切换导航

Roscovitine (Seliciclib,CYC202)

现货
Catalog No.
A1723
CDK抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 800.00
现货
5mg
¥ 500.00
现货
10mg
¥ 800.00
现货
25mg
¥ 1,300.00
现货
100mg
¥ 2,000.00
现货

电话: 021-55669583

邮箱: sales@apexbio.cn

全球经销商

Background

Roscovitine, also known as seliciclib or CYC202, is a selective cyclin-dependent kinases (cdk), which are essential cell cycle regulators frequently involved in the deregulation of human tumors, inhibitor that potently inhibits cdc2 (cdc2/cyclin B), cdk2 (cdk2/cyclin A and cdk2/cyclin E) and cdk5 (cdk5/p35) with half maximal inhibition concentration IC50 of 0.65 μM, 0.7 μM, 0.7 μM and 0.16 μM respectively [1].

Roscovitine has been found to inhibit cellular prophase/metaphase transition at micromolar concentrations, where it inhibits progesterone-induced oocyte maturation of Xenopus oocytes and arrests starfish oocytes and sea urchin embryos in late prophase [1].

Additionally, roscovitine is capable of inhibiting extracelluar regulated kinases, erk1 and erk2, with IC50 of 34 μM and 14 μM respectively [1].

References:
[1] Meijer L, Borgne A, Mulner O, Chong JP, Blow JJ, Inagaki N, Inagaki M, Delcros JG, Moulinoux JP. Biochemical and cellular effects of roscovitine, a potent and selective inhibitor of the cyclin-dependent kinases cdc2, cdk2 and cdk5. Eur J Biochem. 1997 Jan 15;243(1-2):527-36.

文献引用

1. Azimi A, Caramuta S, et al. "Targeting CDK2 overcomes melanoma resistance against BRAF and Hsp90 inhibitors." Mol Syst Biol. 2018 Mar 5;14(3):e7858. PMID:29507054
2. Ruegsegger GN, Toedebusch RG, et al. "Loss of Cdk5 function in the nucleus accumbens decreases wheel running and may mediate age-related declines in voluntary physical activity." J Physiol. 2016 Jul 27. PMID:27461471

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt354.45
Cas No.186692-46-6
FormulaC19H26N6O
Solubility≥17.7225mg/mL in DMSO
Chemical Name(2R)-2-[[6-(benzylamino)-9-propan-2-ylpurin-2-yl]amino]butan-1-ol
SDFDownload SDF
Canonical SMILESCCC(CO)NC1=NC2=C(C(=N1)NCC3=CC=CC=C3)N=CN2C(C)C
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议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。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

有丝分裂海胆胚胎

溶解方法

该化合物在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。

反应条件

IC50: 10 μM, 60 min

实验结果

受精后60分钟添加roscovitine,研究发现,roscovitine以剂量依赖性方式将细胞阻滞在晚期前期。在roscovitine滞留卵中可以观察到较大的核,这种阻滞是完全可逆的,使用海水洗涤后,卵再次进入有丝分裂周期并发育成正常的长腕幼虫。100 μM最高浓度的roscovitme可以观察到相同的现象。

动物实验 [2]:

动物模型

注射A4573细胞的雄性无胸腺裸鼠

剂量

腹膜内注射,每天50 mg/kg,持续5天或两个5天系列,其间休息2天。

实验结果

Roscovitine治疗小鼠的肿瘤生长速度显著低于对照组,反映了切除后观察到的显著更小的个体肿瘤体积。相对于治疗开始时的肿瘤体积,第一个5天治疗系列完成后一天,roscovitine治疗动物的肿瘤大小仅生长了f1.25倍,而未治疗的小鼠中的肿瘤已经达到原始大小的14.5倍。这些值意味着肿瘤体积产生了11.5倍的差异。从roscovitine治疗的第1天开始计数,对照动物中的肿瘤在2天内达到原始体积的三倍,而治疗动物中的肿瘤需要10天才能达到初始体积三倍。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1] Meijer L, Borgne A, Mulner O, et al. Biochemical and cellular effects of roscovitine, a potent and selective inhibitor of the cyclin-dependent kinases cdc2, cdk2 and cdk5. European Journal of Biochemistry, 1997, 243(1-2): 527-536.

[2] Tirado O M, Mateo-Lozano S, Notario V. Roscovitine is an effective inducer of apoptosis of Ewing's sarcoma family tumor cells in vitro and in vivo. Cancer Research, 2005, 65(20): 9320-9327.

生物活性

描述 Roscovitine是一种有效的Cdk2/cyclin E、Cdk7/cyclin H、Cdk5/p35和cdc/cyclin B抑制剂,IC50值分别为0.1、0.49、0.16和0.65 ?M。
靶点 Cdk2/cyclin E Cdk7/cyclin H Cdk5/p35 cdc/cyclin B    
IC50 0.1 ?M 0.49 ?M 0.16 ?M 0.65 ?M    

质量控制

化学结构

Roscovitine (Seliciclib,CYC202)

相关生物数据

Roscovitine (Seliciclib,CYC202)

相关生物数据

Roscovitine (Seliciclib,CYC202)