MK-4827 (tosylate)
- CAS NO.：1038915-73-9
- Empirical Formula: C26H28N4O4S
- Molecular Weight: 492.58992
- MDL number: MFCD28167748
- SAFETY DATA SHEET (SDS)
- Update Date: 2026-01-20 19:14:41
What is MK-4827 (tosylate)?
Description
Niraparib tosylate (MK-4827 tosylate) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with an IC50 of 3.8 and 2.1 nM, respectively; with significant activity in cancer cells with mutant BRCA-1 and BRCA-2; >330-fold selective against PARP3, V-PARP, and Tank1. Niraparib tosylate leads to inhibition of repair of DNA damage, activates apoptosis, and shows anti-tumor activity.
The Uses of MK-4827 (tosylate)
Niraparib is a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors.
in vitro
In a whole-cell assay, Niraparib (MK-4827) tosylate hydrate inhibits PARP activity with EC50=4 nM and EC90=45 nM. Niraparib tosylate hydrate inhibits the proliferation of cancer cells with mutant BRCA-1 and BRCA-2 with CC50 in the 10-100 nM range. Niraparib tosylate hydrate displays excellent PARP 1 and 2 inhibition with IC50=3.8 and 2.1 nM, respectively, and in a whole-cell assay. Niraparib tosylate hydrate inhibits PARP within 15 minutes of treatment, reaching about 85% inhibition in the A549 cells at 1 h and about 55% inhibition at 1 h for the H1299 cells.
Properties of MK-4827 (tosylate)
| Melting point: | >142oC (dec.) |
| storage temp. | -20°C Freezer |
| solubility | Methanol (Slightly) |
| form | Solid |
| color | Off-White to Pale Yellow |
Safety information for MK-4827 (tosylate)
| Signal word | Warning |
| Pictogram(s) |
 Exclamation Mark Irritant GHS07 |
| GHS Hazard Statements |
H302:Acute toxicity,oral H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
| Precautionary Statement Codes |
P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for MK-4827 (tosylate)
| InChIKey | LCPFHXWLJMNKNC-XOIICWPPNA-N |
| SMILES | S(C1C=CC(C)=CC=1)(O)(=O)=O.C(C1=CC=CC2=CN(C3C=CC([C@H]4CNCCC4)=CC=3)N=C12)(=O)N |&1:23,r| |
MK-4827 (tosylate) manufacturer
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