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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
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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
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Hazard statements

H301Toxic if swalloed

Precautionary statements

P301+P310IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML1257
Product name
KU-0060648
Purity
≥98% (HPLC)
Packaging
5 mg
Price
$178
Updated
2025/07/31
Sigma-Aldrich
Product number
SML1257
Product name
KU-0060648
Purity
≥98% (HPLC)
Packaging
25 mg
Price
$712
Updated
2025/07/31
Cayman Chemical
Product number
15344
Product name
Ku-0060648
Purity
≥98%
Packaging
1mg
Price
$37
Updated
2024/03/01
Cayman Chemical
Product number
15344
Product name
Ku-0060648
Purity
≥98%
Packaging
5mg
Price
$142
Updated
2024/03/01
Cayman Chemical
Product number
15344
Product name
Ku-0060648
Purity
≥98%
Packaging
10mg
Price
$266
Updated
2024/03/01
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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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KU 0060648 Suppliers

China 104 United Kingdom 1 United States 12 Global 117
Tocris Bioscience
Tel
--
Fax
--
Email
customerservice@tocris.co.uk
Country
United Kingdom
ProdList
5726
Advantage
77

881375-00-4, KU 0060648Related Search:

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  • 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
  • KU 0060648 trihydrochloride
  • CS-768
  • KU0060648;KU 0060648
  • KU 0060648
  • ku-0060648
  • KU 0060648 USP/EP/BP
  • 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
  • 2-(4-Ethylpiperazin-1-yl)-N-(4-(2-morpholino-4-oxo-4H-chromen-8-yl)dibenzo[b,d]thiophen-1-yl)acetamide , KU-0060648
  • KU-0060648 ，S8045
  • 881375-00-4
  • Akt
  • mTOR
  • PI3K