NU1025 | CAS#90417-38-2 | PARP inhibitor

MedKoo Cat#: 406359 | Name: NU1025

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Description:

WARNING: This product is for research use only, not for human or veterinary 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.

Chemical Structure

NU1025

CAS#90417-38-2

Theoretical Analysis

MedKoo Cat#: 406359

Name: NU1025

CAS#: 90417-38-2

Chemical Formula: C9H8N2O2

Exact Mass:

Molecular Weight: 176.17

Elemental Analysis:

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 240.00
25mg	USD 530.00
50mg	USD 980.00

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Related CAS #

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Synonym

NU-1025; NU1025; NU 1025.

IUPAC/Chemical Name

8-Hydroxy-2-methyl-4(3H)-quinazolinone

InChi Key

YJDAOHJWLUNFLX-UHFFFAOYSA-N

InChi Code

InChI=1S/C9H8N2O2/c1-5-10-8-6(9(13)11-5)3-2-4-7(8)12/h2-4,12H,1H3,(H,10,11,13)

SMILES Code

O=C1NC(C)=NC2=C1C=CC=C2O

Appearance

white solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble to 100 mM in 1eq. NaOH and to 100 mM in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

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Product Data

Product Data

Instruction

View handling instruction

Biological target:

NU1025 is a potent PARP inhibitor with an IC50 of 400 nM and a Ki of 48 nM.

In vitro activity:

Both cell lines were equisensitive to the growth-inhibitory effects of NU1025 per se (IC50 370 microM). Co-exposure of the cell lines to TM (100 microM) with increasing concentrations of NU1025 led to a synergistic enhancement of cytotoxicity, with IC50 values for NU1025 decreasing to 17 +/- 4 microM (TZR) and 37 +/- 6 microM (WT). Reference: Br J Cancer. 1998 Nov;78(10):1269-77. https://pubmed.ncbi.nlm.nih.gov/9328141/

In vivo activity:

The present study evaluated the effects of PARP inhibitor, 8-hydroxy-2 methyl-quinazolin-4-[3H]one (NU1025) in H2O2 and 3-morphilinosyndonimine (SIN-1) induced cytotoxicity in PC12 cells as well as in middle cerebral artery occlusion (MCAO) induced focal cerebral ischemia in rats. In MCAO studies, NU1025 was administered at different time points (1 h before reperfusion, immediately before reperfusion, 3 h after reperfusion and 6 h after reperfusion). NU1025 at 1 and 3 mg/kg reduced total infarct volume to 25% and 45%, respectively, when administered 1 h before reperfusion. NU1025 also produced significant improvement in neurological deficits. Neuroprotection with NU1025 was associated with reduction in PAR accumulation, reversal of brain NAD depletion and reduction in DNA fragmentation. Reference: Life Sci. 2006 Nov 10;79(24):2293-302. https://pubmed.ncbi.nlm.nih.gov/16935310/

	Solvent	mg/mL	mM
Solubility
	DMF	16.0	90.82
	DMF:PBS (pH 7.2) (1:1)	0.5	2.84
	DMSO	57.0	323.55
	Ethanol	0.1	0.62

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 176.17 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. 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. doi: 10.1038/bjc.1998.670. PMID: 9823965; PMCID: PMC2063197. 2. Boulton S, Kyle S, Durkacz BW. Low nicotinamide mononucleotide adenylyltransferase activity in a tiazofurin-resistant cell line: effects on NAD metabolism and DNA repair. Br J Cancer. 1997;76(7):845-51. doi: 10.1038/bjc.1997.473. PMID: 9328141; PMCID: PMC2228057. 3. Wang L, Gu Y, Zhang J, Gong L. Effects of Sleep Deprivation (SD) on Rats via ERK1/2 Signaling Pathway. Med Sci Monit. 2019 Apr 19;25:2886-2895. doi: 10.12659/MSM.913839. PMID: 31002658; PMCID: PMC6486800. 4. 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. doi: 10.1016/j.lfs.2006.07.034. Epub 2006 Aug 2. PMID: 16935310.

In vitro protocol:

In vivo protocol:

1. Wang L, Gu Y, Zhang J, Gong L. Effects of Sleep Deprivation (SD) on Rats via ERK1/2 Signaling Pathway. Med Sci Monit. 2019 Apr 19;25:2886-2895. doi: 10.12659/MSM.913839. PMID: 31002658; PMCID: PMC6486800. 2. 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. doi: 10.1016/j.lfs.2006.07.034. Epub 2006 Aug 2. PMID: 16935310.

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.