NU 2058 Chemical Properties

Melting point:

199°C(lit.)

Boiling point:

424.8±55.0 °C(Predicted)

Density 

1.52±0.1 g/cm3(Predicted)

storage temp. 

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

solubility 

DMSO: 22 mg/mL

pka

7.36±0.20(Predicted)

form 

powder to crystal

color 

white

λmax

281nm(MeOH)(lit.)

InChIKey

MWGXGTJJAOZBNW-UHFFFAOYSA-N

Safety Information

Hazard Codes 

Xi

Risk Statements 

36/37/38

Safety Statements 

26-36/37

WGK Germany 

3

HS Code 

2933.99.9000

NU 2058 Usage And Synthesis

Description

NU 2058 is an inhibitor of cyclin-dependent kinase 1 (Cdk1) and Cdk2 (IC₅₀s = 7.0 and 17 μM, respectively). Increased Cdk activity is often associated with human tumors, and inhibitors of Cdks, including NU 2058, can arrest cell cycling in cancer cells in vitro.

Uses

NU 2058 is an intermediate of NU 6140 (N925295), a cyclin-dependant kinase 2 inhibitor which demonstrates 10-36 fold selectivity against Cdk2-cyclin A. This selectivity induces cell-cycle arrest at the G2-M phase and potentiates the apoptotic effect of pacitaxel.

Biological Activity

Cyclin-dependent kinase (cdk) 1 and cdk2 inhibitor (K i values are 5 and 12 μ M respectively). Inhibits growth of human tumor cells in vitro (mean GI 50 = 13 μ M). Also inhibits DNA topoisomerase II ATPase activity (IC 50 = 300 μ M).

storage

Store at +4°C

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