(R)-CR8

Cat. No. 3605 7 篇引用文献提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

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说明： Cdk inhibitor; potently inhibits cdk1 and cdk2; also inhibits CK1; acts as molecular glue

化学名： (2R)-2-[[9-(Methylethyl)-6-[[[4-(2-pyridinyl)phenyl]methyl]amino]-9H-purin-2-yl]amino]-1-butanol trihydrochloride

纯度： ≥99% (HPLC)

引用文献 (7)

生物活性技术数据溶解性计算器说明书参考文献

生物活性 for (R)-CR8

(R)-CR8 is a cyclin dependent kinase (cdk) inhibitor (reported IC₅₀ values are 0.036 - 0.07, 0.09 - 0.8, 0.13 - 0.68, 0.18 - 1 and >1 μM for cdk2, cdk1, cdk5, cdk9 and cdk7, respectively). Also inhibits casein kinase 1 (CK1; IC₅₀ = 0.6 μM). Acts as molecular glue; forms a complex between CDK12-cyclin K and the CUL4 adapter protein DDB1 resulting in ubiquination and degradation of cyclin K.

化合物库 for (R)-CR8

(R)-CR8 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。

技术数据 for (R)-CR8

分子量	540.92
公式	C₂₄H₂₉N₇O.3HCl
储存	Store at +4°C
纯度	≥99% (HPLC)
CAS Number	1786438-30-9
PubChem ID	90488866
InChI Key	ORYSYXHQFOWNDK-RGFWRHHQSA-N
Smiles	CC(C)N2C1=NC(N[C@H](CC)CO)=NC(NCC3=CC=C(C4=NC=CC=C4)C=C3)=C1N=C2.Cl.Cl.Cl

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for (R)-CR8

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
	water	54.09	100
	DMSO	54.09	100

制备储备液 for (R)-CR8

以下数据基于产品分子量 540.92。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

浓度/溶剂体积/质量	1 mg	5 mg	10 mg
1 mM	1.85 mL	9.24 mL	18.49 mL
5 mM	0.37 mL	1.85 mL	3.7 mL
10 mM	0.18 mL	0.92 mL	1.85 mL
50 mM	0.04 mL	0.18 mL	0.37 mL

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产品说明书 for (R)-CR8

分析证书/产品说明书

化学品安全技术说明书

参考文献 for (R)-CR8

参考文献是支持产品生物活性的出版物。

Oumata et al (2008) Roscovitine-derived, dual-specificity inhibitors of cyclin-dependent kinases and casein kinases 1. J.Med.Chem. 51 5229 PMID: 18698753

Jorda et al (2018) How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases? J.Med.Chem. 61 9105 PMID: 30234987

Słabicki et al (2020) The CDK inhibitor CR8 acts as a molecular glue degrader that depletes cyclin K. Nature 585 293 PMID: 32494016

If you know of a relevant reference for (R)-CR8, please let us know.

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