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Niraparib R-enantiomer Inhibitor

For Research Use Only. Not for use in diagnostic procedures. Catalog #: MBS5753495

MBS5753495 is an inhibitor targeting Niraparib R-enantiomer. Niraparib R-enantiomer is an inhibitor of PARP1(IC50 of 2.4nM). More details

Product Documentation
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Sample Manual Insert View PDF
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Testing Data View PDF
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Certificate of Analysis (COA) View PDF
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QC Report View PDF
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Material Safety Data Sheet View PDF
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Technical Datasheet View PDF
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Protocol View PDF

Product Overview

Online Datasheet in PDF
Product Name
Niraparib R-enantiomer, Inhibitor
Full Product Name
Niraparib R-enantiomer
Product Synonym Names
MK 4827 (R-enantiomer)
Form/Format
Solid. Powder
Purity/Purification
98.00%
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent
Molecular Weight
320.39
Solubility
DMSO: 32mg/mL (99.88mM)
(<1mg/ml refers to the product slightly soluble or insoluble)
Formula
C19H20N4O
SMILES
O=C(C1=CC=CC2=CN(C3=CC=C([C@@H]4CNCCC4)C=C3)N=C12)N
CAS Number
1038915-58-0
Target & IC50
PARP-1: ic50 2.4nM
In Vitro
Niraparib R-enantiomer has somewhat lower in vitro metabolic clearance than the Niraparib S-enantiomer in rat liver microsomes, but Niraparib S-enantiomer is more potent in cell based assays (PARylation EC50, Niraparib R-enantiomer=30nM, Niraparib S-enantiomer=4.0nM; BRCA1-HeLa CC50, Niraparib R-enantiomer=470, Niraparib S-enantiomer=34nM). [1].

Product References and Citations for Niraparib R-enantiomer, inhibitor

Jones P, et al. Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors. J Med Chem. 2009 Nov 26;52(22):7170-85.
Jones P, et al. Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors. J Med Chem. 2009 Nov 26;52(22):7170-85.

Other Notes

Small volumes of Niraparib R-enantiomer, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.
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