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  • DC Chemicals Limited
  • China
  • Product Name: NU1025
  • Price: $450.0/100mg $800.0/250mg $1600.0/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao

90417-38-2

90417-38-2 structure
90417-38-2 structure
  • Name: NU1025
  • Chemical Name: nu 1025
  • CAS Number: 90417-38-2
  • Molecular Formula: C9H8N2O2
  • Molecular Weight: 176.172
  • Catalog: Biochemical Inhibitor DNA damage PARP inhibitor
  • Create Date: 2018-10-04 17:47:06
  • Modify Date: 2024-01-02 16:09:22
  • NU1025 is a potent PARP inhibitor with an IC50 of 400 nM and a Ki of 48 nM. NU1025 potentiates the cytotoxicity of ionizing radiation and anticancer drugs. NU1025 has anti-cancer and neuroprotective activity[1][2][3].

Name nu 1025
Synonyms 8-Hydroxy-2-methylquinazolin-4(1H)-one
2-methylquinazoline-4,8-diol
MFCD00942555
4,8-quinazolinediol, 2-methyl-
8-hydroxy-2-methyl-1H-quinazolin-4-one
8-hydroxy-2-methylquinazolin-4(3H)-one
8-Hydroxy-2-methyl-4(1H)-quinazolinone
4(1H)-Quinazolinone, 8-hydroxy-2-methyl-
8-Hydroxy-2-methyl-4(3H)-quinazolinone
Description NU1025 is a potent PARP inhibitor with an IC50 of 400 nM and a Ki of 48 nM. NU1025 potentiates the cytotoxicity of ionizing radiation and anticancer drugs. NU1025 has anti-cancer and neuroprotective activity[1][2][3].
Related Catalog
Target

IC50: 400 nM (PARP)[2] Ki: 48 nM (PARP)[3]

In Vitro NU1025 (0.2 mM) pretreatment restores cell viability to approximately 73% and 82% in H2O2 and SIN-1 injured cells, respectively[1]. NU1025 enhances the cytotoxicity of the DNA-methylating agent MTIC, γ-irradiation and bleomycin 3.5-, 1.4- and 2-fold respectively in L1210 cells. The recovery from potentially lethal γ-irradiation damage cytotoxicity in plateau-phase cells is also inhibited by NU 1025. NU1025 causes a marked retardation of DNA repair[2]. Cell Viability Assay[1] Cell Line: PC12 cells Concentration: 0.2 mM Incubation Time: 6.5 hours Result: Restored cell viability to approximately 73% and 82% in H2O2 and SIN-1 injured cells.
In Vivo NU1025 (1-3 mg/kg; intraperitoneal injection; male Sprague Dawley rats) treatment at 1 and 3 mg/kg reduces total infarct volume to 25% and 45%, respectively, when administered 1 h before reperfusion. NU1025 also produces significant improvement in neurological deficits. Neuroprotection with NU1025 is associated with reduction in PAR accumulation, reversal of brain NAD depletion and reduction in DNA fragmentation[1]. Animal Model: Male Sprague Dawley rats (250-270 g) induced focal cerebral ischemia[1] Dosage: 1 mg/kg, 3 mg/kg Administration: Intraperitoneal injection Result: At 1 and 3 mg/kg, reduced total infarct volume to 25% and 45%, respectively.
References

[1]. Kaundal RK, et al. Neuroprotective effects of NU1025, a PARP inhibitor in cerebral ischemia are mediated through reduction in NAD depletion and DNA fragmentation. Life Sci. 2006 Nov 10;79(24):2293-302.

[2]. Bowman KJ, et al. Potentiation of anti-cancer agent cytotoxicity by the potent poly(ADP-ribose) polymerase inhibitors NU1025 and NU1064. Br J Cancer. 1998 Nov;78(10):1269-77.

[3]. Delaney CA, et al. Potentiation of temozolomide and topotecan growth inhibition and cytotoxicity by novel poly(adenosine diphosphoribose) polymerase inhibitors in a panel of human tumor cell lines. Clin Cancer Res. 2000 Jul;6(7):2860-7.

Density 1.4±0.1 g/cm3
Boiling Point 345.4±44.0 °C at 760 mmHg
Melting Point 253-258ºC
Molecular Formula C9H8N2O2
Molecular Weight 176.172
Flash Point 162.7±28.4 °C
Exact Mass 176.058578
PSA 65.98000
LogP 0.35
Appearance solid | off-white
Vapour Pressure 0.0±0.8 mmHg at 25°C
Index of Refraction 1.678
Storage condition −20°C
Water Solubility DMSO: 35 mg/mL, soluble
Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H302-H319
Precautionary Statements P305 + P351 + P338
Personal Protective Equipment dust mask type N95 (US);Eyeshields;Gloves
Hazard Codes Xn: Harmful;
Risk Phrases 22
Safety Phrases 26
RIDADR NONH for all modes of transport
WGK Germany 3
HS Code 2933990090

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Literature: Newcastle University Ventures Limited Patent: US6156739 A1, 2000 ;

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Literature: Journal of Medicinal Chemistry, , vol. 41, # 26 p. 5247 - 5256

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Literature: Journal of Medicinal Chemistry, , vol. 41, # 26 p. 5247 - 5256

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Literature: Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry, , vol. 24, p. 1182 - 1184

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Literature: Journal of Scientific and Industrial Research, , vol. 17 C, p. 193,194

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Literature: WO2004/31161 A1, ; Page 117 ;
HS Code 2933990090
Summary 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%