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

目录号: HY-18340 纯度: 99.61%: FAQs
Data Sheet SDS COA 产品使用指南技术支持

(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。

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(R)-CR8 Chemical Structure

CAS No. : 294646-77-8

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥2750	In-stock
5 mg	￥2500	In-stock
10 mg	￥4000	In-stock
50 mg		询价
100 mg		询价

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Customer Review

Other Forms of (R)-CR8:

(S)-CR8 In-stock
(R)-CR8 trihydrochloride In-stock

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

生物活性
纯度 & 产品资料
参考文献

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^[1]^[2]. (R)-CR8 acts as a molecular glue degrader that depletes cyclin K^[3].

IC₅₀ & Target^[1]

Cdk1/cyclin B

0.09 μM (IC₅₀)

cdk2/cyclin A

0.072 μM (IC₅₀)

CDK2/cyclinE

0.041 μM (IC₅₀)

Cdk5/p25

0.11 μM (IC₅₀)

CDK7/cyclin H

1.1 μM (IC₅₀)

CDK9/Cyclin T

0.18 μM (IC₅₀)

CK1δ/ε

0.4 μM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
G-361	IC₅₀	0.503 μM Compound: CR8	Cytotoxicity against human G361 cells assessed as reduction in cell viability after 72 hrs by calcein AM staining based fluorescence assay Cytotoxicity against human G361 cells assessed as reduction in cell viability after 72 hrs by calcein AM staining based fluorescence assay	[PMID: 26851505]
HCT-116	IC₅₀	0.35 μM Compound: CR8	Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by calcein AM staining based fluorescence assay Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by calcein AM staining based fluorescence assay	[PMID: 26851505]
HEK293	IC₅₀	0.56 μM Compound: 8m, (R)-C&R8	Antiproliferative activity against HEK293 cells assessed as survival after 48 hrs by MTS reduction assay Antiproliferative activity against HEK293 cells assessed as survival after 48 hrs by MTS reduction assay	[PMID: 18698753]
HT	GI₅₀	0.263 μM Compound: CR8	Antiproliferative activity against human HT cells measured after 72 hrs by calcein AM dye-based fluorescence assay Antiproliferative activity against human HT cells measured after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 30943029]
K562	IC₅₀	0.175 μM Compound: CR8	Cytotoxicity against human K562 cells assessed as reduction in cell viability after 72 hrs by calcein AM staining based fluorescence assay Cytotoxicity against human K562 cells assessed as reduction in cell viability after 72 hrs by calcein AM staining based fluorescence assay	[PMID: 26851505]
MCF7	IC₅₀	0.16 μM Compound: CR8	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by calcein AM staining based fluorescence assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by calcein AM staining based fluorescence assay	[PMID: 26851505]
Sf9	IC₅₀	0.062 μM Compound: CR8	Inhibition of His-tagged CDK2/Cyclin-E1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured in presence of [gamma-33P]ATP Inhibition of His-tagged CDK2/Cyclin-E1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured in presence of [gamma-33P]ATP	[PMID: 30943029]
Sf9	IC₅₀	0.062 μM Compound: CR8	Inhibition of CDK2/Cyclin E (unknown origin) expressed in sf9 cells using histone H1 as substrate in presence of [gamma33P]-ATP Inhibition of CDK2/Cyclin E (unknown origin) expressed in sf9 cells using histone H1 as substrate in presence of [gamma33P]-ATP	[PMID: 26851505]
Sf9	IC₅₀	0.225 μM Compound: CR8	Inhibition of recombinant human full-length N-terminal GST-His6 fused CDK5 (M1 to P292 residues)/N-terminal His6-tagged p25 (A104 to R307 residues) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured in presence of [g Inhibition of recombinant human full-length N-terminal GST-His6 fused CDK5 (M1 to P292 residues)/N-terminal His6-tagged p25 (A104 to R307 residues) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured in presence of [g	[PMID: 30943029]
Sf9	IC₅₀	0.272 μM Compound: CR8	Inhibition of recombinant human N-terminal GST-His6-fused CDK9 (M1 to F372 residues)/N-terminal His6-tagged cyclin T1 (M1 to K726 residues) expressed in baculovirus infected Sf9 insect cells using (YSPTSPS)2KK as substrate measured in presence of [gamma-3 Inhibition of recombinant human N-terminal GST-His6-fused CDK9 (M1 to F372 residues)/N-terminal His6-tagged cyclin T1 (M1 to K726 residues) expressed in baculovirus infected Sf9 insect cells using (YSPTSPS)2KK as substrate measured in presence of [gamma-3	[PMID: 30943029]
Sf9	IC₅₀	0.787 μM Compound: CR8	Inhibition of His-tagged CDK1/Cyclin-B1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured in presence of [gamma-33P]ATP Inhibition of His-tagged CDK1/Cyclin-B1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured in presence of [gamma-33P]ATP	[PMID: 30943029]
Sf9	IC₅₀	1.769 μM Compound: CR8	Inhibition of recombinant human N-terminal GST-His6-fused CDK7 (M1 to F346 residues)/N-terminal His-tagged cyclin H (M1 to L323 residues)/N-terminal His6-tagged MAT1 (M1 to S306 residues) expressed in baculovirus infected Sf9 insect cells using (YSPTSPS)2 Inhibition of recombinant human N-terminal GST-His6-fused CDK7 (M1 to F346 residues)/N-terminal His-tagged cyclin H (M1 to L323 residues)/N-terminal His6-tagged MAT1 (M1 to S306 residues) expressed in baculovirus infected Sf9 insect cells using (YSPTSPS)2	[PMID: 30943029]
Sf9	IC₅₀	26.09 μM Compound: CR8	Inhibition of recombinant human N-terminal GST-fused CDK4 (S4 to E303 residues)/cyclin D1 (Q4 to I295 residues) expressed in baculovirus infected Sf9 insect cells using RPPTLSPIPHIPR as substrate measured in presence of [gamma-33P]ATP Inhibition of recombinant human N-terminal GST-fused CDK4 (S4 to E303 residues)/cyclin D1 (Q4 to I295 residues) expressed in baculovirus infected Sf9 insect cells using RPPTLSPIPHIPR as substrate measured in presence of [gamma-33P]ATP	[PMID: 30943029]
SH-SY5Y	IC₅₀	0.43 μM Compound: 8m, (R)-C&R8	Antiproliferative activity against human SH-SY5Y cells assessed as survival after 48 hrs by MTS reduction assay Antiproliferative activity against human SH-SY5Y cells assessed as survival after 48 hrs by MTS reduction assay	[PMID: 18698753]

