[CAS NO. 1262417-51-5] NMS-P118
PRODUCTS SPECIFICATIONS [1262417-51-5]
DESCRIPTION [1262417-51-5]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 395.42 |
| Molecular Formula | C20H24F3N3O2 |
| SMILES | FC(CC1)(F)CCC1N(CC2)CCC2N(C3=O)CC4=C3C(C(N)=O)=CC(F)=C4 |
1 Publications Citing Use of MCE
Summary
NMS-P118 is a potent, orally available, and highly selective PARP-1 Inhibitor for cancer therapy.
IC50 & Target
|
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 IC 50 : 8.15 μM; CYP-2D6 IC 50 : 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 (K D =0.009 μM) PARP-1 inhibitor, showing 150-fold selectivity over PARP-2 (K D =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.
Appearance
Solid
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
DMSO : 16 mg/mL ( 40.46 mM ; Need ultrasonic and warming)
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 |