Lapatinib (Synonyms: GW572016; GW2016) |
Catalog No.GC13608
One-Click Copy Product Info
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Lapatinib is an orally administered dual EGFR and HER2 tyrosine kinase inhibitor that has shown significant efficacy in the treatment of HER2-positive breast cancer. The IC₅₀ values of Lapatinib against purified EGFR and HER2 are 10.2nM and 9.8nM, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 231277-92-2
Sample solution is provided at 25 µL, 10mM.
Lapatinib is an orally administered dual EGFR and HER2 tyrosine kinase inhibitor that has shown significant efficacy in the treatment of HER2-positive breast cancer[1]. The IC₅₀ values of Lapatinib against purified EGFR and HER2 are 10.2nM and 9.8nM, respectively[2].
In vitro, Lapatinib (50000, 10000, 2000, 400, 80, 0nM; 96h) and poziotinib combined with paclitaxel synergizes to inhibit the proliferation of ABCB1-overexpressing ovarian cancer cells in vitro[2]. Lapatinib (5μM; 24h) attenuated TOCP-induced ErbB2 expression in RSC96 cells[3]. Lapatinib (25, 50, 100, and 200μM; 24h) inhibits the proliferation of synovial fibroblasts in patients with arthritis[4]. Lapatinib (0-10μM; 24 and 48h) decreases the ACTH production and proliferation of corticotroph tumor cells[5].
In vivo, Lapatinib (25mg/kg; 4 days; p.o.) alleviates Tri-o-cresyl phosphate (TOCP)-induced axonal damage in the spinal cord of mouse[3]. Lapatinib (30mg/kg; 15 days; p.o.) reduces synovial hyperplasia and pannus formation in rats with arthritis and prevents the development of cartilage and bone destruction[6].
References:
[1] Raja Sharin RNFS, Khan J, Ibahim MJ, et al. Role of ErbB1 in the Underlying Mechanism of Lapatinib-Induced Diarrhoea: A Review. Biomed Res Int. 2022 Jun 28;2022:4165808.
[2] Rusnak DW, Lackey K, Affleck K, et al. The effects of the novel, reversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, GW2016, on the growth of human normal and tumor-derived cell lines in vitro and in vivo. Mol Cancer Ther. 2001 Dec;1(2):85-94.
[3] McCorkle JR, Gorski JW, Liu J, et al. Lapatinib and poziotinib overcome ABCB1-mediated paclitaxel resistance in ovarian cancer. PLoS One. 2021 Aug 4;16(8):e0254205.
[4] Xu HY, Sun YJ, Sun YY, et al. Lapatinib alleviates TOCP-induced axonal damage in the spinal cord of mouse. Neuropharmacology. 2021 May 15;189:108535.
[5] Kehribar DY, Emmungil H, Türkmen NB, et al. EGFR blocker lapatinib inhibits the synthesis of matrix metalloproteinases from synovial fibroblasts. Turk J Med Sci. 2022 Aug;52(4):1355-1361.
[6] Asari Y, Kageyama K, Sugiyama A, et al. Lapatinib decreases the ACTH production and proliferation of corticotroph tumor cells. Endocr J. 2019 Jun 28;66(6):515-522.
[7] Ozgen M, Koca SS, Karatas A, et al. Lapatinib ameliorates experimental arthritis in rats. Inflammation. 2015 Feb;38(1):252-9.
| Cell experiment [1]: | |
Cell lines | ovarian cancer cell lines TOV-21G and OVCAR-3 |
Preparation Method | Cells were seeded in white-walled 96-well microplates at a density of 3×10³ cells per well in 100μL growth media and incubated for 24h at 37°C, 5% CO₂ to allow cells to attach. Subsequently, the growth media was removed and replaced with fresh media containing serially diluted drugs of interest or blank media (for untreated controls), and incubated for 96h. We tested each drug alone and in combination with five serially diluted concentrations, and cell viability was measured using CellTiter-Glo 2.0. For each pair of drugs, every concentration was tested in combination in at least 3 independent experiments using a 6×6 matrix design. The percentage viability for each combination was calculated by dividing the drug-treated signals by the untreated signals and multiplying by 100. Paclitaxel (1000, 167, 28, 4.6, 0.77, 0nM) was tested in combination with Lapatinib (50000, 10000, 2000, 400, 80, 0nM) and poziotinib (12500, 4167, 1389, 463, 154, 0nM). Synergy for each drug combination was assessed using the synergyfinder package in R, with the percentage of viable cells relative to untreated control cells as the basis for evaluation. |
Reaction Conditions | 50000, 10000, 2000, 400, 80, 0nM; 96h |
Applications | Lapatinib and poziotinib combined with paclitaxel synergizes to inhibit the proliferation of ABCB1-overexpressing ovarian cancer cells in vitro. |
| Animal experiment [2]: | |
Animal models | male Balb/c mice, 8 weeks old and 20-25g |
Preparation Method | Seventy-six mice were divided into three groups: Tri-o-cresyl phosphate (TOCP) treatment (n=33); TOCP plus Lapatinib (LPT) treatment (n=33); vehicle treatment (n=10). Mice from TOCP-treated group were given a single dose of TOCP at 900mg/kg by gavage, while mice from TOCP plus Lapatinib-treated group were treated twice with Lapatinib dissolved in 10% sulfobutyl-β-cyclodextrin at a dose of 25mg/kg (p.o.), 4h before and 4 days after TOCP treatment. Mice from control group were given corresponding vehicles. Mice were examined daily for the signs of TOCP intoxication for 21 days. |
Dosage form | 25mg/kg; 4 days; p.o. |
Applications | Lapatinib alleviates Tri-o-cresyl phosphate (TOCP)-induced axonal damage in the spinal cord of mouse. |
References: | |
| Cas No. | 231277-92-2 | SDF | |
| Synonyms | GW572016; GW2016 | ||
| Chemical Name | N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[(2-methylsulfonylethylamino)methyl]furan-2-yl]quinazolin-4-amine | ||
| Canonical SMILES | CS(=O)(=O)CCNCC1=CC=C(O1)C2=CC3=C(C=C2)N=CN=C3NC4=CC(=C(C=C4)OCC5=CC(=CC=C5)F)Cl | ||
| Formula | C29H26ClFN4O4S | M.Wt | 581.06 |
| Solubility | ≥ 29.05mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.721 mL | 8.605 mL | 17.2099 mL |
| 5 mM | 344.2 μL | 1.721 mL | 3.442 mL |
| 10 mM | 172.1 μL | 860.5 μL | 1.721 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)