CAS 90417-38-2|NU1025
| Common Name | NU1025 | ||
|---|---|---|---|
| CAS Number | 90417-38-2 | Molecular Weight | 176.172 |
| Density | 1.4±0.1 g/cm3 | Boiling Point | 345.4±44.0 °C at 760 mmHg |
| Molecular Formula | C9H8N2O2 | Melting Point | 253-258ºC |
| MSDS | ChineseUSA | Flash Point | 162.7±28.4 °C |
| Symbol | GHS07 | Signal Word | Warning |
Names
| Name | nu 1025 |
|---|---|
| Synonym | More Synonyms |
NU1025 BiologicalActivity
| 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 | Research Areas >>CancerSignaling Pathways >>Epigenetics >>PARPResearch Areas >>Neurological DiseaseSignaling Pathways >>Cell Cycle/DNA Damage >>PARP |
| 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. |
Chemical & Physical Properties
| 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 of Characters | solid | off-white |
| Vapour Pressure | 0.0±0.8 mmHg at 25°C |
| Index of Refraction | 1.678 |
| InChIKey | YJDAOHJWLUNFLX-UHFFFAOYSA-N |
| SMILES | Cc1nc2c(O)cccc2c(=O)[nH]1 |
| Storage condition | −20°C |
| Water Solubility | DMSO: 35 mg/mL, soluble |
Safety Information
| Symbol | 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 |
Customs
| 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% |
Articles1
More Articles| Rapamycin-resistant poly (ADP-ribose) polymerase-1 overexpression is a potential therapeutic target in lymphangioleiomyomatosis. Am. J. Respir. Cell. Mol. Biol. 51(6) , 738-49, (2014) Lymphangioleiomyomatosis (LAM) is a female-predominant cystic lung disease that can lead to respiratory failure. LAM cells typically have inactivating tuberous sclerosis complex 2 (TSC2) mutations and... |
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 |
