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KU-0060648

Cat. No. M2798
KU-0060648 Structure
Size Price Availability Quantity
5mg USD 150  USD150 In stock
10mg USD 250  USD250 In stock
25mg USD 550  USD550 In stock
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Quality Control & Documentation
Biological Activity

KU-0060648 is a dual inhibitor of DNA-PK and PI3Kα, PI3Kβ, PI3Kδ with IC50 of 8.6 nM and 4 nM, 0.5 nM, 0.1 nM respectively, less inhibition of PI3Kγ with IC50 of 0.59 μM.

Chemical Information
Molecular Weight 582.71
Formula C33H34N4O4S
CAS Number 881375-00-4
Solubility (25°C) DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Valentina Perini, et al. PARP Inhibitor Olaparib Causes No Potentiation of the Bleomycin Effect in VERO Cells, Even in the Presence of Pooled ATM, DNA-PK, and LigIV Inhibitors

[2] Mintao Mao, et al. Feedback autophagy activation as a key resistance factor of Ku-0060648 in colorectal cancer cells

[3] Min-Bin Chen, et al. KU-0060648 inhibits hepatocellular carcinoma cells through DNA-PKcs-dependent and DNA-PKcs-independent mechanisms

[4] Francis Robert, et al. Pharmacological inhibition of DNA-PK stimulates Cas9-mediated genome editing

[5] Joanne M Munck, et al. Chemosensitization of cancer cells by KU-0060648, a dual inhibitor of DNA-PK and PI-3K

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Keywords: KU-0060648 supplier, DNA-PK, inhibitors, activators


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