中文名称: | (R)-CR8 trihydrochloride | ||||
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英文名称: | (R)-CR8 trihydrochloride | ||||
别名: | (2R)-2-[[[9-丙-2-基-6-[(4-吡啶-2-基苯基)甲基氨基]嘌呤-2-基]氨基]丁烷-1-醇;三盐酸盐 CR8, (R)-Isomer trihydrochloride | ||||
CAS No: | 1786438-30-9 | 分子式: | C24H32Cl3N7O | 分子量: | 540.92 |
CAS No: | 1786438-30-9 | ||||
分子式: | C24H32Cl3N7O | ||||
分子量: | 540.92 |
基本信息
产品编号:C10817 |
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产品名称:(R)-CR8 trihydrochloride |
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CAS: |
1786438-30-9 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
六个月 |
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分子量 |
540.92 |
-20℃ |
一个月 |
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化学名: |
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Solubility (25°C) |
体外 |
DMSO |
50mg/mL (92.44mM; Need ultrasonic) |
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Ethanol |
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Water |
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体内 |
现配现用 |
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<1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
1.8487mL |
9.2435mL |
18.4870mL |
5mM |
0.3697mL |
1.8487mL |
3.6974mL |
10mM |
0.1849mL |
0.9244mL |
1.8487mL |
生物活性
产品描述 |
Roscovitine 的第二代类似物,是一种有效的 CDK1/2/5/7/9 抑制剂。 |
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靶点/IC50 |
CDK1/cyclinB1 0.09μM (IC50) |
cdk2/cyclin A 0.072μM (IC50) |
CDK2/cyclinE 0.041μM (IC50) |
Cdk5/p25 0.11μM (IC50) |
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CDK7/cyclin H 1.1μM (IC50) |
CDK9/Cyclin T 0.18μM (IC50) |
CK1δ/ε 0.4μM (IC50) |
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体外研究 |
(R)-CR8 (CR8) trihydrochloride (0.1-100μM; 48 hours) is a potent inducer of apoptotic cell death with an IC50 of 0.49μM for SH-SY5Y cell line. (R)-CR8 trihydrochloride (0.25-10μM) 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: |
SH-SY5Y cell line |
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Concentration: |
0.1, 1, 10, 100μM |
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Incubation Time: |
24 hours |
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Result: |
Reduced cell survival in a dose-dependent manner. |
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体内研究 |
(R)-CR8 trihydrochloride (5mg/Kg; i.p.) results in a significant reduction in lesion size at 28 days in histological assessment . |
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Animal Model: |
Adult (10 to 12 weeks old) male Sprague-Dawley rats (310 to 330 g) |
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Dosage: |
5mg/Kg |
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Administration: |
i.p. |
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Result: |
Resulted in a significant reduction in lesion size. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )