| Chemical Properties | Back Directory | [Melting point ]
188-189 °C | [Boiling point ]
633.6±55.0 °C(predicted) | [density ]
1.42±0.1 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted) | [pka]
14.71±0.10(predicted) |
| Hazard Information | Back Directory | [Uses]
EGFR/HER2-IN-11 (compound 20) is an orally active dual inhibitor for human epidermal growth factor receptor 2 (HER2) and epidermal growth factor receptor (EGFR), with IC50s of 7.7 and 22 nM, respectively. EGFR/HER2-IN-11 exhibits antitumor efficacy and inhibits proliferation against cancer cells BT-474 with GI50 of 601 nM[1]. | [in vivo]
EGFR/HER2-IN-11 (10 mg/kg, p.o.) reveals a metabolic stability of 59 μL/min/mg and an AUC0-8 h of 2.476 μg·h/mL in BALB/c mice[1]. | [References]
[1] Ishikawa T, et al., Design and synthesis of novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2-d]pyrimidine scaffold. J Med Chem. 2011 Dec 8;54(23):8030-50. DOI:10.1021/jm2008634 |
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