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
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 |
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中文同义词 | 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;PD 166285 双盐酸盐 |
英文名称 | PD 166285 |
英文同义词 | 6-(2,6-Dichlorophenyl)-2-[[4-[2-(diethylamino)ethoxy]phenyl]amino]-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one Hydrochloride;PD 166285;6-(2,6-Dichlorophenyl)-2-[[4-[2-(diethylamino)ethoxy]phenyl]amino]-8-methylpyrido[2,3-d]pyrimidin-7(8H)-onedihydrochloride;PD 166285 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]pyrimi;6-(2,6-Dichlorophenyl)-2-[[4-[2-(diethylaMino)ethoxy]phenyl]aMino]-8-Methylpyrido[2,3-d]pyriMidin-7(8H)-one;PD 166285 - CAS 212391-63-4 - Calbiochem |
CAS号 | 212391-63-4 |
分子式 | C26H29Cl4N5O2 |
分子量 | 585.37 |
EINECS号 | |
相关类别 | Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Protein Kinase Inhibitors and Activators |
Mol文件 | 212391-63-4.mol |
结构式 |
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 性质
熔点 | 239-242?C |
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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 | 粘黄色 |
稳定性 | 吸湿性 |
IC50: 24 nM (WEE1), 72 nM (Myt1), 3.433 μM (Chk1).
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. |
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. |