| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg |
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| Other Sizes |
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| Targets |
EGFR 10.8 nM (IC50) ErbB2 9.2 nM (IC50)
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|---|---|
| ln Vitro |
In BT474 and HN5 cells, lapatinib (GW2016; 0.03-10 µM; 6 hours) therapy suppresses EGFR and ErbB-2 receptor autophosphorylation in a dose-dependent manner. GW2016 suppressed AKT's serine 473 phosphorylation in a dose-dependent manner [1]. The administration of lapatinib (GW2016; 72 hours; HN5, A-43, BT474, N87, and CaLu-3 cells) selectively inhibits the growth of human tumor cell lines[1]. G1 arrest is induced by lapatinib (GW2016; 1- 10 µM; 72 hours; HN5 cells) treatment[1].
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| ln Vivo |
Treatment with lapatinib (GW2016; 30-100 mg/kg; oral administration; twice daily; for 21 days; CD-1 nude female mice) significantly reduces the growth of HN5 tumor xenografts at doses of 30 and 100 mg/kg, completely inhibiting tumor growth at the higher dose[1].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: BT474 and HN5 cells 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: 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 Types: HN5, A-43, BT474, N87, and CaLu-3 cells Tested Concentrations: Incubation Duration: 72 hrs (hours) Experimental Results: Inhibited the growth of tumor cells overexpressing EGFR or ErbB-2. Cell Cycle Analysis[1] Cell Types: HN5 cells Tested Concentrations: 1 µM, or 10 µM Incubation Duration: 72 hrs (hours) Experimental Results: Resulted in induction of G1 arrest. |
| Animal Protocol |
Animal/Disease Models: CD-1 nude female mice (4-6 weeks old) with HN5 cells[1]
Doses: 30 mg/kg, 100 mg/kg Route of Administration: Oral administration; twice (two times) daily; for 21 days Experimental Results: Inhibited tumor xenograft growth of the HN5 cells in a dose-responsive 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 |
C43H44CLFN4O11S3
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|---|---|
| Molecular Weight |
943.48
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| CAS # |
388082-78-8
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| Related CAS # |
Lapatinib;231277-92-2;Lapatinib ditosylate;388082-77-7
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| SMILES |
ClC1=C(C([H])=C([H])C(=C1[H])N([H])C1C2=C(C([H])=C([H])C(=C2[H])C2=C([H])C([H])=C(C([H])([H])N([H])C([H])([H])C([H])([H])S(C([H])([H])[H])(=O)=O)O2)N=C([H])N=1)OC([H])([H])C1C([H])=C([H])C([H])=C(C=1[H])F
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| Solubility (In Vitro) |
DMSO : 50 mg/mL (53.00 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (2.65 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.0599 mL | 5.2995 mL | 10.5991 mL | |
| 5 mM | 0.2120 mL | 1.0599 mL | 2.1198 mL | |
| 10 mM | 0.1060 mL | 0.5300 mL | 1.0599 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.
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