Products

Enzymes for Research, Diagnostic and Industrial Use

KU-0060648

Cat No.
CEI-0936
Description
KU-0060648 is a dual inhibitor of DNA-PK and PI3Kα, PI3Kβ, PI3Kδ with IC50 of 8.6 nM and 4 nM, 0.5 nM, 0.1 nM respectively, less inhibition of PI3Kγ with IC50 of 0.59 μM.
CAS No.
881375-00-4
Molecular Weight
582.71
Storage
2 years -20 centigrade Powder; 2 weeks 4 centigrade in DMSO; 6 months -80 centigrade in DMSO.
Targets
DNA-PK, PI3Kα, PI3Kβ, PI3Kδ
IC50
8.6 nM; 4 nM; 0.5 nM; 0.1 nM
Molecular Formula
C33H34N4O4S
Chemical Name
1-Piperazineacetamide, 4-ethyl-N-[4-[2-(4-morpholinyl)-4-oxo-4H-1-benzopyran-8-yl]-1-dibenzothienyl]-
Solubility
DMSO 0.4 mg/mL; Water <1 mg/mL; Ethanol <1 mg/mL
In vitro
KU-0060648 exhibits differential effects on growth inhibition, but is not profoundly cytotoxic in a panel of human cancer cell lines. It inhibits DNA-PK and PI-3K with greater potency in MCF7 than SW620 cell using cell-based assays. Five-day exposure to 1 mM KU-0060648 inhibits cell proliferation by more than 95% in MCF7 cells but only by 55% in SW620 cells. In clonogenic survival assays, KU-0060648 increases the cytotoxicity of etoposide and doxorubicin across the panel of DNA-PKcs-proficient cells, but not in DNA-PKcs-deficient cells, confirming that enhanced cytotoxicity of the topoisomerase II poisons etoposide and doxorubicin is due to DNA-PK inhibition.
In vivo
KU-0060648 enhances the anti-tumour activity of etoposide in both MCF7 and SW620 xenograft models, and has single-agent activity in the MCF7 xenograft model.
Download Datasheet:



Inquiry
Realted Products
Catalog
ProductName
EC No.
CAS No.
Source
Price
CatalogCEI-0091
ProductNamePIK-90
EC No.
CAS No.677338-12-4
Source
CatalogCEI-0093
ProductNamePKI-402
EC No.
CAS No.1173204-81-3
Source
CatalogCEI-0094
ProductNameYM201636
EC No.
CAS No.371942-69-7
Source
CatalogCEI-0099
ProductName3-Methyladenine
EC No.
CAS No.5142-23-4
Source
+ See More >>
Online Inquiry
Name:
*Phone:
*E-mail Address:
Country:
Company/Institution:
*Products or Services Interested:
Quantity:
Project Description:
Our Products are Not Intended for Private Therapeutic Use!
*Verification Code:
Please input "enzymes"(case insensitive) as verification code.

Welcome! For price inquiries, please feel free to contact us through the form below through the form on the left side. We will get back to you as soon as possible.

Sitemap  Privacy Policy
Copyright ©2011 - 2017 Creative Enzymes.
Contact Us 45-1 Ramsey Road, Shirley, NY 11967, USA
Email: info@creative-enzymes.com
Tel: 1-631-562-8517 1-631-448-7888
Fax: 1-631-938-8127
Distributors To view the contact information for a specific location, select the desired country: