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Niraparib hydrochloride

Name: Niraparib hydrochloride
Brand: TargetMol
SKU: T3353
Price: 34 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T3353Cas No. 1038915-64-8

Alias MK-4827 hydrochloride, MK-4827 (hydrochloride)

Niraparib hydrochloride (MK-4827 hydrochloride) is an inhibitor of poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity. By inhibiting PARP activity, niraparib hydrochloride increases DNA strand breaks, leading to genomic instability and apoptosis. The PARP family of proteins detects and repairs single-strand DNA breaks via the base-excision repair (BER) pathway.

Niraparib hydrochloride

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Purity: 99.26%

Catalog No. T3353Alias MK-4827 hydrochloride, MK-4827 (hydrochloride)Cas No. 1038915-64-8

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$34	In Stock	In Stock
5 mg	$55	In Stock	In Stock
10 mg	$80	In Stock	In Stock
25 mg	$119	-	In Stock
50 mg	$147	-	In Stock
100 mg	$228	Inquiry	Inquiry
1 mL x 10 mM (in DMSO)	$61	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:99.26%

Appearance:Solid

Color:Yellow

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	Niraparib hydrochloride (MK-4827 hydrochloride) is an inhibitor of poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity. By inhibiting PARP activity, niraparib hydrochloride increases DNA strand breaks, leading to genomic instability and apoptosis. The PARP family of proteins detects and repairs single-strand DNA breaks via the base-excision repair (BER) pathway.
Targets&IC50	PARP2:2.1 nM, PARP3:1300 nM, PARP1:3.8nM, PARP4:330 nM, tankyrase 1:570 nM
In vitro	MK-4827 significantly enhances the effectiveness of radiation on human tumor xenografts (whether p53 wild-type or p53 mutant), demonstrating good tolerability in vivo. When used alone, it also exhibits efficacy against BRCA-1 deficient xenograft models.
In vivo	In cell assays, MK-4827 exhibits inhibitory effects on PARP activity (EC50: 4 nM) and suppresses the proliferation of cancer cells carrying BRCA-1/2 mutations (IC50: 10-100 nM). It effectively inhibits PARP-1/2 (IC50: 3.8/2.1 nM) but shows significantly lower selectivity (over 100-fold) against PARP-3, V-PARP, and tankyrase-1 (IC50: 1300/330/570 nM). In MDA-MB-436 human breast adenocarcinoma cells with a BRCA-1 mutation, MK-4827 has a CC50 of 18 nM; in CAPAN-1 human pancreatic cancer cells with a BRCA-2 deficiency, the CC50 is 90 nM. Normal human prostatic and breast epithelial cells exhibit resistance to MK-4827. This indicates that PARP inhibitors like MK-4827 have selective cytotoxicity in cancer cells with BRCA-1/2 mutations, minimizing the impact on surrounding tissue.
Synonyms	MK-4827 hydrochloride, MK-4827 (hydrochloride)

Chemical Properties

Molecular Weight	356.85
Formula	C₁₉H₂₁ClN₄O
Cas No.	1038915-64-8
Smiles	C(N)(=O)C=1C=2C(=CN(N2)C3=CC=C(C=C3)[C@@H]4CCCNC4)C=CC1.Cl
Relative Density.	1.343 g/cm3

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: 180 mg/mL (504.41 mM), Sonication is recommended.

DMSO: 50 mg/mL (140.11 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.6 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO/H2O

	1mg	5mg	10mg	50mg
1 mM	2.8023 mL	14.0115 mL	28.0230 mL	140.1149 mL
5 mM	0.5605 mL	2.8023 mL	5.6046 mL	28.0230 mL
10 mM	0.2802 mL	1.4011 mL	2.8023 mL	14.0115 mL
20 mM	0.1401 mL	0.7006 mL	1.4011 mL	7.0057 mL
50 mM	0.0560 mL	0.2802 mL	0.5605 mL	2.8023 mL
100 mM	0.0280 mL	0.1401 mL	0.2802 mL	1.4011 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc