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NU2058

O6-环甲基己基鸟嘌呤

品牌
J&K
CAS
161058-83-9
货号
144505
规格纯度
99%, 一种CDK抑制剂, 抑制CDK2和CDK1
参考价格
665 *本价格含增值税费
促销
服务
  • 原厂保证
  • 包邮
  • 增值税票
数量
-+
产品名称:
161058-83-9
NU2058
O6-(Cyclohexylmethyl)guanine
O6-环甲基己基鸟嘌呤
产品介绍:

基本信息

分子式C12H17N5O
分子量247.30
MDL编码MFCD05664734
存储条件Freezer -20℃

产品描述

NU2058 is an inhibitor of CDK2 with IC50 value of 17 μM in an isolated enzyme assay. It also potentiates melphalan (DMF 2.3), and monohydroxymelphalan (1.7), but not temozolomide or ionising radiation.

靶点(IC50 & Targe)

CDK1

CDK2

Topo II

体外研究

NU2058 alters the transport of cisplatin, causing more Pt-DNA adducts, as well as sensitizing cells to cisplatin- and melphalan-induced DNA damage. However, the effects of NU2058 are independent of CDK2 inhibition[1]. In LNCaP cells and their Casodex-resistant derivative, LNCaP-cdxR, growth inhibition by NU2058 is accompanied by a concentration-dependent increase in p27 levels, reduced CDK2 activity and pRb phosphorylation, a decrease in early gene expression and G1 cell cycle phase arrest in both cell lines. NU2058 induces cell cycle reduction in S phase and inhibits phosphorylation of pRb. It induces a G1 arrest and increases p27 protein expression in LNCaP cells, showing no significant effect on p21 levels[2].

细胞实验

Cell lines: The human head and neck cancer cell line, SQ20b

Concentrations: 100 μM

Incubation Time: 4 h

Method: Cells are seeded into six-well plates (350,000 cells/well) and allowed to attach overnight. On the day of the experiment, growth media are replaced with media containing 100 μM of either NU2058, NU6102, NU6230 or DMSO (0.1% (v/v) final concentration) for 2 h followed by a further 2 h in the additional presence of cytotoxic drugs, unless otherwise indicated. For the radiation experiments, cells are treated for a total of 4 h with NU2058, and irradiated after the first 2 h. After treatment, the cells are washed twice with PBS, trypsinised, and replated into 100 mm Petri dishes at various cell densities (300-50,000 cells per plate). After approximately 12 days, media is removed, and cells are fixed with Carnoy's reagent (75% (v/v) methanol, 25% (v/v) acetic acid), stained with crystal violet (0.4% (w/v) in water) and colonies are counted.

(Only for Reference)

参考文献

[1] Harrison LR, et al. Biochem Pharmacol. 2009, 77(10):1586-92.

[2] Rigas AC, et al. Oncogene. 2007, 26(55):7611-9.

安全信息

图形或危害标志
危险说明H302
H410
防范说明P264
P270
P273
P301+P312
P330
P391
P501
UN号码3077
危险分类9
包装等级III

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