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KU-0060648
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C33H34N4O4S
- MW: 582.71
Description
Potent and selective inhibitor of DNA-dependent protein kinase (DNA-PK), (IC50 = 8.6 nM); with 20-1000 fold selectivity for DNA-PK over other PIKKs and a panel of 60 kinases.
* The 3HCl salt of KU-0060648 (Axon 1584) used to be available as well, but was discontinued (Autumn 2016)
More Information
| Parent CAS No. | 881375-00-4 |
|---|---|
| Chemical Name | 2-(4-Ethyl-piperazin-1-yl)-N-[4-(2-morpholin-4-yl-4-oxo-4H-chromen-8-yl)-dibenzothiophen-1-yl]-acetamide |
| SMILES | C12C3C=CC=CC=3SC=1C(C1C3OC(N4CCOCC4)=CC(=O)C=3C=CC=1)=CC=C2NC(=O)CN1CCN(CC)CC1 |
| MFCD | MFCD18089827 |
| InChi | InChI=1S/C33H34N4O4S/c1-2-35-12-14-36(15-13-35)21-29(39)34-26-11-10-23(33-31(26)25-6-3-4-9-28(25)42-33)22-7-5-8-24-27(38)20-30(41-32(22)24)37-16-18-40-19-17-37/h3-11,20H,2,12-19,21H2,1H3,(H,34,39) |
| InChiKey | AATCBLYHOUOCTO-UHFFFAOYSA-N |
| CID | 11964036 |
| Short Description | DNA-PK inhibitor |
References
- C Cano et al. 1-substituted (Dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-ones endowed with dual DNA-PK/PI3-K inhibitory activity. J Med Chem. 2013 Aug 22;56(16):6386-401.
- J Bardos et al. Radio- and chemosensitization through inhibition of DNA-PK by KU-0060648. Mol. Cancer Ther. 2009, 8(12 Suppl), A116.
- F Dumont et al. Radiosensitising agents for the radiotherapy of cancer: novel molecularly targeted approaches. Expert Opin. Ther. Pat. 2009, 19(6), 775-799.
- JM Munck et al. Chemosensitization of cancer cells by KU-0060648, a dual inhibitor of DNA-PK and PI-3K. Mol Cancer Ther. 2012 Aug;11(8):1789-98.
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