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NU2058 CDK inhibitor

Cat.No.S5316

NU2058 (O(6)-Cyclohexylmethylguanine) is an inhibitor of CDK2 with IC50 value of 17 μM in an isolated enzyme assay. This compound also potentiates melphalan (DMF 2.3), and monohydroxymelphalan (1.7), but not temozolomide or ionising radiation.
NU2058 CDK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 247.30

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Quality Control

Batch: S531601 DMSO]49 mg/mL]false]Ethanol]49 mg/mL]false]Water]Insoluble]false Purity: 99.32%
99.32

Chemical Information, Storage & Stability

Molecular Weight 247.30 Formula

C12H17N5O

 Storage (From the date of receipt)
CAS No. 161058-83-9 -- Storage of Stock Solutions

Synonyms O(6)-Cyclohexylmethylguanine Smiles C1CCC(CC1)COC2=NC(=NC3=C2NC=N3)N

Solubility

In vitro
Batch:

DMSO : 49 mg/mL (198.13 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 49 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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In vivo Formulation Calculator (Clear solution)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
CDK2 [1]
(Cell-free assay)
17 μM
CDK1 [2]
(Cell-free assay)
26 μM
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].
References

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