161058-83-9|NU2058|CsnPharm

CAS No.: 161058-83-9

NU2058 Catalog No. CSN11589

Synonyms: O6-(Cyclohexylmethyl)guanine

NU2058 is a CDK inhibitor with IC50 of 17 μM and 26 μM for CDK2 and CDK1.

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生物活性

描述Cyclin-dependent kinases (CDK), and their partner cyclins, are key proteins in the regulation of the cell cycle and are frequently deregulated in cancer cells. NU2058 is a potent and selective inhibitor of CDKs with IC₅₀ values of 17 and 26 μM for CDK2 and CDK1 in an isolated enzyme assay, respectively^[3]. In SQ20b cancer cells, NU2058 (100 μM; 2h) increased cisplatin cytotoxicity, by clonogenic assay, with a dose modification factor (DMF) of 3.1. It increased total intracellular platinum levels 1.5-fold, and platinum-DNA adduct levels twofold. Furthermore, NU2058 also potentiated melphalan (DMF 2.3), and monohydroxymelphalan (1.7)^[4]. NU2058 induced growth inhibition in LNCaP and LNCaP-cdxR cell lines with GI₅₀ values of 15 ± 4 and 17 ± 3 μM, respectively. In both cell lines, treatment with NU2058 for 24h or 48h caused an accumulation of cells in G0/G1 and a profound decrease in the S-phase fraction in a concentration-dependent manner^[3].
参考文献

[1] Jensen LH, Thougaard AV, et al. Substituted purine analogues define a novel structural class of catalytic topoisomerase II inhibitors. Cancer Res. 2005 Aug 15;65(16):7470-7.
[2] Arris CE, Boyle FT, et al. Identification of novel purine and pyrimidine cyclin-dependent kinase inhibitors with distinct molecular interactions and tumor cell growth inhibition profiles. J Med Chem. 2000 Jul 27;43(15):2797-804.
[3] Rigas AC, Robson CN, Curtin NJ. Therapeutic potential of CDK inhibitor NU2058 in androgen-independent prostate cancer. Oncogene. 2007 Dec 6;26(55):7611-9
[4] Harrison LR, Ottley CJ, et al. The kinase inhibitor O6-cyclohexylmethylguanine (NU2058) potentiates the cytotoxicity of cisplatin by mechanisms that are independent of its effect upon CDK2. Biochem Pharmacol. 2009 May 15;77(10):1586-92

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.0437 mL
- 20.2187 mL
- 40.4373 mL
- 5 mM
- 0.8087 mL
- 4.0437 mL
- 8.0875 mL
- 10 mM
- 0.4044 mL
- 2.0219 mL
- 4.0437 mL

技术信息

CAS号

161058-83-9

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C12H17N5O

运输

蓝冰

分子量

247.30

别名

O6-(Cyclohexylmethyl)guanine

溶解度

DMSO	100.0 mg/mL (404.4 mM)
Water	insoluble

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