(2R)-2-[[9-异丙基-6-[[[4-(2-吡啶基)苯基]甲基]氨基]-9H-嘌呤-2-基]氨基]-1-丁醇
![(2R)-2-[[9-异丙基-6-[[[4-(2-吡啶基)苯基]甲基]氨基]-9H-嘌呤-2-基]氨基]-1-丁醇,294646-77-8,结构式](https://www.chemicalbook.com/CAS/GIF/294646-77-8.gif)
- CAS号:294646-77-8
- 英文名:2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-(4-(2-pyridyl)benzyl)-9-isopropylpurinetrihydrochloride
- 中文名:(2R)-2-[[9-异丙基-6-[[[4-(2-吡啶基)苯基]甲基]氨基]-9H-嘌呤-2-基]氨基]-1-丁醇
- CBNumber:CB32518863
- 分子式:C24H29N7O
- 分子量:431.53
- MOL File:294646-77-8.mol
- 熔点 :98-100℃
- 沸点 :671.4±65.0 °C(Predicted)
- 密度 :1.27±0.1 g/cm3(Predicted)
- 储存条件 :2-8°C
- 溶解度 :DMSO: ≥10mg/mL
- 酸度系数(pKa) :14.56±0.10(Predicted)
- 形态 :powder
- 颜色 :off-white
- 稳定性 :Stable for 2 years as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
(2R)-2-[[9-异丙基-6-[[[4-(2-吡啶基)苯基]甲基]氨基]-9H-嘌呤-2-基]氨基]-1-丁醇性质、用途与生产工艺
- 生物活性 (R)-CR8 (CR8) 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 (CR8) 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 (CR8) 诱导细胞凋亡并具有神经保护作用。(R)-CR8 作为一种分子胶降解剂来消耗细胞周期蛋白 K。
-
靶点
Cdk1/cyclin B
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 )
-
体外研究
(R)-CR8 (CR8) (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 (0.25-10 μM) induces a dose-dependent induction of poly-(ADP-ribose)polymerase (PARP) cleavage.
The CDK-bound form of (R)-CR8 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. -
体内研究
(R)-CR8 (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: i.p. Administration: 5 mg/Kg Result: Resulted in a significant reduction in lesion size.
- 更新日期：2024/11/08
- 产品编号：HY-18340
- 产品名称：(2R)-2-[[9-异丙基-6-[[[4-(2-吡啶基)苯基]甲基]氨基]-9H-嘌呤-2-基]氨基]-1-丁醇 (R)-CR8
- CAS编号：294646-77-8
- 包装：5mg
- 价格：2500元
- 更新日期：2024/11/08
- 产品编号：HY-18340
- 产品名称：(2R)-2-[[9-异丙基-6-[[[4-(2-吡啶基)苯基]甲基]氨基]-9H-嘌呤-2-基]氨基]-1-丁醇 (R)-CR8
- CAS编号：
- 包装：10 mM * 1 mLin DMSO
- 价格：2750元
- 公司名称：TOCRIS-US
- 联系电话：--
- 电子邮件：customerservice@tocris.co.uk
- 国家：英国
- 产品数：5726
- 优势度：77
