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Niraparib (MK-4827) tosylate

Cat. No. M8926
Niraparib (MK-4827) tosylate Structure
Synonym:

MK-4827 tosylate

Size Price Availability Quantity
10mg USD 180 In stock
50mg USD 450 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Niraparib tosylate inhibits PARP1/PARP2 with IC50 of 3.8 nM/2.1 nM respectively. MK-4827 (Niraparib) inhibits PARP activity with EC50=4 nM and EC90=45 nM in a whole cell assay. MK-4827 inhibits proliferation of cancer cells with mutant BRCA-1 and BRCA-2 with CC50 in the 10−100 nM range.

MK-4827 is well tolerated in vivo and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer. MK-4827 enhances radiation response of p53 mutant Calu-6 tumor in both cases, with the single daily dose of 50 mg/kg being more effective than 25 mg/kg given twice daily.

Protocol
Cell Experiment
Cell lines V-C8 cells
Preparation method V-C8 (BRCA2-negative) Chinese hamster cells are treated with the PARP inhibitor MK-4827 for 24 h, washed and incubated in drug-free medium for 5-7 days until colonies formed.
Concentrations 50 nM
Incubation time 24 h
Animal Experiment
Animal models Female nude mice (Ncr Nu/Nu)
Formulation Suspended in 0.5% Methocel in deionized water
Dosages 25 or 50 mg/kg
Administration p.o.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 492.59
Formula C19H20N4O.C7H8O3S
CAS Number 1038915-73-9
Purity >99%
Solubility DMSO: ≥ 60 mg/mL
Storage at -20°C
References

Niraparib (MK-4827), a novel poly(ADP-Ribose) polymerase inhibitor, radiosensitizes human lung and breast cancer cells.
Bridges KA, et al. Oncotarget. 2014 Jul 15;5(13):5076-86. PMID: 24970803.

Poly (ADP-Ribose) polymerase inhibitor MK-4827 together with radiation as a novel therapy for metastatic neuroblastoma.
Mueller S, et al. Anticancer Res. 2013 Mar;33(3):755-62. PMID: 23482742.

Enhanced killing of cancer cells by poly(ADP-ribose) polymerase inhibitors and topoisomerase I inhibitors reflects poisoning of both enzymes.
Patel AG, et al. J Biol Chem. 2012 Feb 3;287(6):4198-210. PMID: 22158865.

MK-4827, a PARP-1/-2 inhibitor, strongly enhances response of human lung and breast cancer xenografts to radiation.
Wang L, et al. Invest New Drugs. 2012 Dec;30(6):2113-20. PMID: 22127459.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Niraparib (MK-4827) tosylate, MK-4827 tosylate supplier, PARP, inhibitors

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