PKI 166
| 中文名称 | PKI 166 |
|---|---|
| 中文同义词 | 化合物 T16549;化合物PKI-166;(R)-6-(4-羟基苯基)-4-[(1-苯乙基)氨基]-7H-吡咯并[2,3-D]嘧啶;(R)-4-(4-((1-苯基乙基)氨基)-7H-吡咯并[2,3-D]嘧啶-6-基)苯酚;化合物PKI-166,10 MM DMSO 溶液 |
| 英文名称 | PKI 166 |
| 英文同义词 | PKI 166;(R)-4-[4-[(1-Phenylethyl)amino]-1H-pyrrolo[2,3-d]pyrimidin-6-yl]-phenol;(R)-6-(4-Hydroxyphenyl)-4-[(1-phenylethyl)amino]-7H-pyrrolo[2,3-d]pyrimidine;4-[4-(((R)-1-Phenylethyl)amino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]phenol;4-[4-[[(1R)-1-Phenylethyl]amino]-1H-pyrrolo[2,3-d]pyrimidin-;Phenol, 4-[4-[[(1R)-1-phenylethyl]amino]-7H-pyrrolo[2,3-d]pyrimidin-6-yl]-;PKI-166 >=98% (HPLC);PKI 166,PKI166 |
| CAS号 | 187724-61-4 |
| 分子式 | C20H18N4O |
| 分子量 | 330.38 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 187724-61-4.mol |
| 结构式 |  |
PKI 166 性质
| 密度 | 1.324±0.06 g/cm3(Predicted) |
|---|---|
| 储存条件 | 2-8°C |
| 溶解度 | DMSO：可溶10mg/mL，澄清 |
| 酸度系数(pKa) | 9.67±0.15(Predicted) |
| 形态 | 粉末 |
| 颜色 | 白色至米色 |
| InChI | 1S/C20H18N4O/c1-13(14-5-3-2-4-6-14)23-19-17-11-18(24-20(17)22-12-21-19)15-7-9-16(25)10-8-15/h2-13,25H,1H3,(H2,21,22,23,24)/t13-/m1/s1 |
| InChIKey | XRYJULCDUUATMC-CYBMUJFWSA-N |
| SMILES | OC(C=C1)=CC=C1C2=CC3=C(N2)N=CN=C3N[C@H](C)C4=CC=CC=C4 |
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。
IC50: 0.7 nM (EGFR tyrosine kinase)
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. |
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. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2025/12/22 | HY-117155 | PKI-166 | 187724-61-4 | 1 mg | 700元 |
| 2025/12/22 | HY-117155 | PKI 166 PKI-166 | 187724-61-4 | 5mg | 1500元 |