product name NU1025
Description: NU1025 is a potent poly(ADP-ribose) polymerase (PARP) inhibitor, which potentiates the cytotoxicity of a panel of mechanistically diverse anti-cancer agents in L1210 cells. NU1025 enhanced the cytotoxicity of the DNA-methylating agent MTIC, gamma-irradiation and bleomycin 3.5-, 1.4- and 2-fold respectively. Additionally, NU 1025 amplifies the cytotoxic effect of camptothecin, which is a topoisomerase I (Topo I) inhibitor.
References: Life Sci. 2006 Nov 10;79(24):2293-302.
176.17
Formula
C9H8N2O2
CAS No.
90417-38-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 35 mg/mL (198.7 mM)
Water: <1 mg/mL
Ethanol: 6 mg/mL warmed (34.1 mM)
Solubility (In vivo)
40% PEG 400+saline: 18mg/mL
Synonyms
NSC 696807
other peoduct :
| In Vitro |
In vitro activity: NU1025 (0.2 mM) treatment attenuates H2O2 induced cytotoxicity. NU1025 per se does not have any effect on cell viability. NU1025 pretreatment significantly increases cell viability (82.59 ?4.67%) in SIN-1 (0.8 mM) exposed cells. NU1025 has no detectable effect on the proliferation of D54 and U251 cells. Treatment with NU1025 markedly inhibits the enhanced activation of PARP-1 induced by TPT and RT treatment. No DNA strand breakage is detected following exposure to 200 µM NU1025 alone Kinase Assay: Cells are suspended in hypotonic buffer (9 mM HEPES, pH 7.8, 4.5% (v/v) dextran, 4.5 mM MgCl2 and 5 mM DTT) at 1.5 × 107/mL on ice for 30 min, then 9 vol of isotonic buffer (40 mM HEPES, pH 7.8, 130 mM KCl, 4% (v/v) dextran, 2 mM EGTA, 2.3 mM MgCl2, 225 mM sucrose and 2.5 mM DTT) is added. The reaction is started by adding 300 µL cells to 100 µL 300 µM NAD+ containing [32P]-NAD+, and terminated by the addition of 2 mL ice-cold 10% (w/v) TCA +10% (w/v) sodium pyrophosphate. After 30 min on ice the precipitated 32P-labelled ADP-ribose polymers are filtered, washed five times with 1% (v/v) TCA, 1% (v/v) sodium pyrophosphate, dried and counted. Cell Assay: Cells (D54 and U251 cells) are seeded in 96-well plates at a density of 2,500 cells/well and treated with the indicated doses of NU1025. Adherent cells are irradiated in medium with 250 kVp X-rays (dose rate 0.5 Gy/min). Untreated cells are used as a control. Following an up to 5 day incubation, cell proliferation is assessed by MTT assay. |
|---|---|
| In Vivo | Treatment with NU1025 (1 and 3 mg/kg) reduces the infarction to 25% and 45% versus vehicle treated rats, respectively. NU1025 (1 and 3 mg/kg) treatment significantly reduces edema volume. NU1025 also produces significant improvement in neurological deficits. |
| Animal model | Male Sprague Dawley rats |
| Formulation & Dosage | Dissolved in 40% PEG 400 in saline; 3 mg/kg; i.p. injection |
| References | Life Sci. 2006 Nov 10;79(24):2293-302. |
