2. Cell Cycle/DNA Damage PI3K/Akt/mTOR
  3. DNA-PK PI3K mTOR
  4. KU-0060648

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.

KU-0060648 Chemical Structure

KU-0060648 Chemical Structure

CAS No. : 881375-00-4

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1 mg USD 71 In-stock
5 mg USD 130 In-stock
10 mg USD 210 In-stock
25 mg USD 380 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

KU-0060648 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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)

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 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.

KU-0060648 Related Antibodies

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.
Molecular Weight

582.71

Formula

C33H34N4O4S
CAS No.
Appearance

Solid

Color

Off-white to 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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7161 mL 8.5806 mL 17.1612 mL
5 mM --- --- ---
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
References

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
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KU-0060648 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

KU-0060648881375-00-4KU0060648KU 0060648DNA-PKPI3KmTORDNA-dependent protein kinasePhosphoinositide 3-kinaseMammalian target of RapamycinInhibitorinhibitorinhibit

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