CEP-8983

Names

[ CAS No. ]:
374071-46-2

[ Name ]:
CEP-8983

[Synonym ]:
7-methoxy-1,2,3,11-tetrahydro-5,11-diaza-benzo[a]trindene-4,6-dione
1H-Cyclopenta(a)pyrrolo(3,4-c)carbazole-1,3(2H)-dione,4,5,6,7-tetrahydro-11-methoxy

Biological Activity

[Description]:

CEP-8983 is a PARP-1 and PARP-2 inhibitor (IC50: 20 and 6 nM). CEP-8983 is an effective chemosensitizing agent, and can sensitize chemotherapy-resistant cell lines and subcutaneous xenografts to Temozolomide (HY-17364) and Camptothecin (HY-16560)[1].

[Related Catalog]:

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

[Target]

20 and 6 nM (PARP-1/2)[1].


[References]

[1]. Miknyoczki S, et al. The selective poly(ADP-ribose) polymerase-1(2) inhibitor, CEP-8983, increases the sensitivity of chemoresistant tumor cells to temozolomide and irinotecan but does not potentiate myelotoxicity. Mol Cancer Ther. 2007 Aug;6(8):2290-302.  

Chemical & Physical Properties

[ Molecular Formula ]:
C18H14N2O3

[ Molecular Weight ]:
306.31500

[ Exact Mass ]:
306.10000

[ PSA ]:
74.68000

[ LogP ]:
2.71240

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream