187724-61-4
中文名稱
PKI 166
英文名稱
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
2024/12/13 09:53:00
187724-61-4 結構式
基本信息
中文別名
化合物 T16549 英文別名
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
物理化學性質
密度1.324±0.06 g/cm3(Predicted)
儲存條件2-8°C
溶解度DMSO：可溶10mg/mL，澄清
酸度系數(shù)(pKa)9.67±0.15(Predicted)
形態(tài)粉末
顏色白色至米色
InChI1S/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
InChIKeyXRYJULCDUUATMC-CYBMUJFWSA-N
SMILESOC(C=C1)=CC=C1C2=CC3=C(N2)N=CN=C3N[C@H](C)C4=CC=CC=C4
PKI 166價格(試劑級)
| 報價日期 | 產品編號 | 產品名稱 | CAS號 | 包裝 | 價格 |
| 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 |
| 2025/12/22 | HY-117155 | PKI-166 | 187724-61-4 | 10 mM * 1 mLin DMSO | 1650元 |
常見問題列表
生物活性
PKI-166 是一種高效、選擇性的，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
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. |
體內研究
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. |