187724-61-4
中文名称
PKI 166
英文名称
PKI 166
CAS
187724-61-4
分子式
C20H18N4O
分子量
330.38
MOL 文件
187724-61-4.mol
更新日期
2023/03/20 15:41:19
187724-61-4 结构式
基本信息
中文别名
化合物 T16549 英文别名
PKI 166PKI-166 >=98% (HPLC)
4-[4-[[(1R)-1-Phenylethyl]amino]-1H-pyrrolo[2,3-d]pyrimidin-
4-[4-(((R)-1-Phenylethyl)amino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]phenol
(R)-4-[4-[(1-Phenylethyl)amino]-1H-pyrrolo[2,3-d]pyrimidin-6-yl]-phenol
Phenol, 4-[4-[[(1R)-1-phenylethyl]amino]-7H-pyrrolo[2,3-d]pyrimidin-6-yl]-
(R)-6-(4-Hydroxyphenyl)-4-[(1-phenylethyl)amino]-7H-pyrrolo[2,3-d]pyrimidine
常见问题列表
生物活性
PKI-166 是一种高效、选择性的，有口服生物活性的 EGFR 酪氨酸激酶抑制剂，IC50 值为 0.7 nM。靶点
IC50: 0.7 nM (EGFR tyrosine kinase)
体外研究
Pretreatment with PKI-166 (0-0.5 μM; 1 hour) inhibits EGFR autophosphorylation in human pancreatic cancer cells.
PKI-166 (0.03μ M; 6 days) enhanced 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. |
体内研究
PKI-166 (100 mg/kg; p.o.; daily; day 7-day 35 after xenograft) 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; from day 7 to day 35 after xenograft |
| Result: | Significantly decreased median tumor volume. |