1. Cell Cycle/DNA Damage
    Epigenetics
  2. PARP
  3. NMS-P118

NMS-P118 

Cat. No.: HY-18954 Purity: 99.80%
Handling Instructions

NMS-P118 is a potent, orally available, and highly selective PARP-1 Inhibitor for cancer therapy.

For research use only. We do not sell to patients.

NMS-P118 Chemical Structure

NMS-P118 Chemical Structure

CAS No. : 1262417-51-5

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10 mM * 1 mL in DMSO USD 125 In-stock
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2 mg USD 84 In-stock
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5 mg USD 144 In-stock
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10 mg USD 252 In-stock
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25 mg USD 540 In-stock
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50 mg USD 972 In-stock
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100 mg USD 1740 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

NMS-P118 is a potent, orally available, and highly selective PARP-1 Inhibitor for cancer therapy.

IC50 & Target[1]

PARP-1

9 nM (Kd)

PARP-2

1390 nM (Kd)

In Vitro

NMS-P118 is found to be less myelotoxic in vitro than olaparib (now marketed as Lynparza), a dual PARP-1/-2 inhibitor. NMS-P118 proves to be metabolically stable, it modestly inhibites two cytochrome P450 family members (CYP-2B6 IC50: 8.15 μM; CYP-2D6 IC50: 9.51 μM) out of eight isoforms tested. Its ability in hampering the proliferation of bone marrow cells is from 5 to > 60 times lower then olaparib according to the species[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

NMS-P118 is a potent (KD=0.009 μM) PARP-1 inhibitor, showing 150-fold selectivity over PARP-2 (KD=1.39 μM). NMS-P118 possesses excellent pharmacokinetic profile and nearly complete oral bioavailability both in mice and rats. It proved to be highly efficacious in vivo both as single agent in MDA-MB-436 human breast cancer tumors and in combination with temozolomide in CAPAN-1 human pancreatic tumors growing as xenografts in the mouse. The compound is well tolerated at highly efficacious doses and is endowed with an excellent ADME profile[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

395.42

Formula

C₂₀H₂₄F₃N₃O₂

CAS No.

1262417-51-5

SMILES

FC(CC1)(F)CCC1N(CC2)CCC2N(C3=O)CC4=C3C(C(N)=O)=CC(F)=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 16 mg/mL (40.46 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5290 mL 12.6448 mL 25.2896 mL
5 mM 0.5058 mL 2.5290 mL 5.0579 mL
10 mM 0.2529 mL 1.2645 mL 2.5290 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

NMS-P118 is profiled on 56 different kinases (ABL, ACK1, AKT1, ALK, AUR1, AUR2, BRK, BUB1, CDC7/DBF4, CDK2/CYCA, CHK1, CK2, EEF2K, EGFR1, ERK2, EphA2, FAK, FGFR1, FLT3, GSK3beta, Haspin, IGFR1, IKK2, IR, JAK1, JAK2, JAK3, KIT, LCK, LYN, MAPKAPK2, MELK, MET, MNK2, MPS1, MST4, NEK6, NIM1, P38alpha, PAK4, POLYDATINGFRb, POLYDATINK1, PERK, PIM1, PIM2, PKAalpha, PKCbeta, PLK1, RET, SULU1, Syk, TLK2, TRKA, TYK2, VEGFR2, ZAP70). The IC50 values are found to be >10 μM for all enzymes tested[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

NMS-P118 is dissolved in DMSO and diluted with appropriate medium before use. Cellular activity of PARP-1 inhibitors is assessed by measuring the inhibition of the hydrogen peroxide induced PAR formation in HeLa cells (ECACC). Cellular PAR levels are measured by immunocytochemistry, and quantified using an ArrayScan vTi instrument[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

The pharmacokinetic profile and the oral bioavailability of the compounds have been investigated in rat in ad hoc pharmacokinetic studies. NMS-P118 is formulated for intravenous bolus administration in 20% DMSO + 40% PEG 400 in 5% dextrose. Oral administration is performed using a NMS-P118 suspension in 0.5% methylcellulose. A single administration at the dose of 10 mg/kg for each route and a single oral administration at the dose of 100 mg/kg are given. Three male animals for each study are used[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

NMS-P118PARPpoly ADP ribose polymeraseInhibitorinhibitorinhibit

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