NMS-P118
NMS-P118 Basic information
- Product Name:
- NMS-P118
- Synonyms:
-
- 2-(1-(4,4-difluorocyclohexyl)piperidin-4-yl)-6-fluoro-3-oxoisoindoline-4-carboxamide
- NMS-P118
- 2-[1-(4,4-Difluorocyclohexyl)-4-piperidinyl]-6-fluoro-2,3-dihydro-3-oxo-1H-isoindole-4-carboxamide
- NMS-P118; NMS-P 118; NMS P118
- 2-[1-(4,4-difluorocyclohexyl)-piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide
- CS-2354
- 1H-Isoindole-4-carboxamide, 2-[1-(4,4-difluorocyclohexyl)-4-piperidinyl]-6-fluoro-2,3-dihydro-3-oxo-
- NMS-P118,inhibit,NMS P118,PARP,NMSP118,Inhibitor,poly ADP ribose polymerase,NMS-P-118
- CAS:
- 1262417-51-5
- MF:
- C20H24F3N3O2
- MW:
- 395.42
- Mol File:
- 1262417-51-5.mol
NMS-P118 Chemical Properties
- storage temp.
- Store at -20°C
- solubility
- DMF: 5 mg/ml; DMSO: 2 mg/ml; Ethanol: slightly soluble
- form
- A crystalline solid
- color
- White to off-white
- InChI
- InChI=1S/C20H24F3N3O2/c21-13-9-12-11-26(19(28)17(12)16(10-13)18(24)27)15-3-7-25(8-4-15)14-1-5-20(22,23)6-2-14/h9-10,14-15H,1-8,11H2,(H2,24,27)
- InChIKey
- ARYVAQSYRLZVQD-UHFFFAOYSA-N
- SMILES
- C1C2=C(C(C(N)=O)=CC(F)=C2)C(=O)N1C1CCN(C2CCC(F)(F)CC2)CC1
NMS-P118 Usage And Synthesis
Uses
2-[1-(4,4-Difluorocyclohexyl)-4-piperidinyl]-6-fluoro-2,3-dihydro-3-oxo-1H-isoindole-4-carboxamide is a nuclear protein poly(ADP-ribose) polymerase-1 (PARP-1) inhibitor. PARP-1 is involved with the signaling and repair of DNA and a target in oncology.
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].
IC 50
PARP-1: 9 nM (Kd); PARP-2: 1390 nM (Kd)
NMS-P118Supplier
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- 021-20986266 18019349802
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- sales@boylechem.com
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- +86-21-20908456
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