(R)-CR8 (trihydrochloride)
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- CAS号:
- 1786438-30-9
- 英文名:
- (R)-CR8 (trihydrochloride)
- 英文别名:
- (R)?-?CR8 triHCl;(R)-Isomer trihydrochloride;(R)?-?CR8 (trihydrochloride);CR8, (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
- 中文名:
- (R)-CR8 (trihydrochloride)
- 中文别名:
- 化合物 T12617;(R)-CR8 3HCL;(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;(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
- CBNumber:
- CB65848911
- 分子式:
- C24H30ClN7O
- 分子量:
- 468
- MOL File:
- 1786438-30-9.mol
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(R)-CR8 (trihydrochloride)化学性质
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储存条件:
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Store at -20°C
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溶解度:
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DMSO: 62.5 mg/mL (115.54 mM)
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(R)-CR8 (trihydrochloride)性质、用途与生产工艺
(R)-CR8 (CR8) trihydrochloride 是 Roscovitine 的第二代类似物，是一种有效的 CDK1/2/5/7/9 抑制剂。(R)-CR8 trihydrochloride 抑制 CDK1/cyclin B (IC50=0.09 μM)、CDK2/cyclin A (0.072 μM)、CDK2/cyclin E (0.041 μM)、CDK5/p25 (0.11 μM)、CDK7/cyclin H (1.1 μM)、CDK9/cyclin T (0.18 μM) 和 CK1δ/ε (0.4 μM)。(R)-CR8 trihydrochloride 诱导细胞凋亡并具有神经保护作用。(R)-CR8 trihydrochloride 作为一种分子胶降解剂来消耗细胞周期蛋白 K。
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CDK1/cyclinB1
0.09 μM (IC
50
)
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cdk2/cyclin A
0.072 μM (IC
50
)
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CDK2/cyclinE
0.041 μM (IC
50
)
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Cdk5/p25
0.11 μM (IC
50
)
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CDK7/cyclin H
1.1 μM (IC
50
)
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CDK9/Cyclin T
0.18 μM (IC
50
)
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CK1δ/ε
0.4 μM (IC
50
)
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(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
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Cell Line:
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SH-SY5Y cell line
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Concentration:
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0.1, 1, 10, 100 μM
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Incubation Time:
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24 hours
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Result:
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Reduced cell survival in a dose-dependent manner.
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(R)-CR8 trihydrochloride (5 mg/Kg; i.p.) results in a significant reduction in lesion size at 28 days in histological assessment.
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Animal Model:
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Adult (10 to 12 weeks old) male Sprague-Dawley rats (310 to 330 g)
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Dosage:
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5 mg/Kg
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Administration:
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i.p.
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Result:
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Resulted in a significant reduction in lesion size.
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(R)-CR8 (trihydrochloride)
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上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 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 |
(R)-CR8 (trihydrochloride)
生产厂家
1786438-30-9, (R)-CR8 (trihydrochloride) 相关搜索:
- 酶
- (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
- (R)-CR8 三盐酸盐,CDK抑制剂
- (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
- 化合物 T12617
- (R)-CR8 3HCL
- 1786438-30-9
- (R)-2-((9-Isopropyl-6-((4-(pyridin-2-yl)benzyl)amino)-9H-purin-2-yl)amino)butan-1-ol trihydrochloride
- (R) CR8 trihydrochloride,(R)-CR-8 trihydrochloride,(R)CR8 trihydrochloride
- (R)-Isomer trihydrochloride
- (R)?-?CR8 triHCl
- CR8, (R)-Isomer trihydrochloride
- (R)?-?CR8 (trihydrochloride)