PH, glycogen and Serum Estrogen upon exposure to Lapatinib Ditosylate
Lapatinib ditosylate monohydrate purchased from AbMole
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Source | Proc Natl Acad Sci U S A (2018) . Figure 6. Lapatinib Ditosylate (AbMole BioScience) |
| Method | i.v. | |
| Cell Lines | NSG mice | |
| Concentrations | 100 mg/kg | |
| Incubation Time | 5 d | |
| Results | Again, the single agents displayed modest activity, inhibiting tumor growth, whereas the combination shrank most of the tumors, similar to the BT-474 xenograft model. |
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Source | Proc Natl Acad Sci U S A (2018) . Figure 5. Lapatinib Ditosylate (AbMole BioScience) |
| Method | Western blotting | |
| Cell Lines | HCC-1419 and MDA-MB-453 cells | |
| Concentrations | 1 μM | |
| Incubation Time | 6, 12, and 24 h | |
| Results | To verify that both MCL-1:BIM and MCL-1:BAK complexes were disrupted by S63845, we immunoprecipitated MCL-1 complexes in lysates of the HER2-amplified breast cancer cells, HCC- 1419 and MDA-MB-453, following treatment with lapatinib, S63845 (at two concentrations of 300 nM and 1 μM), or their combination. |
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Source | Proc Natl Acad Sci U S A (2018) . Figure 4. Lapatinib Ditosylate (AbMole BioScience) |
| Method | Western blotting | |
| Cell Lines | MDA-MB-361 and BT-474 cells | |
| Concentrations | 1 μM | |
| Incubation Time | 24 h | |
| Results | Importantly, since HER2 inhibitors like lapatinib block ERK signaling in HER2-amplified breast cancers, it is likely that miR-4728 only has an antagonistic effect in the presence of HER2 inhibitors, while miR-4728 likely promotes tumorigenesis in the absence of HER2 inhibition. |
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Source | Int J Pharm Pharm Sci (2016). Figure 3.Lapatinib (Abmole) |
| Method | PH test | |
| Cell Lines | ||
| Concentrations | ||
| Incubation Time | 1~21 days | |
| Results | No significant changes in the vaginal pH were observed between control and treated animals throughout the three phases of the estrous cycle. Even though, on the 12th d, prolonged diestrus phase in treated group animals was evidenced with the vaginal pH as compared with the control mice [fig. 3]. |
| Cell Experiment | |
|---|---|
| Cell lines | HFF; BT474, MCF-7, N87, and CaLu-3; HN5, A-431, T47D, HB4a, and HB4a c5.2 cell lines |
| Preparation method | In Vitro Growth Inhibition Assays For assessment of cell-based potency, cells were plated in 96-well Falcon plates (Becton Dickinson) in the growth media described above. Plating densities that resulted in logarithmic growth of vehicle-treated cells for the duration of the assay were used: HFF, 15,000 cells/cm2; BT474, MCF-7, N87, and CaLu-3, 30,000 cells/cm2; and HN5, A-431, T47D, HB4a, and HB4a c5.2, 10,000 cells/cm2. After 24 h, cells were exposed to compounds at the concentrations indicated in Fig. 2. HFF, BT474, HN5, and N87 cells were treated in low-glucose DMEM containing 5% FBS, 50 μg/ml gentamicin, and 0.3% v/v DMSO. MCF-7 cells were treated in 50% high-glucose DMEM, 50% low-glucose DMEM containing 5% FBS, 50 μg/ml gentamicin, and 0.3% v/v DMSO. T47D, A-431, and CaLu-3 cells were treated in 50% RPMI, 50% low-glucose DMEM containing 5% FBS, 50 μg/ml gentamicin, and 0.3% v/v DMSO. HB4a and HB4a c5.2 cells were treated in 50% DMEM, 50% RPMI 1640 supplemented with 5% FBS, 2.5 μg/ml hydrocortisone, 2.5 μg/ml insulin, 25 μg/ml hygromycin B, 50 μg/ml gentamicin, and 0.3% v/v DMSO. After 3 days, relative cell number was estimated using methylene blue staining. The media were removed, and 100 μl of 0.5% w/v methylene blue dissolved in 50% ethanol and 50% water were added to each well. Plates were washed by immersion in deionized water and allowed to air dry. 1% w/v n-lauroylsarcosine (100 μl) dissolved in PBS was added to each well, and plates were incubated for 30 min at room temperature. The absorbance at 620 nm was read in a Spectra (Tecan) microplate reader. Data were analyzed using curve-fitting macros written for Microsoft Excel. Concentrations with IC50 were interpolated using the method of Levenberg and Marquardt and this equation: y = Vmax × [1 − (xn/(Kn + xn))], where “K” is equal to IC50. |
| Concentrations | 0~100 μM |
| Incubation time | 3 days |
| Animal Experiment | |
|---|---|
| Animal models | CD-1 nude female mice were used for HN5 human tumor xenografts, C.B-17 SCID female mice were used for BT474 human tumor xenografts |
| Formulation | sulfo-butyl-ether-β-cyclodextrin 10% aqueous solution (CD10) |
| Dosages | 30 or 100 mg/kg twice daily for 21 days |
| Administration | p.o. |
| Molecular Weight | 943.48 |
| Formula | C43H44ClFN4O11S3 |
| CAS Number | 388082-78-8 |
| Solubility (25°C) | DMSO 60 mg/mL |
| Storage | -20°C, dry, sealed |
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