网站主页 >> CAS数据库列表 >> (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
|
|
- CAS号:
- 294646-77-8
- 英文名:
- 2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-(4-(2-pyridyl)benzyl)-9-isopropylpurinetrihydrochloride
- 英文别名:
- R8;(S)-CR8;(R)-CR8;CR8 3HCl (R);CR8, (R)-Isomer;(R)?-?CR8/CR8/(R)-Isomer;(R)-CR8|||(R)-Isomer|||CR8;CR8, (R)-Isomer - CAS 294646-77-8 - Calbiochem;(R)-2-((9-Isopropyl-6-((4-(pyridin-2-yl)benzyl)amino)-9H-purin-2-yl)amino)butan-1-ol;(R)-2-(1-Hydroxybut-2-ylamino)-6-[4-(2-pyridyl)phenylmethylamino]-9-iso-propylpurine
- 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
- 中文别名:
- 化合物(R)-CR8;(R)-2-((9-异丙基-6-((4-(吡啶-2-基)苄基)氨基)-9H-嘌呤-2-基)氨基)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;(R)-CR8|||(R)-ISOMER|||(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|||CR8
- CBNumber:
- CB32518863
- 分子式:
- C24H29N7O
- 分子量:
- 431.53
- MOL File:
- 294646-77-8.mol
|
|
|
(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-丁醇化学性质
-
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
(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。
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
)
|
(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.
|
(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.
|
(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
上下游产品信息
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 |
---|
2024/08/19 | HY-18340 | (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 | 294646-77-8 | 5mg | 2500元 |
2024/08/19 | HY-18340 | (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 | | 10 mM * 1 mLin DMSO | 2750元 |
(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
生产厂家
294646-77-8, (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 相关搜索:
- 多肽-药物肽
- 抑制剂
- 有机化学
- C24H29N7O3HCl
- (R)-CR8|||(R)-ISOMER|||(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|||CR8
- 化合物(R)-CR8
- (R)-2-((9-异丙基-6-((4-(吡啶-2-基)苄基)氨基)-9H-嘌呤-2-基)氨基)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
- (R)-CR8|||(R)-Isomer|||CR8
- (R)?-?CR8/CR8/(R)-Isomer
- Inhibitor,(R)??CR8,caspases,Cyclin dependent kinase,lesion,death,inhibit,cell,(R)?-?CR-8,CDK,CR8, (R)-Isomer,(R)?-?CR8,(R)? ?CR8,Hippocampus,neuroprotective,Apoptosis,PARP
- CR8 3HCl (R)
- (R)-2-((9-Isopropyl-6-((4-(pyridin-2-yl)benzyl)amino)-9H-purin-2-yl)amino)butan-1-ol
- CR8, (R)-Isomer - CAS 294646-77-8 - Calbiochem
- (R)-2-(1-Hydroxybut-2-ylamino)-6-[4-(2-pyridyl)phenylmethylamino]-9-iso-propylpurine
- (2R)-2-[[9-(1-Methylethyl)-6-[[[4-(2-pyridinyl)phenyl]methyl]amino]-9H-purin-2-yl]amino]-butanol-1
- CR8, (R)-Isomer
- R8
- (2R)-2-[[9-(1-Methylethyl)-6-[[[4-(2-pyridinyl)phenyl]methyl]amino]-9H-purin-2-yl]amino]-1-butanol
- (S)-CR8
- 1-Butanol,2-[[9-(1-Methylethyl)-6-[[[4-(2-pyridinyl)phenyl]Methyl]aMino]-9H-purin-2-yl]aMino]-,(2R)-
- 2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-(4-(2-pyridyl)benzyl)-9-isopropylpurinetrihydrochloride
- (R)-CR8