NU1025 Chemical Properties

Melting point:

253-258°C

Boiling point:

345.4±44.0 °C(Predicted)

Density 

1.42

storage temp. 

−20°C

solubility 

DMSO: 35 mg/mL, soluble

form 

solid

pka

8.68±0.20(Predicted)

color 

off-white

CAS DataBase Reference

90417-38-2

Safety Information

Hazard Codes 

Xn

Risk Statements 

22

Safety Statements 

26

WGK Germany 

3

HS Code 

29335990

MSDS

• Language:English Provider:SigmaAldrich

NU1025 Usage And Synthesis

Description

NU 1025 is an inhibitor of poly(ADP-ribose) polymerases (PARP) (IC₅₀ = 400 nM). It enhances the cytotoxicity of γ-irradiation and certain anticancer drugs. NU 1025 is also used to study the regulation of deoxyribonucleic acid repair by PARP enzymes.

Chemical Properties

Off-White to Pale Yellow Solid

Uses

NU 1025 is an inhibitor of poly(ADP-ribose) polymerases (PARP) (IC50 = 400 nM). It enhances the cytotoxicity of γ-irradiation and certain anticancer drugs. NU 1025 is also used to study the regulation of deoxyribonucleic acid repair by PARP enzymes.[Cayman Chemical]

Uses

A potent inhibitor of poly (ADP-ribose) polymerase (PARP). Ki and IC50 values are 48 and 400 nM respectively.

Definition

ChEBI: A member of the class of quinazolines that is quinazolin-4(1H)-one substituted by a hydroxy group at position 8 and a methyl group at position 2. It has been shown to exhibit inhibitory activity against poly(ADP-ribose) polymerase.

Biological Activity

Novel, potent inhibitor of poly(ADP-ribose) polymerase (PARP). K i and IC 50 values are 48 and 400 nM respectively.

References

[1] ROGER J. GRIFFIN. Resistance-Modifying Agents. 5. 1 Synthesis and Biological Properties of Quinazolinone Inhibitors of the DNA Repair Enzyme Poly(ADP-ribose) Polymerase (PARP)[J]. Journal of Medicinal Chemistry, 1998, 41 26: 5247-5256. DOI: 10.1021/jm980273t
[2] KJ BOWMAN. Potentiation of anti-cancer agent cytotoxicity by the potent poly(ADP-ribose) polymerase inhibitors NU1025 and NU1064[J]. British Journal of Cancer, 1998, 78 10: 1269-1277. DOI: 10.1038/bjc.1998.670
[3] C A DELANEY. Potentiation of temozolomide and topotecan growth inhibition and cytotoxicity by novel poly(adenosine diphosphoribose) polymerase inhibitors in a panel of human tumor cell lines.[J]. Clinical Cancer Research, 2000, 6 7: 2860-2867.
[4] SLAWOMIR KUMALA. Repair of DNA strand breaks in a minichromosome in vivo: kinetics, modeling, and effects of inhibitors.[J]. PLoS ONE, 2013: e52966. DOI: 10.1371/journal.pone.0052966

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