All AbMole products are for research use only, cannot be used for human consumption.
MK-4827 (Niraparib) is an oral potent, selective PARP-1 and PARP-2 inhibitor currently in phase I clinical trials for cancer treatment. MK-4827 shows excellent PARP 1 and 2 inhibition with IC(50) = 3.8 and 2.1 nM, respectively, and in a whole cell assay, it inhibited PARP activity with EC(50) = 4 nM and inhibited proliferation of cancer cells with mutant BRCA-1 and BRCA-2 with CC(50) in the 10-100 nM range. MK-4827 reduced PAR levels in tumors by 1 h after administration which persisted for up to 24 h. MK-4827 was well tolerated in vivo and demonstrated efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer. In addition, MK-4827 strongly enhances the effect of radiation on a variety of human tumor xenografts, both p53 wild type and p53 mutant.
Sci Rep. 2023 Feb 27;13(1):3334.
Inhibition of nicotinamide dinucleotide salvage pathway counters acquired and intrinsic poly(ADP-ribose) polymerase inhibitor resistance in high-grade serous ovarian cancer
Niraparib (MK-4827) purchased from AbMole
Nat Commun. 2019 Jun 11;10(1):2556.
Exploiting interconnected synthetic lethal interactions between PARP inhibition and cancer cell reversible senescence.
Niraparib (MK-4827) purchased from AbMole
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Source | Oncotarget (2017). Figure 3. MK-4827 |
| Method | Western blotting | |
| Cell Lines | J45.01 cells | |
| Concentrations | - | |
| Incubation Time | 48 hrs | |
| Results | Similar analysis for DNMT1 showed increased levels of DNMT1 in the chromatin-bound fraction from cells exposed to [DAC+Rom+Npb] compared with cells exposed to [DAC+Rom]; the DNMT1 ratio was 0.25:1 ([DAC+Rom+Npb]:[DAC+Rom]) in the soluble extracts and 2.09:1 in the chromatin-bound fractions |
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
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| Animal models | Female nude mice (Ncr Nu/Nu) with solitary tumor xenografts |
| Formulation | suspended in 0.5% HPMC in deionized water, mixed for 24 h |
| Dosages | 25 or 50 mg/kg |
| Administration | orally gavage |
| Molecular Weight | 320.39 |
| Formula | C19H20N4O |
| CAS Number | 1038915-60-4 |
| Solubility (25°C) | DMSO ≥ 20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PARP Products |
|---|
| 2-Methylquinazolin-4-ol
2-Methylquinazolin-4-ol is a potent competitive poly(ADP-ribose) synthetase inhibitor, with a Ki of 1.1 μM. 2-Methylquinazolin-4-ol mammalian aspartate transcarbamylase (ATCase) inhibitor, with IC50 of 0.20 mM. |
| DPQ
DPQ is a potent PARP-1 inhibitor. |
| OUL232
OUL232 is a potent inhibitor of mono-ARTs PARP7, PARP10, PARP11, PARP12, PARP14, and PARP15. |
| AZ3391
AZ3391 is a potent inhibitor of PARP. |
| PARP1-IN-5
PARP1-IN-5 is a low toxicity, orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). |
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Products are for research use only. Not for human use. We do not sell to patients.
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