| Identification | Back Directory | [Name]
8]naphthyridin-6(5H)-one | [CAS]
53439-81-9 | [Synonyms]
XU1
benzo[c][1
8]naphthyridin-6(5H)-one
benzo[c][1,8]naphthyridin-6(5h)-one | [Molecular Formula]
C12H8N2O | [MDL Number]
MFCD12828371 | [MOL File]
53439-81-9.mol | [Molecular Weight]
196.2 |
| Hazard Information | Back Directory | [Description]
XU1 is a potent and selective pan Aurora inhibitor; Phosphorylation of histone H3 (pHH3) inhibitor. | [Uses]
Benzo[c][1,8]naphthyridin-6(5H)-one exhibits low micromolar affinity to human adenosine receptor (AR) A1 and hA2A, with Ki of 4.6 and 4.8 μM. Benzo[c][1,8]naphthyridin-6(5H)-one is inhibitor for poly ADP-ribose polymerase-1 (PARP-1) and aurora kinase A, with IC50 of 0.311 and 5.5 μM[1][2][3]. | [IC 50]
PARP-1: 0.311 μM (IC50); Aurora A: 5.5 μM (IC50); hA1AR: 4.6 μM (Ki); hA2AAR: 4.8 μM (Ki) | [References]
[1] van der Horst E, et al., Multi-objective evolutionary design of adenosine receptor ligands. J Chem Inf Model. 2012 Jul 23;52(7):1713-21. DOI:10.1021/ci2005115
[2] Ferraris D, et al., Design and synthesis of poly ADP-ribose polymerase-1 inhibitors. 2. Biological evaluation of aza-5[H]-phenanthridin-6-ones as potent, aqueous-soluble compounds for the treatment of ischemic injuries. J Med Chem. 2003 Jul 3;46(14):3138-51. DOI:10.1021/jm030109s
[3] Karra S, et al., SAR and evaluation of novel 5H-benzo[c][1,8]naphthyridin-6-one analogs as Aurora kinase inhibitors. Bioorg Med Chem Lett. 2013 May 15;23(10):3081-7. DOI:10.1016/j.bmcl.2013.03.008 |
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| Company Name: |
AstaTech, Inc
|
| Tel: |
(215) 785 3197 |
| Website: |
www.astatechinc.com |
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