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100mg | ||
250mg | ||
500mg |
ln Vitro |
In BT474 and HN5 cells, lapatinib (GW2016; 0.03-10 µM; 6 hours) tosylate treatment suppresses the dose-dependent autophosphorylation of the EGFR and ErbB-2 receptors. AKT serine 473 phosphorylation is inhibited by GW2016 in a dose-dependent manner [1]. Human tumor cell line growth is specifically inhibited by lapatinib (GW2016; 72 hours; HN5, A-43, BT474, N87, and CaLu-3 cells) tosylate therapy [1]. G1 arrest is brought on by lapatinib (GW2016; 1–10 µM; 72 hours; HN5 cells) therapy [1].
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ln Vivo |
Lapatinib (GW2016; 30-100 mg/kg; oral; twice daily; for 21 days; CD-1 nude female mice) tosylate therapy in a dose-response manner at 30 and 100 mg/kg The growth of tumor xenografts of HN5 cells was decreased by kg, and tumor growth was totally stopped at higher doses [1].
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Cell Assay |
Cell proliferation assay[1]
Cell Types: HN5, A-43, BT474, N87 and CaLu-3 Cell Tested Concentrations: 1 nM-100 µM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibition of growth of tumor cells overexpressing EGFR or ErbB-2 . Cell cycle analysis[1] Cell Types: HN5 Cell Tested Concentrations: 1 µM or 10 µM Incubation Duration: 72 hrs (hours) Experimental Results: Induction of G1 arrest. Western Blot Analysis[1] Cell Types: BT474 and HN5 Cell Tested Concentrations: 0.03 µM, 0.1 µM, 0.3 µM, 1 µM, 3 µM or 10 µM Incubation Duration: 6 hrs (hours) Experimental Results: Inhibition of receptor autophosphorylation of EGFR and ErbB-2 dose-response approach. Phosphorylation of AKT serine 473 was also inhibited in a dose-dependent manner. |
Animal Protocol |
Animal/Disease Models: CD-1 female nude mice (4-6 weeks old) HN5 cells [1]
Doses: 30 mg/kg, 100 mg/kg Route of Administration: oral; twice (two times) daily; for 21 days Experimental Results: Inhibition of tumor xenograft growth of HN5 cells in a dose-response manner. |
References |
[1]. Rusnak DW, 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
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Molecular Formula |
C36H34CLFN4O7S2
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Molecular Weight |
753.259169101715
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CAS # |
1187538-35-7
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Related CAS # |
Lapatinib;231277-92-2;Lapatinib ditosylate;388082-77-7
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SMILES |
S(C1C=CC(C)=CC=1)(O)(=O)=O.N(C1C=CC(OCC2C=CC=C(F)C=2)=C(Cl)C=1)C1=NC=NC2=CC=C(C3=CC=C(CNCCS(=O)(=O)C)O3)C=C12
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.3276 mL | 6.6378 mL | 13.2756 mL | |
5 mM | 0.2655 mL | 1.3276 mL | 2.6551 mL | |
10 mM | 0.1328 mL | 0.6638 mL | 1.3276 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.