212391-63-4

中文名称 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)-酮盐酸盐

英文名称 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 2024/10/15 09:02:46

212391-63-4 结构式

基本信息物理化学性质常见问题列表

基本信息

中文别名

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)-酮盐酸盐

英文别名

PD 166285
PD 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

所属类别

医药中间体：乙基吡啶

物理化学性质

熔点239-242?C

储存条件Desiccate at RT

溶解度可溶于二甲基亚砜、甲醇

形态淡黄色固体

颜色黄色

稳定性吸湿性

常见问题列表

生物活性

PD0166285 dihydrochloride是 P-gp 的一个底物，是 WEE1 抑制剂，也可微弱抑制 Myt1，IC50 值分别为 24 和 72 nM。PD0166285 dihydrochloride 对 Chk1 的 IC50 值为3.433 μM。

靶点

IC50: 24 nM (WEE1), 72 nM (Myt1), 3.433 μM (Chk1).

体外研究

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.

体内研究

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.