Art. -Nr.: HY-13431

KU-0060648

4 Cited Publications

Kundenbewertung

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.

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Reinheit: 99.87%
CAS. Nr.: 881375-00-4
Formel: C₃₃H₃₄N₄O₄S
Molecular Weight:582.71

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

KU-0060648 Chemical Structure

CAS. Nr.: 881375-00-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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^[1].

IC₅₀ & Target

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)

Alle PI3K Isoform-spezifische Produkte anzeigen :

Alle mTOR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	>20 μM Compound: 39	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	[PMID: 23855836]
HeLa	EC₅₀	136 nM Compound: 39	Inhibition of DNA-PK autophosphorylation at S2056 in human HeLa cells Inhibition of DNA-PK autophosphorylation at S2056 in human HeLa cells	[PMID: 23855836]
HeLa	IC₅₀	>25 μM Compound: 39	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	[PMID: 23855836]
HeLa	IC₅₀	6 nM Compound: 3	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	[PMID: 21080722]

In Vitro

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.

Cell Proliferation Assay^[1]

Cell Line:

Human breast (MCF7, T47D and MDA-MB-231) and colon (LoVo and SW620) cancer cells
Concentration:

0.1-1 μM
Incubation Time:

5 days
Result:

Resulted in> 50% inhibition of cell growth in all cell lines.

Western Blot Analysis^[2]

Cell Line:

HCC cells; HepG2/Huh-7 cells
Concentration:

100-300 nM
Incubation Time:

12 hours
Result:

Inhibited phosphatidylinositol 3-kinase (PI3K) and in-activates AKT-mTOR signaling.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Chemical Information

CAS. Nr. 881375-00-4
Appearance Solid
Molecular Weight 582.71
Formel C₃₃H₃₄N₄O₄S
Color Off-white to light brown
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

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
Nat Methods

Exonuclease-enhanced prime editors. [Abstract]

2024 Mar;21(3):455-464. PMID: 38302659
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

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7161 mL

8.5806 mL

17.1612 mL

5 mM

---

10 mM

---

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 0.28 mg/mL (0.48 mM); Clear solution

This protocol yields a clear solution of ≥ 0.28 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (2.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

KU-0060648

4 Cited Publications

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KU-0060648

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Antioxidant Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

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Cytoskeleton Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

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Anti-Cancer Metabolism Compound Library

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Angiogenesis-Related Compound Library

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Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Mitochondrial Protection Compound Library

Membrane Protein-targeted Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

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Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) KU-0060648

Alle PI3K Isoform-spezifische Produkte anzeigen

Alle mTOR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

KU-0060648 Related Classifications

HY-13431 Related Classifications