NU2058

製品コードS5316 バッチS531601

印刷

化学情報

Synonyms

O(6)-Cyclohexylmethylguanine

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₂H₁₇N₅O

分子量

247.30

CAS No.

161058-83-9

Solubility (25°C)*

体外

DMSO

49 mg/mL (198.13 mM)

Ethanol

49 mg/mL (198.13 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	NU2058 (O(6)-Cyclohexylmethylguanine) 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.
in vitro	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 this compound are independent of CDK2 inhibition^[1]. In LNCaP cells and their Casodex-resistant derivative, LNCaP-cdxR, growth inhibition by this chemical 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. It 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].

製品説明

NU2058 (O(6)-Cyclohexylmethylguanine) 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.

in vitro

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 this compound are independent of CDK2 inhibition^[1]. In LNCaP cells and their Casodex-resistant derivative, LNCaP-cdxR, growth inhibition by this chemical 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. It 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].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	The human head and neck cancer cell line, SQ20b
	濃度	100 μM
	反応時間	4 h
	実験の流れ	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 this compound, 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.

参考

https://pubmed.ncbi.nlm.nih.gov/19426695/
https://pubmed.ncbi.nlm.nih.gov/17599054/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Combined therapy with DR5-targeting antibody-drug conjugate and CDK inhibitors as a strategy for advanced colorectal cancer [ Cell Rep Med, 2025, S2666-3791(25)00231-9]	PubMed: 40449480
Blockade of Nuclear β-Catenin Signaling via Direct Targeting of RanBP3 with NU2058 Induces Cell Senescence to Suppress Colorectal Tumorigenesis [ Adv Sci (Weinh), 2022, e2202528]	PubMed: 36270974

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。