2230253-82-2
中文名稱
PKI 166 hydrochloride
英文名稱
PKI 166 hydrochloride
CAS
2230253-82-2
分子式
C20H19ClN4O
分子量
366.85
MOL 文件
2230253-82-2.mol
2230253-82-2 結(jié)構(gòu)式
常見問題列表
生物活性
PKI-166 hydrochloride 是一種高效、選擇性的，具有口服生物活性的 EGFR 酪氨酸激酶抑制劑，IC50 值為 0.7 nM。靶點
IC50: 0.7 nM (EGFR tyrosine kinase)
體外研究
PKI-166 hydrochloride (0-0.5 μM; 1 hour; pretreatment) inhibits EGFR autophosphorylation in human pancreatic cancer cells.
PKI-166 hydrochloride (0.03 μM; 6 days) enhances the cytotoxicity mediated by gemcitabine.
Western Blot Analysis
| Cell Line: | L3.6pl cells |
| Concentration: | 0.01 μM, 0.05 μM, 0.5 μM |
| Incubation Time: | 1 hour |
| Result: | Inhibited EGFR autophosphorylation in a dose-dependent manner. |
Cell Cytotoxicity Assay
| Cell Line: | L3.6pl cells |
| Concentration: | 0.03 μM |
| Incubation Time: | 6 days |
| Result: | Enhanced the cytotoxicity mediated by gemcitabine. |
體內(nèi)研究
PKI-166 hydrochloride (100 mg/kg; p.o.; daily; for 29 days) inhibits of pancreatic cancer growth.
| Animal Model: | Male athymic nude mice with L3.6pl cells xenograft (8-12 weeks) |
| Dosage: | 100 mg/kg |
| Administration: | Oral administration; daily; for 29 days |
| Result: | Significantly decreased median tumor volume. |