(R)-CR8 (trihydrochloride)
| 中文名称 | (R)-CR8 (trihydrochloride) |
|---|---|
| 中文同义词 | (R)-CR8 3HCL;化合物 T12617;(2R)-2-[[9-(甲基乙基)-6-[[4-(2-吡啶基)苯基]甲基]氨基]-9H-嘌呤-2-基]氨基]-1-丁醇三盐酸盐;(R)-CR8 三盐酸盐,CDK抑制剂;(R)-2-((9-异丙基-6-((4-(吡啶-2-基)苄基)氨基)-9H-嘌呤-2-基)氨基)丁-1-醇三盐酸盐 |
| 英文名称 | (R)-CR8 (trihydrochloride) |
| 英文同义词 | (R)?-?CR8 (trihydrochloride);CR8, (R)-Isomer trihydrochloride;(R)?-?CR8 triHCl;(R)-Isomer trihydrochloride;(R) CR8 trihydrochloride,(R)-CR-8 trihydrochloride,(R)CR8 trihydrochloride;(R)-2-((9-Isopropyl-6-((4-(pyridin-2-yl)benzyl)amino)-9H-purin-2-yl)amino)butan-1-ol trihydrochloride |
| CAS号 | 1786438-30-9 |
| 分子式 | C24H30ClN7O |
| 分子量 | 468 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 1786438-30-9.mol |
| 结构式 |  |
(R)-CR8 (trihydrochloride) 性质
| 储存条件 | Store at -20°C |
|---|---|
| 溶解度 | 二甲基亚砜：62.5 mg/mL（115.54 mM） |
| 形态 | 固体 |
| 颜色 | 白色至米白色 |
|
CDK1/cyclinB1 0.09 μM (IC 50 ) |
cdk2/cyclin A 0.072 μM (IC 50 ) |
CDK2/cyclinE 0.041 μM (IC 50 ) |
Cdk5/p25 0.11 μM (IC 50 ) |
CDK7/cyclin H 1.1 μM (IC 50 ) |
CDK9/Cyclin T 0.18 μM (IC 50 ) |
CK1δ/ε 0.4 μM (IC 50 ) |
(R)-CR8 (CR8) trihydrochloride (0.1-100 μM; 48 hours) is a potent inducer of apoptotic cell death with an IC
50
of 0.49 μM for SH-SY5Y cell line.
(R)-CR8 trihydrochloride (0.25-10 μM) induces a dose-dependent induction of poly-(ADP-ribose)polymerase (PARP) cleavage.
The CDK-bound form of (R)-CR8 trihydrochloride has a solvent-exposed pyridyl moiety that induces the formation of a complex between CDK12-cyclin K and the CUL4 adaptor protein DDB1, bypassing the requirement for a substrate receptor and presenting cyclin K for ubiquitination and degradation
Apoptosis Analysis
| Cell Line: | SH-SY5Y cell line |
| Concentration: | 0.1, 1, 10, 100 μM |
| Incubation Time: | 24 hours |
| Result: | Reduced cell survival in a dose-dependent manner. |
(R)-CR8 trihydrochloride (5 mg/Kg; i.p.) results in a significant reduction in lesion size at 28 days in histological assessment.
| Animal Model: | Adult (10 to 12 weeks old) male Sprague-Dawley rats (310 to 330 g) |
| Dosage: | 5 mg/Kg |
| Administration: | i.p. |
| Result: | Resulted in a significant reduction in lesion size. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-18340A | (R)-CR8 (trihydrochloride) (R)-CR8 trihydrochloride | 1786438-30-9 | 10mM * 1mLin DMSO | 1071元 |
| 2024/04/30 | HY-18340A | (R)-CR8 (trihydrochloride) (R)-CR8 trihydrochloride | 1786438-30-9 | 10mg | 1450元 |