体外研究
(In Vitro)

(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^[1].
(R)-CR8 (0.25-10 μM) induces a dose-dependent induction of poly-(ADP-ribose)polymerase (PARP) cleavage^[1].
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^[3].

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

Apoptosis Analysis^[1]

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^[2].

MCE 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)^[2]
Dosage:	i.p.
Administration:	5 mg/Kg
Result:	Resulted in a significant reduction in lesion size.

Clinical Trial

分子量

431.53

Formula

C₂₄H₂₉N₇O

CAS 号

294646-77-8

性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

细胞实验：

DMSO 中的溶解度 : 50 mg/mL (115.87 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

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

查看完整储备液配制表

* 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。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

计算结果

工作液所需浓度 : mg/mL

纯度 & 产品资料

纯度: 99.61%

选择批次：

Data Sheet (607 KB) SDS (393 KB)

COA (195 KB) HNMR (253 KB) LCMS (94 KB)

产品使用指南 (1538 KB)

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. [Content Brief]

[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. [Content Brief]

[3]. Słabicki M, et al. The CDK inhibitor CR8 acts as a molecular glue degrader that depletes cyclin K [published online ahead of print, 2020 Jun 3]. Nature. 2020;10.1038/s41586-020-2374-x. [Content Brief]

(R)-CR8 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.3173 mL	11.5867 mL	23.1734 mL	57.9334 mL
	5 mM	0.4635 mL	2.3173 mL	4.6347 mL	11.5867 mL
	10 mM	0.2317 mL	1.1587 mL	2.3173 mL	5.7933 mL
	15 mM	0.1545 mL	0.7724 mL	1.5449 mL	3.8622 mL
	20 mM	0.1159 mL	0.5793 mL	1.1587 mL	2.8967 mL
	25 mM	0.0927 mL	0.4635 mL	0.9269 mL	2.3173 mL
	30 mM	0.0772 mL	0.3862 mL	0.7724 mL	1.9311 mL
	40 mM	0.0579 mL	0.2897 mL	0.5793 mL	1.4483 mL
	50 mM	0.0463 mL	0.2317 mL	0.4635 mL	1.1587 mL
	60 mM	0.0386 mL	0.1931 mL	0.3862 mL	0.9656 mL
	80 mM	0.0290 mL	0.1448 mL	0.2897 mL	0.7242 mL
	100 mM	0.0232 mL	0.1159 mL	0.2317 mL	0.5793 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

(R)-CR8294646-77-8CR8, (R)-IsomerMolecular GluesCDKApoptosisCyclin dependent kinasecelldeathapoptosisneuroprotectivelesionHippocampusPARPcaspasesInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

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上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

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

Customer Review

Other Forms of (R)-CR8: