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OSI-420 is an active metabolite of erlotinib which is an orally active EGFR tyrosin kinase inhibitor with IC50 of 2 and 20 nM for the inhibition of human EGFR and EGFR autophosphorylation in tumor cells. Erlotinib disappearance from plasma after a short IV infusion was biexponential with a mean terminal half-life of 5.2 h and a mean clearance of 128 ml/min per m2. OSI-420 exposure (AUC) in plasma was 30% (range 12–59%) of erlotinib, and OSI-420 clearance was more than 5-fold higher than erlotinib. Erlotinib and OSI-420 were detectable in CSF. The CSF penetration (AUCCSF:AUCplasma) of erlotinib and OSI-420 was <5% relative to total plasma concentration, but CSF compound exposure was ∼30% of plasma free compound exposure, which was calculated from published plasma protein binding values. The intravenous administration of erlotinib was well tolerated.
| Cell Experiment | |
|---|---|
| Cell lines | A549, H322, H3255, H358 H661, H1650, H1975, H1299, H596 cells |
| Preparation method | Exponentially growing cells are seeded in 96-well plastic plates and exposed to serial dilutions of erlotinib, pemetrexed, or the combination at a constant concentration ratio of 4:1 in triplicates for 72 h. Using cell count and the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay to assay cell viability . Expressing growth inhibition as the percentage of surviving cells in drug-treated versus PBS-treated control cells (which is considered as 100% viability). The IC50 value is the concentration resulting in 50% cell growth inhibition by a 72-h exposure to drug(s) compared with untreated control cells and is calculated by the CalcuSyn software |
| Concentrations | 30 nM-20 μM |
| Incubation time | 72 hour |
| Animal Experiment | |
|---|---|
| Animal models | Male 5-week-old BALB-nu/nu mice with HPAC |
| Formulation | 6% Captisol |
| Dosages | 50 mg/kg |
| Administration | Oral administration |
| Molecular Weight | 415.87 |
| Formula | C21H21N3O4.HCl |
| CAS Number | 183320-51-6 |
| Solubility (25°C) | DMSO 80 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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Erlotinib is an inhibitor of human EGFR tyrosine kinase (IC50 = 2 nM) and decreases EGFR autophosphorylation in tumor cells (IC50 = 20 nM). |
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