Niraparib (MK-4827) tosylate - 10mM in DMSO , CAS No.1038915-73-9

CAS: 1038915-73-9 Cat. No.: N408309 Molecular Weight: 492.59

GRADE & PURITY 10mM in DMSO

Synonyms

Niraparib tosylate, MK 4827 tosylate, ZEJULA | 2H-​Indazole-​7-​carboxamide, 2-​[4-​(3S)​-​3-​piperidinylphenyl]​-​, 4-​methylbenzenesulfona​te (1:1)

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Niraparib tosylate (MK-4827, ZEJULA) is a selective inhibitor ofPARP1/PARP2withIC50of 3.8 nM/2.1 nM. Niraparib increases formation of PARP-DNA complexes resulting in DNA damage,apoptosis, and cell death.
In vitro

Micromolar concentrations of niraparib radiosensitizes tumor cell lines derived from lung, breast, and prostate cancers independently of their p53 status but not cell lines derived from normal tissues. Niraparib also sensitizes tumor cells to H2O2 and converts H2O2-induced single strand breaks (SSBs) into DSBs during DNA replication.

In vivo

MK-4827 strongly enhances the effect of radiation on a variety of human tumor xenografts, both p53 wild type and p53 mutant. MK-4827 reduces PAR levels in tumors by 1 h after administration which persisted for up to 24 h. In vivo treatment with MK-4827 and radiation prolonged survival (p<0.01) compared to single modalities. In vivo superiority of MK-4827 plus radiation is further documented by significant elevations of cleaved caspase-3 and γ-H2AX in tumors from the combination group compared to single modality cohorts.
Cell Data

cell lines：

Concentrations：50 nM

Incubation Time：24 h

Powder Purity:≥99%

Specifications

Synonyms

Niraparib tosylate, MK 4827 tosylate, ZEJULA | 2H-​Indazole-​7-​carboxamide, 2-​[4-​(3S)​-​3-​piperidinylphenyl]​-​, 4-​methylbenzenesulfona​te (1:1)

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

Niraparib tosylate (MK-4827, ZEJULA) is a selective inhibitor of PARP1/PARP2 with IC50 of 3.8 nM/2.1 nM. Niraparib increases formation of PARP-DNA complexes resulting in DNA damage, apoptosis, and cell death.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Names and Identifiers

• Isomeric SMILES: CC1=CC=C(C=C1)S(=O)(=O)O.C1C[C@H](CNC1)C2=CC=C(C=C2)N3C=C4C=CC=C(C4=N3)C(=O)N
• Molecular Weight: 492.59
• Reaxy-Rn: 42083915
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=42083915&ln=

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro DMSO: 81 mg/mL (198.8 mM); Water: Insoluble; Ethanol: Insoluble