(R)-CR8 CR8, (R-Isomer)|cas:294646-77-8|西域试剂

(R)-CR8 CR8, (R-Isomer),98.47%

产品编号：Bellancom-18340| CAS NO：294646-77-8| 分子式：C₂₄H₂₉N₇O| 分子量：431.53

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-18340		￥5500.00	杭州北京（现货）
Bellancom-18340		￥9900.00	杭州北京（现货）

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(R)-CR8 CR8, (R-Isomer)

产品介绍

(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。

生物活性

(R)-CR8 (CR8), a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)-CR8 inhibits 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) and CK1δ/ε (0.4 μM). (R)-CR8 induces apoptosis and has neuroprotective effect. (R)-CR8 acts as a molecular glue degrader that depletes cyclin K.

体外研究

(R)-CR8 (CR8) (0.1-100 μM; 48 hours) is a potent inducer of apoptotic cell death with an IC₅₀ 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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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
(In Vivo)

(R)-CR8 (5 mg/Kg; i.p.) results in a significant reduction in lesion size at 28 days in histological assessment.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (231.73 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3173 mL	11.5867 mL	23.1734 mL
5 mM	0.4635 mL	2.3173 mL	4.6347 mL
10 mM	0.2317 mL	1.1587 mL	2.3173 mL

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。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式