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N-(3-Chlorophenyl)-3-(1-oxo-4-phenylphthalazin-2(1H)-yl)propanamide

Names

[ CAS No. ]:
836640-15-4

[ Name ]:
N-(3-Chlorophenyl)-3-(1-oxo-4-phenylphthalazin-2(1H)-yl)propanamide

Biological Activity

[Description]:

PARP1-IN-8 (compound 11c) is a potent and BBB-penetrated PARP1 inhibitor, with an IC50 of 97 nM. PARP1-IN-8 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Epigenetics >> PARP
Signaling Pathways >> Cell Cycle/DNA Damage >> PARP

[Target]

PARP-1:97 nM (IC50)


[In Vitro]

PARP1-IN-8 (compound 11c) (0-10 μM, 24-48 h) shows significantly potent anti-proliferative activity against A549 cells[1]. Cell Proliferation Assay Cell Line: A549, HFF cells[1] Concentration: 0, 0.1, 1, 10 μM Incubation Time: 24, 48 h Result: Showed significantly potent anti-proliferative activity against A549 cells, and didn’t display any significant cytotoxicity on HFF cells[1].

[References]

[1]. Almahli H, Hadchity E, Jaballah MY, Daher R, Ghabbour HA, Kabil MM, Al-Shakliah NS, Eldehna WM. Development of novel synthesized phthalazinone-based PARP-1 inhibitors with apoptosis inducing mechanism in lung cancer. Bioorg Chem. 2018 Apr;77:443-456.

Chemical & Physical Properties

[ Molecular Formula ]:
C23H18ClN3O2

[ Molecular Weight ]:
403.86

Related Compounds