Molecular Formula | C20H18N4O |
Molar Mass | 330.38 |
Solubility | DMSO: soluble10mg/mL, clear |
Appearance | Solid |
Color | white to beige |
Storage Condition | 2-8°C |
Hazard Symbols | T - Toxic |
Risk Codes | 25 - Toxic if swallowed |
Safety Description | 45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) |
UN IDs | UN 2811 6.1 / PGIII |
WGK Germany | 3 |
biological activity | PKI-166 is a highly potent, selective, orally bioactive EGFR tyrosine kinase inhibitor, the IC50 value was 0.7 nM. |
Target | IC50: 0.7 nM (EGFR tyrosine kinase) |
Cell Line: | L3.6pl cells L3.6pl cells |
Concentration: | 0.01 μM, 0.05 μM, 0.5 μM 0.03 μM |
Incubation Time: | 1 hour 6 days |
Result: | Inhibited EGFR autophosphorylation in a dose-dependent manner. Enhanced the cytotoxicity mediated by gemcitabine. Significantly decreased median tumor volume. |
Animal Model: | Male athymic nude mice with L3.6pl cells xenograft (8–12 weeks) |
Dosage: | 100 mg/kg |
Administration: | Oral administration; daily; from day 7 to day 35 after xenograft |