NU1025 | PARP inhibitor | CAS 90417-38-2

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Quality Control

Batch: Purity: 99.29%

99.29

Related Targets	HDAC ATM/ATR DNA-PK WRN DNA/RNA Synthesis Topoisomerase PPAR Sirtuin Casein Kinase eIF
Other PARP Inhibitors	XAV-939 AZD5305 (Saruparib) Veliparib (ABT-888) PJ34 HCl AG-14361 Iniparib (BSI-201) G007-LK Pamiparib UPF 1069 A-966492

Solubility

In vitro
Batch:

DMSO : 35 mg/mL (198.67 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 6 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	40% PEG 400 1 saline Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	10.000mg/ml (56.76mM)	Taking the 1 mL working solution as an example, take 10 mg of the product and add it to 1 ml of 40% PEG 400+saline solution, and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	176.17	Formula	C₉H₈N₂O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	90417-38-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	NSC 696807			Smiles	CC1=NC2=C(C=CC=C2O)C(=O)N1

Mechanism of Action

Targets/IC₅₀/Ki	PARP 400 nM
In vitro	NU1025 (0.2 mM) treatment attenuates H₂O₂ induced cytotoxicity. This compound per se does not have any effect on cell viability. Its pretreatment significantly increases cell viability (82.59 ?4.67%) in SIN-1 (0.8 mM) exposed cells. It has no detectable effect on the proliferation of D54 and U251 cells. Treatment with this chemical 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 of this compound alone.
Kinase Assay	PARP activation assay
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.
In vivo	Treatment with NU1025 (1 and 3 mg/kg) reduces the infarction to 25% and 45% versus vehicle treated rats, respectively. This compound (1 and 3 mg/kg) treatment significantly reduces edema volume. It also produces significant improvement in neurological deficits.
References	[1] https://pubmed.ncbi.nlm.nih.gov/16251802/ [2] https://pubmed.ncbi.nlm.nih.gov/16935310/ [3] https://pubmed.ncbi.nlm.nih.gov/25182801/ [4] https://pubmed.ncbi.nlm.nih.gov/11139322/

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NU1025 PARP inhibitor

Chemical Structure

Molecular Weight: 176.17