KU 0060648
- Product Name
- KU 0060648
- CAS No.
- 881375-00-4
- Chemical Name
- KU 0060648
- Synonyms
- CS-768;ku-0060648;KU 0060648;KU-0060648 ,S8045;KU0060648;KU 0060648;KU 0060648 USP/EP/BP;KU 0060648 trihydrochloride;KU-0060648 DNA-PK inhibitor Axon2604 Axon-2604 KU0060648;2-(4-ethylpiperazin-1-yl)-N-[4-(2-morpholin-4-yl-4-oxochromen-8-yl)dibenzothiophen-1-yl]acetamide;4-Ethyl-N-[4-[2-(4-morpholinyl)-4-oxo-4H-1-benzopyran-8-yl]-1-dibenzothienyl]-1-piperazineacetamide
- CBNumber
- CB12667538
- Molecular Formula
- C33H34N4O4S
- Formula Weight
- 582.71
- MOL File
- 881375-00-4.mol
KU 0060648 Property
- 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
N-Bromosuccinimide Price
- Product number
- SML1257
- Product name
- KU-0060648
- Purity
- ≥98% (HPLC)
- Packaging
- 5 mg
- Price
- $178
- Updated
- 2025/07/31
- Product number
- SML1257
- Product name
- KU-0060648
- Purity
- ≥98% (HPLC)
- Packaging
- 25 mg
- Price
- $712
- Updated
- 2025/07/31
- Product number
- 15344
- Product name
- Ku-0060648
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $37
- Updated
- 2024/03/01
- Product number
- 15344
- Product name
- Ku-0060648
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $142
- Updated
- 2024/03/01
- Product number
- 15344
- Product name
- Ku-0060648
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $266
- Updated
- 2024/03/01
KU 0060648 Chemical Properties,Usage,Production
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 nM, respectively. The compound KU-0060648 inhibits MCF7 PI3K activity with an IC50 of 39 nM, but is inactive against PI3K in SW620, suggesting 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
KU 0060648 Preparation Products And Raw materials
Raw materials
Preparation Products
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