Icotinib (BPI-2009H), a highly selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR TKI), in two EGFR-mutated lung cancer cell lines compared to A549, a cell line without EGFR mutations. Icotinib blocked EGFR-mediated intracellular tyrosine phosphorylation (IC50 = 45 nM) in the human epidermoid carcinoma A431 cell line and inhibits tumor cell proliferation.
| Cell Experiment | |
|---|---|
| Cell lines | A431 cell line |
| Preparation method | MTT assay Cells (103/well) were seeded into 96-well plates in RPMI-1640 medium containing 10% FBS and grown in a 5% CO2 incubator at 37 ◦C. After 24 h, cells were treated with Icotinib at 0, 0.78, 1.56, 3.125, 6.25, 12.5 or 25 µM for 96 h. Cell proliferation was calculated by subtracting the mean absorbance value on day 0 from the mean absorbance value on day 4. |
| Concentrations | 0, 0.78, 1.56, 3.125, 6.25, 12.5 or 25 µM |
| Incubation time | 96h |
| Animal Experiment | |
|---|---|
| Animal models | mice bearing A431, A549, H460 and HCT8 tumor xenografts |
| Formulation | 0.5% CMCNa |
| Dosages | 30 mg/kg once a week |
| Administration | i.p. |
| Molecular Weight | 391.4 |
| Formula | C22H21N3O4 |
| CAS Number | 610798-31-7 |
| Solubility (25°C) | DMSO 68 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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