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

KU-0060648 

Cat. No.: HY-13431
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 Stock
1 mg   Get quote  
5 mg   Get quote  

* Please select Quantity before adding items.

Top Publications Citing Use of Products
  • 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)

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].

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].

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.

881375-00-4

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

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
KU-0060648
Cat. No.:
HY-13431
Quantity: