PKI 166
|
|
|
- CAS号:
- 187724-61-4
- 英文名:
- PKI 166
- 英文别名:
- PKI 166;PKI 166,PKI166;PKI-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
- 中文名:
- PKI 166
- 中文别名:
- 化合物PKI-166;化合物 T16549;(R)-6-(4-羟基苯基)-4-[(1-苯乙基)氨基]-7H-吡咯并[2,3-D]嘧啶
- CBNumber:
- CB41399257
- 分子式:
- C20H18N4O
- 分子量:
- 330.38
- MOL File:
- 187724-61-4.mol
|
|
|
PKI 166化学性质
-
密度:
-
1.324±0.06 g/cm3(Predicted)
-
|
-
储存条件:
-
2-8°C
-
|
-
溶解度:
-
DMSO: soluble10mg/mL, clear
-
|
-
形态:
-
powder
-
|
-
酸度系数(pKa):
-
9.67±0.15(Predicted)
-
|
-
颜色:
-
white to beige
-
|
PKI 166性质、用途与生产工艺
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.
|
PKI 166
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-117155 | PKI-166 | | 1 mg | 700元 |
| 2024/04/30 | HY-117155 | PKI 166
PKI-166 | 187724-61-4 | 5mg | 1500元 |
187724-61-4, PKI 166 相关搜索:
- (R)-6-(4-羟基苯基)-4-[(1-苯乙基)氨基]-7H-吡咯并[2,3-D]嘧啶
- 化合物PKI-166
- 化合物 T16549
- 187724-61-4
- PKI 166,PKI166
- PKI-166 >=98% (HPLC)
- Phenol, 4-[4-[[(1R)-1-phenylethyl]amino]-7H-pyrrolo[2,3-d]pyrimidin-6-yl]-
- 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)-6-(4-Hydroxyphenyl)-4-[(1-phenylethyl)amino]-7H-pyrrolo[2,3-d]pyrimidine
- (R)-4-[4-[(1-Phenylethyl)amino]-1H-pyrrolo[2,3-d]pyrimidin-6-yl]-phenol
- PKI 166