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Medchemexpress LLC 1H-Isoindole-4-carboxamide, 2-[1-(4,4-difluorocyclohexyl)-4-piperidinyl]-6-fluoro-2,3-dihydro-3-oxo- | 1262417-51-5 | 99.5% | 395.42 | 200 MG

Supplier: Medchemexpress LLC HY18954200MG
NMS-P118 is a potent, orally available, and highly selective PARP-1 inhibitor for cancer therapy. It is for research use only and not sold to patients.
- Potent PARP-1 inhibitor (Kd=0.009 μM) with 150-fold selectivity over PARP-2 (Kd=1.39 μM).
- Less myelotoxic in vitro compared to olaparib.
- Metabolically stable.
- Modestly inhibits CYP-2B6 (IC50: 8.15 μM) and CYP-2D6 (IC50: 9.51 μM) out of eight isoforms tested.
- Possesses excellent pharmacokinetic profile and nearly complete oral bioavailability in mice and rats.
- Highly efficacious in vivo as a single agent in MDA-MB-436 human breast cancer tumors and in combination with temozolomide in CAPAN-1 human pancreatic tumors.
- Well tolerated at highly efficacious doses and has an excellent ADME profile.
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