212391-63-4
中文名稱
6-(2,6-二氯苯基)-2-[[4-[2-(二乙基氨基)乙氧基]苯基]氨基]-8-甲基吡啶并[2,3-D]嘧啶-7(8H)-酮鹽酸鹽
英文名稱
PD 166285
CAS
212391-63-4
分子式
C26H29Cl4N5O2
分子量
585.37
MOL 文件
212391-63-4.mol
更新日期
2024/12/17 14:15:45
212391-63-4 結構式
基本信息
中文別名
6-(2,6-二氯苯基)-2-[[4-[2-(二乙基氨基)乙氧基]苯基]氨基]-8-甲基吡啶并[2,3-D]嘧啶-7(8H)-酮鹽酸鹽 英文別名
PD 166285PD 166285 dihydrochloride
PD0166285 dihydrochloride
PD 166285 ISO 9001：2015 REACH
PD 166285 - CAS 212391-63-4 - Calbiochem
6-(2,6-Dichlorophenyl)-2-[[4-[2-(diethylamino)ethoxy]phenyl]amino]-8-methylpyrido[2,3-d]pyrimi
6-(2,6-Dichlorophenyl)-2-[[4-[2-(diethylaMino)ethoxy]phenyl]aMino]-8-Methylpyrido[2,3-d]pyriMidin-7(8H)-one
6-(2,6-dichlorophenyl)-2-[4-[2-(diethylamino)ethoxy]anilino]-8-methylpyrido[2,3-d]pyrimidin-7-one,dihydrochloride
6-(2,6-Dichloro-phenyl)-2-[4-(2-diethylaMino-ethoxy)-phenylaMino]-8-Methyl-8H-pyrido[2,3-d]pyriMidin-7-one hydrochloride
6-(2,6-Dichlorophenyl)-2-[[4-[2-(diethylamino)ethoxy]phenyl]amino]-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one Hydrochloride
所屬類別
醫(yī)藥中間體：乙基吡啶常見問題列表
生物活性
PD0166285 dihydrochloride是 P-gp 的一個底物，是 WEE1 抑制劑，也可微弱抑制 Myt1，IC50 值分別為 24 和 72 nM。PD0166285 dihydrochloride 對 Chk1 的 IC50 值為3.433 μM。靶點
IC50: 24 nM (WEE1), 72 nM (Myt1), 3.433 μM (Chk1).
體外研究
PD0166285 (0.5 μM) dramatically inhibits irradiation-induced Cdc2 phosphorylation at the Tyr-15 and Thr-14 in seven of seven cancer cell lines.
PD0166285 sensitizes radiation-induced cell killing in p53 mutant HT29 cells and in the E6-transfected, p53-null ovarian cancer cell line PA-1 but to a lesser extent in p53 wild-type PA-1 cells. PD0166285 abrogates irradiation-induced G2 arrest and significantly increases mitotic cell populations.
PD0166285 acts as a radiosensitizer to sensitize cells to radiation-induced cell death with a sensitivity enhancement ratio of 1.23.
Western Blot Analysis
| Cell Line: | Human and mouse cancer cell lines (HCT116, HT29, DLD-1, HCT8, H460, HeLa, C 26). |
| Concentration: | 0.5 μM. |
| Incubation Time: | 4 h. |
| Result: | Inhibited Cdc2Y15 and CdcT14 phosphorylation. |
體內研究
| Animal Model: | Wild-type, Abcg2 -/- , Abcb1a/b -/- and Abcb1a/b;Abcg2 -/- FVB mice. |
| Dosage: | 5 mg/kg. |
| Administration: | IV. |
| Result: |
C
max
is about 400 ng/mL.
P-gp, but not BCRP, limited the brain penetration of PD0166285. |