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Niraparib (tosylate hydrate)

Product Specifications

UNSPSC Description

Niraparib (MK-4827) tosylate hydrate is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib tosylate hydrate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity[1][2][3].

Target Antigen

Apoptosis; PARP

Type

Reference compound

Related Pathways

Apoptosis;Cell Cycle/DNA Damage;Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/niraparib-tosylate-hydrate.html

Purity

99.97

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

NC(C1=CC=CC2=CN(C3=CC=C([C@H]4CNCCC4)C=C3)N=C21)=O.O=S(C5=CC=C(C)C=C5)(O)=O.O

Molecular Weight

510.61

References & Citations

[1]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.|[2]Bridges KA, et al. Niraparib (MK-4827), a novel poly(ADP-Ribose) polymerase inhibitor, radiosensitizes human lung and breast cancer cells. Oncotarget. 2014 Jul 15;5(13):5076-86.|[3]Wang L, et al. MK-4827, a PARP-1/-2 inhibitor, strongly enhances response of human lung and breast cancer xenografts to radiation. Invest New Drugs. 2012 Dec;30(6):2113-20.|[4]Mirza MR, et al. Niraparib Maintenance Therapy in Platinum-Sensitive, Recurrent Ovarian Cancer. N Engl J Med. 2016 Dec 1;375(22):2154-2164.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, sealed storage, away from moisture)

Product Datasheet

http://file.medchemexpress.com/batch_PDF/HY-10619E/Niraparib-tosylate-hydrate-DataSheet-MedChemExpress.pdf

Product MSDS

http://file.medchemexpress.com/batch_PDF/HY-10619E/Niraparib-tosylate-hydrate-SDS-MedChemExpress.pdf

Clinical Information

Launched

CAS Number

1613220-15-7

Available Sizes

Curated Selection

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