NMS-P118

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].

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

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].

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

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].

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