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

KU-0060648 

Cat. No.: HY-13431 Purity: 99.39%
Handling Instructions

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

Size Price Stock Quantity
5 mg USD 480 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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)

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].

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].

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.
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)

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 --- --- ---
10 mM --- --- ---
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are available by MCE.
References
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Product Name:
KU-0060648
Cat. No.:
HY-13431
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