| Identification | Back Directory | [Name]
NMS-P515 | [CAS]
1262395-13-0 | [Synonyms]
NMS-P515
1H-Isoindole-4-carboxamide, 2-(1-cyclohexyl-4-piperidinyl)-2,3-dihydro-1-methyl-3-oxo-, (1S)- | [Molecular Formula]
C21H29N3O2 | [MDL Number]
MFCD32067978 | [MOL File]
1262395-13-0.mol | [Molecular Weight]
355.47 |
| Chemical Properties | Back Directory | [Boiling point ]
513.3±50.0 °C(Predicted) | [density ]
1.200±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
15.80±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
NMS-P515 is a potent inhibitor of PARP-1 both in biochemical (Kd: 0.016 μM) and cellular (IC50: 0.027 μM) assays. | [Uses]
NMS-P515 is a potent, orally active and stereospecific PARP-1 inhibitor, with a Kd of 16 nM and an IC50 of 27 nM (in Hela cells). Anti-tumor activity[1]. | [in vivo]
NMS-P515 (80 mg/kg, orally daily for 12 days) exhibits potent antitumor activity in mouse models based pancreatic cancer[1]. | Animal Model: | Subcutaneously implanted Capan-1 pancreatic (BRCA2-mutated) mouse xenografts[1]. | | Dosage: | 80 mg/kg. | | Administration: | Orally, once daily for 12 days. | | Result: | Clearly reduced the tumor growth (maximal tumor growth inhibition observed: 48%, maximum body weight loss: 6%). |
| [IC 50]
PARP-1: 16 nM (Kd); PARP-1: 27 nM (IC50, in Hela cells) | [storage]
Store at -20°C | [References]
[1] Papeo G, et al. Discovery of Stereospecific PARP-1 Inhibitor Isoindolinone NMS-P515. ACS Med Chem Lett. 2019 Mar 13;10(4):534-538. DOI:10.1021/acsmedchemlett.8b00569 |
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