| Identification | Back Directory | [Name]
KU 0060648 | [CAS]
881375-00-4 | [Synonyms]
CS-768
KU 0060648
ku-0060648
KU 0060648 USP/EP/BP
KU0060648;KU 0060648
KU 0060648 trihydrochloride
4-Ethyl-N-[4-[2-(4-morpholinyl)-4-oxo-4H-1-benzopyran-8-yl]-1-dibenzothienyl]-1-piperazineacetamide
1-Piperazineacetamide, 4-ethyl-N-[4-[2-(4-morpholinyl)-4-oxo-4H-1-benzopyran-8-yl]-1-dibenzothienyl]-
2-(4-Ethylpiperazin-1-yl)-N-(4-(2-morpholino-4-oxo-4H-chromen-8-yl)dibenzo[b,d]thiophen-1-yl)acetamide | [Molecular Formula]
C33H35N4O4S | [MDL Number]
MFCD17214218 | [MOL File]
881375-00-4.mol | [Molecular Weight]
583.72 |
| Chemical Properties | Back Directory | [Boiling point ]
819.9±65.0 °C(Predicted) | [density ]
1.337±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Limited solubility, soluble in HCl | [form ]
Powder | [pka]
14.10±0.43(Predicted) | [color ]
Off-white to brown | [InChIKey]
AATCBLYHOUOCTO-UHFFFAOYSA-N | [SMILES]
N1(CC(NC2=C3C4=CC=CC=C4SC3=C(C3=C4OC(N5CCOCC5)=CC(=O)C4=CC=C3)C=C2)=O)CCN(CC)CC1 | [CAS DataBase Reference]
881375-00-4 |
| Hazard Information | Back Directory | [Uses]
KU-0060648 is a dual inhibitor of DNA-PK and PI3Kα, PI3Kβ, PI3Kδ. | [Definition]
ChEBI: 2-(4-ethyl-1-piperazinyl)-N-[4-[2-(4-morpholinyl)-4-oxo-1-benzopyran-8-yl]-1-dibenzothiophenyl]acetamide is a member of dibenzothiophenes. | [Biological Activity]
KU-0060648 is a very potent dual inhibitor of DNA-PK and PI3K. The IC50 values for inhibition of DNA-PK in MCF7 and SW620 cells are 19 and 170 nMrespectively. The compound KU-0060648 inhibits MCF7 PI3K activity with an IC50 of 39 nMbut is inactive against PI3K in SW620suggesting a cell-dependent mechanism of inhibition. KU-0060648 increases sensitivity to DNA damaging cytotoxic drugs such as etoposide and doxorubicin in tumor cell lines expressing DNA-PK. KU-0060648 stimulates Cas9 (CRISPR associated protein 9) mediated genome editing by enhancing the rate of homology directed-repair (HDR) and decreasing the rate of NHEJ (non-homologous end-joining).''KU-0060648 is observed to inhibit proliferation and initiate apoptosis in hepatocellular carcinoma. KU-0060648 is useful in chemotherapy as it increases the efficiency of double stranded breaks initiated by anticancer drugs. | [in vivo]
KU-0060648 (intraperitoneal injection; 10 and 50 mg/kg; once daily; daily for 21 days) dramatically inhibits HepG2 xenograft growth in nude mice, the tumor weights (at week 5) of KU-0060648 group mice are dramatically lighter than that of vehicle control mice and exert a dose-dependent effect in vivo[1]. | Animal Model: | HepG2 xenograft nude mice model[1] | | Dosage: | 10 and 50 mg/kg | | Administration: | Intraperitoneal injection; 10 and 50 mg/kg; once daily; daily for 21 days | | Result: | Suppressed HepG2 xenograft growth in nude mice. |
| [IC 50]
PI3Kα: 4 nM (IC50); PI3Kβ: 0.5 nM (IC50); PI3Kγ: 0.594 μM (IC50); PI3Kδ: 0.1 nM (IC50); DNA-PK: 8.6 nM (IC50) | [storage]
Store at -20°C |
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| Company Name: |
China Langchem Inc.
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| Tel: |
0086-21-58956006 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList19141/0_EN.htm |
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