902279-44-1
902279-44-1 結(jié)構(gòu)式
基本信息
中文別名
3-(1-哌啶基)-5-[[2-(1-吡咯烷基)乙基]氨基]-6H-蒽并[1,9-CD]異噁唑-6-酮 英文別名
CPUY0740203-(1-Piperidyl)-5-[[2-(1-pyrrolidinyl)ethyl]amino]-6H-anthra[1,9-cd]isoxazol-6-one
6H-Anthra[1,9-cd]isoxazol-6-one, 3-(1-piperidinyl)-5-[[2-(1-pyrrolidinyl)ethyl]amino]-
物理化學(xué)性質(zhì)
沸點677.6±55.0 °C(Predicted)
密度1.305±0.06 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)9.90±0.20(Predicted)
常見問題列表
生物活性
CPUY074020 是一種高效、有口服活性的組蛋白甲基轉(zhuǎn)移酶 G9a 抑制劑，其 IC50 值為 2.18 μM。CPUY074020 具有抗增殖活性。靶點
IC50: 2.18 μM (G9a)
體外研究
CPUY074020 (2-8μM; 24 hours) induces cell death through apoptosis.
CPUY074020 (2.5-10μM ; 48 hours) dose-dependently de-regulates H3K9 trimethylation.
Apoptosis Analysis
| Cell Line: | MCF-7 cells |
| Concentration: | 2 μM, 4 μM, 8 μM |
| Incubation Time: | 24 hours |
| Result: | Induced MCF-7 cells apoptosis. |
Western Blot Analysis
| Cell Line: | MCF-7 cells |
| Concentration: | 2.5 μM, 5 μM, 10 μM |
| Incubation Time: | 48 hours |
| Result: | Dose-dependently de-regulated H3K9 trimethylation. |
體內(nèi)研究
CPUY074020 exhibits reasonable PK properties, with an oral bioavailability of 55.5% and a T
1/2
value of 4.0 hours at an oral dose of 10 mg/kg.
| Animal Model: | Mice |
| Dosage: | 10 mg/kg |
| Administration: | Oral administration |
| Result: | t 1/2 =4.0 hours |