KU-0060648
Based on 4 publication(s) in Google Scholar
KU-0060648 is a dual inhibitor of PI3K and DNA-PK with IC50s of 4 nM, 0.5 nM, 0.1 nM, 0.594 nM and 8.6 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ and DNA-PK, respectively.
For research use only. We do not sell to patients.
- Purity: 99.87%
- CAS No.: 881375-00-4
- Formula: C33H34N4O4S
- Molecular Weight:582.71
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) KU-0060648
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Biological Activity
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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) |
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
>20 μM
Compound: 39
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Inhibition of human ERG expressed in cisapride treated CHO cells by Ion Works assay
Inhibition of human ERG expressed in cisapride treated CHO cells by Ion Works assay
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[PMID: 23855836] |
| HeLa | EC50 |
136 nM
Compound: 39
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Inhibition of DNA-PK autophosphorylation at S2056 in human HeLa cells
Inhibition of DNA-PK autophosphorylation at S2056 in human HeLa cells
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[PMID: 23855836] |
| HeLa | IC50 |
>25 μM
Compound: 39
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Antiproliferative activity against human HeLa cells assessed as cell viability after 6 to 8 days by DMR clonogenic assay
Antiproliferative activity against human HeLa cells assessed as cell viability after 6 to 8 days by DMR clonogenic assay
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[PMID: 23855836] |
| HeLa | IC50 |
6 nM
Compound: 3
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Inhibition of DNA-PK isolated from human HeLa cell extract assessed as reduction in p53 Ser15 phosphorylation by chemiluminescence assay
Inhibition of DNA-PK isolated from human HeLa cell extract assessed as reduction in p53 Ser15 phosphorylation by chemiluminescence assay
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[PMID: 21080722] |
KU-0060648 inhibits cellular DNA-PK auto-phosphorylation with IC50 values of 0.019 μM (MCF7 cells) and 0.17 μM (SW620 cells), and PI-3K-mediated AKT phosphorylation with IC50 values of 0.039 μM (MCF7 cells) and >10 μM (SW620 cells)[1]. KU-0060648 (30-500 nM; 72 hours) dose-dependently inhibits HepG2 cell proliferation, IC50=134.32nM[2]. KU-0060648 (0.1-1 μM；5 days) inhibits cell lines growth with GI50s of 0.95 μM, 0.21 μM, 0.27 μM, 0.41 μM and 1 μM in SW620, LoVo, MCF7, T47D and MDA-MB-231 cells[1]. KU-0060648 (100-300 nM;12 hours) significantly inhibits activation of PI3K (p85 phosphorylation), AKT (Ser-473 and Thr-308 phosphorylations) and mTOR (p70S6K1 Thr-389 phosphorylation) in HepG2/Huh-7 lines and primary human HCC cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human breast (MCF7, T47D and MDA-MB-231) and colon (LoVo and SW620) cancer cells
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Concentration:0.1-1 μM
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Incubation Time:5 days
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Result:Resulted in> 50% inhibition of cell growth in all cell lines.
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Cell Line:HCC cells; HepG2/Huh-7 cells
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Concentration:100-300 nM
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Incubation Time:12 hours
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Result:Inhibited phosphatidylinositol 3-kinase (PI3K) and in-activates AKT-mTOR signaling.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:HepG2 xenograft nude mice model[1]
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Dosage:10 and 50 mg/kg
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Administration:Intraperitoneal injection; 10 and 50 mg/kg; once daily; daily for 21 days
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Result:Suppressed HepG2 xenograft growth in nude mice.
Chemical Information
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CAS No. 881375-00-4
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Appearance Solid
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Molecular Weight 582.71
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Formula C33H34N4O4S
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Color Off-white to light brown
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SMILES
O=C(NC1=C(C2=CC=CC=C2S3)C3=C(C4=C5C(C(C=C(N6CCOCC6)O5)=O)=CC=C4)C=C1)CN7CCN(CC)CC7
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (4)
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Journal Impact Factor
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Most Recent
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Nat Biotechnol
Tracking-seq reveals the heterogeneity of off-target effects in CRISPR-Cas9-mediated genome editing. [Abstract]2025 May;43(5):799-810. PMID: 38956324 -
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Int J Mol Sci
CRISPR/Cas9 Ribonucleoprotein Delivery Enhanced by Lipo-Xenopeptide Carriers and Homology-Directed Repair Modulators: Insights from Reporter Cell Lines. [Abstract]2025 May 3;26(9):4361. PMID: 40362595 -
J Cell Mol Med
BNIP3L/BNIP3-Mediated Mitophagy Contributes to the Maintenance of Ovarian Cancer Stem Cells. [Abstract]2025 Oct;29(19):e70704. PMID: 41078116
Solvent & Solubility
DMSO : 2.78 mg/mL (4.77 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.28 mg/mL (0.48 mM); Clear solution
This protocol yields a clear solution of ≥ 0.28 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (2.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.28 mg/mL (0.48 mM); Clear solution
This protocol yields a clear solution of ≥ 0.28 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (2.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (286 KB)
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SDS (420 KB)
- English - EN (420 KB)
- Français - FR (420 KB)
- Deutsch - DE (420 KB)
- Norwegian - NO (420 KB)
- Español - ES (420 KB)
- Swedish - SV (420 KB)
- Italian - IT (420 KB)
- Korean - KR (420 KB)
- Portuguese - PT (420 KB)
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Handling Instructions (2659 KB)
References
[1]. Munck JM, 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. [Content Brief]
[2]. Chen MB, et al. KU-0060648 inhibits hepatocellular carcinoma cells through DNA-PKcs-dependent and DNA-PKcs-independent mechanisms. Oncotarget. 2016 Mar 29;7(13):17047-59. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7161 mL | 8.5806 mL | 17.1612 mL | 42.9030 mL |
KU-0060648 Related Classifications
HY-13431 Related Classifications
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