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CAS: 161058-83-9
分子式: C12H17N5O
分子量: 247.3
熔点: 199 °C(lit.)
中文名称: 
o-环己基甲基鸟嘌呤
英文名称: 
nu 2058
o-cyclohexylmethylguanine
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货号品牌产品名称规格包装、参考价格
N868103MACKLINNU205898%980元/250mg;   咨询
储存:2-8°C
状态:白色到略淡黄色晶体或粉末
N793681MACKLINNU205810mM in DMSO880元/1ml;   咨询
储存:-20°C
N0958TCINU 2058>98.0%(HPLC)290元/20MG;   1190元/100MG;   咨询

基本信息

纯度/分析方法>98.0%(HPLC)
分子式/分子量C12H17N5O = 247.30
外观与形状(20℃)固体
储存温度0-10℃
应避免的情况加热
Reaxys-RN7645499
PubChem物质ID253661766
MDL编号MFCD05664734

技术规格

AppearanceWhite to Light yellow powder to crystal
Purity(HPLC)min. 98.0 area%
Elemental analysis(Nitrogen)27.00 to 29.50 %

物性(参考值)

熔点199 ℃
最大吸收波长281(MeOH) nm

安全信息

图形或危害标志
信号词警告
危险性说明H315 : 造成皮肤刺激。
H319 : 造成严重眼刺激。
防范说明P264 : 作业后彻底清洗皮肤。
P280 : 戴防护手套/戴防护眼罩/戴防护面具。
P302 + P352 : 如皮肤沾染:用水充分清洗。
P337 + P313 : 如仍觉眼刺激:求医/就诊。
P305 + P351 + P338 : 如进入眼睛:用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出,取出隐形眼镜。继续冲洗。
P362+P364 : 脱掉沾污的衣服,清洗后方可重新使用。
P332 + P313 : 如发生皮肤刺激:求医/就诊。
144505J&KNU205899%, 一种CDK抑制剂, 抑制CDK2和CDK1665元/5MG;   1140元/10MG;   咨询

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
N4286Sigma-AldrichNU2058>98% (HPLC)2000.82元/5 MG;   咨询

产品说明

生化/生理作用

Selective cyclin-dependent kinase-2 (CDK2) inhibitor.

基本信息

经验(实验)分子式C12H17N5O
分子量247.30
MDL编号MFCD05664734
PubChem化学物质编号24724549
NACRESNA.77

产品性质

质量水平100
测定>98% (HPLC)
形式solid
颜色 white
溶解性DMSO: 22 mg/mL
H2O: soluble
储存温度2-8℃
SMILES stringNc1nc(OCC2CCCCC2)c3nc[nH]c3n1
InChI1S/C12H17N5O/c13-12-16-10-9(14-7-15-10)11(17-12)18-6-8-4-2-1-3-5-8/h7-8H,1-6H2,(H3,13,14,15,16,17)
InChI keyMWGXGTJJAOZBNW-UHFFFAOYSA-N
Gene Informationhuman ... CDK2(1017)

安全信息

象形图GHS07
警示用语:Warning
危险声明H315 - H319 - H335
预防措施声明P261 - P264 - P271 - P280 - P302 + P352 - P305 + P351 + P338
危险分类Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
靶器官Respiratory system
储存分类代码11 - Combustible Solids
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable
个人防护装备dust mask type N95 (US), Eyeshields, Gloves
436931Fluorochem6-(Cyclohexylmethoxy)-9H-purin-2-amine95%1980元/250mg;   4928元/1g;   咨询

基本信息

CAS Number161058-83-9
MDL NumberMFCD05664734
CAS号首数字顺序排列: 1 2 3 4 5 6 7 8 9