Molecular Formula | C9H8N2O2 |
Molar Mass | 176.17 |
Density | 1.42 |
Melting Point | 253-258°C |
Solubility | Soluble in DMSO |
Appearance | Form solid, color off-white |
Storage Condition | −20°C |
Physical and Chemical Properties | Bioactive NU1025 (NSC 696807) is an effective PARP inhibitor with IC50 of 400 nM. |
Use | 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. |
Target | IC50: 400 nM (PARP) Ki: 48 nM (PARP) |
Hazard Symbols | Xn - Harmful |
Risk Codes | 22 - Harmful if swallowed |
Safety Description | 26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
WGK Germany | 3 |
HS Code | 29335990 |
Reference Show more | 1: Kaundal RK, Shah KK, Sharma SS. 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. Epub 2006 Aug 2. PubMed PMID: 16935310. 2: Bowman KJ, Newell DR, Calvert AH, Curtin NJ. Differential effects of the poly (ADP-ribose) polymerase (PARP) inhibitor NU1025 on topoisomerase I and II inhibitor cytotoxicity in L1210 cells in vitro. Br J Cancer. 2001 Jan 5;84(1):106-12. PubMed PMID: 11139322; PubMed Central PMCID: PMC2363607. 3: Bowman KJ, White A, Golding BT, Griffin RJ, Curtin NJ. 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. PubMed PMID: 9823965; PubMed Central PMCID: PMC2063197. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 5.676 ml | 28.382 ml | 56.763 ml |
5 mM | 1.135 ml | 5.676 ml | 11.353 ml |
10 mM | 0.568 ml | 2.838 ml | 5.676 ml |
5 mM | 0.114 ml | 0.568 ml | 1.135 ml |
solubility | DMSO: 35 mg/mL, soluble |
in vitro study
NU1025(0.2 mM) treatment can reduce H2O2-induced cytotoxicity. NU1025 itself had no effect on cell activity. In cells treated with SIN-1(0.8 mM), NU1025 pretreatment can significantly increase cell survival rate (82.59±4.67%). NU1025 had no detectable pro-proliferative effect in D54 and U251 cells. NU1025 can significantly inhibit the promotion of TPT and RT on PARP-1 activity. No DNA strand breaks were detected after 200 μM NU1025 treatment alone.
in vivo studies
Rats treated with NU1025(1 and 3 mg/kg) can reduce 25% and 45% infarction respectively compared with solvent group. NU1025(1 and 3 mg/kg) treatment can significantly reduce edema volume. NU1025 can significantly improve neurological damage.