BMS-599626 (AC480) is an orally bioavailable inhibitor of the HER1, HER2 and HER4 tyrosine kinases (IC50=22, 32 and 190 nM, respectively), thereby inhibiting the proliferation of tumor cells that overexpress these receptors.
| Cell Experiment | |
|---|---|
| Cell lines | Sal2 mouse salivary gland tumor cells, .KPL-4 cells and PC9 cells |
| Preparation method | Cell assay. All cell lines were maintained in RPMI 1640 supplemented with 10% fetal bovine serum, 100 units/mL penicillin, and 100 Ag/mL streptomycin. Cells were plated at 1,000 per well in 96-well plates and were cultured for 24 hours before test compounds were added.Compounds were diluted in culture medium such that the final concentration of DMSO never exceeded 1%.Following the addition of compounds, the cells were cultured for an additional 72 hours before cell viability was determined by measuring the conversion of 3-(4,5-dimethylthiazol- 2-yl)-2,5-diphenyltetrazolium bromide dye with the CellTiter96 kit (Promega, Madison, WI). |
| Concentrations | 0~10µM |
| Incubation time | 72 h |
| Animal Experiment | |
|---|---|
| Animal models | SAL2 murine salivary gland tumor, mice bearing KPL-4 human breast tumors and GEO human colon tumor models |
| Formulation | dissolved in a mixture of propylene glycol/water (50:50) |
| Dosages | SAL2: 60, 120, 240 mg/kg daily for 14 days(d10-24); GEO human colon tumors：120,180mg/ kg daily for 14 days(d10-24);mice bearing KPL-4 human breast tumors: once daily for 21days) at 60 mg/kg and 180 mg/kg |
| Administration | oral |
| Molecular Weight | 567.01 |
| Formula | C27H27FN8O3.HCl |
| CAS Number | 8173837-23-1 |
| Solubility (25°C) | DMSO |
| 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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