NMS-P118

Catalog No.S8363

NMS-P118 Chemical Structure

Molecular Weight(MW): 395.42

NMS-P118 is a potent, orally available, and highly selective PARP-1 inhibitor endowed with excellent ADME and pharmacokinetic profiles, showing 150-fold selectivity for PARP-1 over PARP-2 (Kd 0.009 μM vs 1.39 μM, respectively).

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Description NMS-P118 is a potent, orally available, and highly selective PARP-1 inhibitor endowed with excellent ADME and pharmacokinetic profiles, showing 150-fold selectivity for PARP-1 over PARP-2 (Kd 0.009 μM vs 1.39 μM, respectively).
Targets
PARP1 [1]
(Cell-free assay)
0.009 μM(Kd)
In vitro

NMS-P118 is a potent (KD = 0.009 μM) PARP-1 inhibitor, showing 150-fold selectivity over PARP-2 (KD = 1.39 μM). The compound shows high solubility and permeability[1].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HeLa cells Ml3LSpVv[3Srb36gZZN{[Xl? NITaTng{OCCvaX7z NInodFJKdmirYnn0bY9vKG:oIGDBVnAyKGmwIHj1cYFvKEinTHGgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJI9nKEh{T{KtbY5lfWOnZDDQRXIh\m:{bXH0bY9vKHC{ZXnuZ5Vj[XSnZDDmc5IhOzBibXnud{Bnd2yub4fl[EBjgSCKMl:yJIFl\Gm2aX;uJI1m[XO3cnXkJIFnfGW{IEG1JI1qdnNiYomgbY1ufW6xY4n0c4Np\W2rY3HsJIFv[Wy7c3nzMEBKSzVyPUCuNFQh|ryP MXSyOlIzOjNzOR?=
MDA-MB-436 cells Mm\GR5l1d3SxeHnjbZR6KGG|c3H5 M2rpNVExKHSxIEG0JIRigXN? MXLDfZRwfG:6aXPpeJkh[WejaX7zeEBDWkODMT3k[YZq[2mnboSgbJVu[W5iTVTBMW1DNTR|NjDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOxbH;ufUBnd3KvYYTpc44h[W[2ZYKgNVAhfG9iMUSg[IF6eyCkeTDjdpl{fGGuII\pc4xmfCC|dHHpcolv\yxiSVO1NF0xNjF2IN88US=> MXuyOlIzOjNzOR?=

... Click to View More Cell Line Experimental Data

In vivo NMS-P118 is proved to be metabolically stable, it modestly inhibits two cytochrome P450 family members (CYP-2B6 IC50, 8.15 μM; CYP-2D6 IC50, 9.51 μM) out of eight isoforms tested. NMS-P118 has low in vivo clearance, and complete oral bioavailability. The pharmacokinetic profile of NMS-P118 in rat dosed iv at 10 mg/kg and orally at 10 and 100 mg/kg, mirrors that observed in the mouse, with oral bioavailability >65%, and linearity of exposure with dose. Its treatment dramatically decreases intratumoral PAR levels at 1, 2, and 6 h after administration and partial recovery of PAR levels is observed at 24 h. NMS-P118 shows excellent ADME and pharmacokinetic profiles, high oral availability in the mouse and rat, and high efficacy both as a single agent and in combination with Temozolomide in BRCA1-mutated MDA-MB-436 and BRCA2 deficient Capan-1 human tumor xenograft models, respectively[1].

Protocol

Cell Research:[1]
+ Expand
  • Cell lines: HeLa cells
  • Concentrations: --
  • Incubation Time: 30 mins
  • Method: 6000 cells/well are seeded in 96-well plates in MEM/10% FCS and incubated for 24 h at 37℃, 5% carbon dioxide. Test compounds are then added at the required concentration for 30 min. DNA damage is then induced by adding hydrogen peroxide at the concentration of 0.1 mM for 15 min. Concentration curves are prepared in MEM/10% FCS from compound stocks in DMSO, and final DMSO concentration is 0.002% (v/v). Duplicate wells for each concentration point are prepared with a typical highest compound concentration of 20 μM and serial dilution 1:3. Plates are dried and fixed by adding cold methanol−acetone (70:30) solution for 15 min at room temperature, fixing solution is aspired, and wells are air-dried for 5 min and then dehydrated in PBS. Nonspecific binding sites are blocked by incubating wells for 30 min in PBS containing 5% (w/v) FBS 0.05% Tween 20. Wells are then incubated for 1 h at room temperature in PBS containing anti-PAR mouse monoclonal antibody diluted 1:200 in blocking solution. After three washes in PBS, wells incubate in PBS (w/v) 5% FBS 0.05% Tween 20 containing 2 μg/mL Cy2-conjugated Goat anti-mouse secondary antibody and 1 μg/mL DAPI. After washing further three times in PBS, cellular PAR immunoreactivity is assessed.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: Balb, Nu/Nu mice
  • Formulation: 10% Tween 80 in 5% dextrose
  • Dosages: 10 mg/kg
  • Administration: i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 24 mg/mL warmed (60.69 mM)
Ethanol 5 mg/mL warmed (12.64 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 395.42
Formula

C20H24F3N3O2

CAS No. 1262417-51-5
Storage powder
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID