(R)-CR8 trihydrochloride|1786438-30-9|(CR8, (R)-Isomer trihydrochloride)-陌孚医药/Medlife

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(R)-CR8 trihydrochloride (Synonyms: CR8, (R)-Isomer trihydrochloride)

目录号: PL04801 纯度: ≥98%

CAS No. :1786438-30-9

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中文名称	(R)-CR8 trihydrochloride
中文别名	(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
英文名称	(R)-CR8 trihydrochloride
英文别名	(R)-CR8;(R)?-?CR8 (trihydrochloride);(2R)-2-[[9-(Methylethyl)-6-[[[4-(2-pyridinyl)phenyl]methyl]amino]-9H-purin-2-yl]amino]-1-butanol trihydrochloride;(2R)-2-[[9-Propan-2-yl-6-[(4-pyridin-2-ylphenyl)methylamino]purin-2-yl]amino]butan-1-ol;trihydrochlo;CR8, (R)-Isomer trihydrochloride;(R)-CR8 trihydrochloride
Cas No.	1786438-30-9
分子式	C₂₄H₃₂Cl₃N₇O
分子量	540.92
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

(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。

生物活性

(R)-CR8 (CR8) trihydrochloride, a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)-CR8 trihydrochloride inhibits CDK1/cyclin B (IC 50 =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 trihydrochloride induces apoptosis and has neuroprotective effect. (R)-CR8 trihydrochloride acts as a molecular glue degrader that depletes cyclin K.

性状

Solid

IC50 & Target[1][2]

CDK1/cyclinB1 0.09 μM (IC50) cdk2/cyclin Aan

体外研究(In Vitro)

(R)-CR8 (CR8) trihydrochloride (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 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 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

(R)-CR8 trihydrochloride (5?mg/Kg; i.p.) results in a significant reduction in lesion size at 28 days in histological assessment. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Adult

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Bettayeb K, et al. CR8, a potent and selective, roscovitine-derived inhibitor of cyclin-dependent kinases. Oncogene. 2008 Oct 2;27(44):5797-807.
[2]. Kabadi SV, et al. CR8, a novel inhibitor of CDK, limits microglial activation, astrocytosis, neuronal loss, and neurologic dysfunction after experimental traumatic brain injury. J Cereb Blood Flow Metab. 2014 Mar;34(3):502-13.

溶解度数据	In Vitro: DMSO : 50 mg/mL (92.44 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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