Products

Enzymes for Research, Diagnostic and Industrial Use

GSK2126458

Cat No.
CEI-0134
Description
GSK2126458 can inhibit p110alpha p110beta,p110gamma, p110delta, mTORC1,mTORC2 with IC50 of 0.019nM, 0.13 nM, 0.024 nM,0.06 nM, 0.18 nM, and 0.3 nM.
CAS No.
1086062-66-9
Molecular Weight
505.5
Purity
>99%
Storage
2 years at -20centigrade Powder
Targets
p110alpha, p110beta, p110gamma, p110delta, mTORC1/mTORC2
Molecular Formula
C25H17F2N5O3S
Chemical Name
2,4-difluoro-N-(2-methoxy-5-(4-(pyridazin-4-yl)quinolin-6-yl)pyridin-3-yl)benzenesulfonamide
Solubility
DMSO 101 mg/mL Water
In vitro
GSK2126458 is an orally available selective inhibitor of the class I phosphoinositide 3-kinase (PI3K) enzymesand MTOR1/2 complexes. GSK2126458 can inhibit PI3K-alpha (p85alpha/p110alpha) with IC50 of 0.04 nM. GSK2126458 has Ki values in the picomolar range for each of the class I PI3K isoforms and MTOR1/2 complexes. GSK2126458 has potent in vitro and in vivo growth-inhibitory effects on cancer cells. In comparison with other clinical PI3K inhibitors, GSK2126458 is around 100-fold more potent than BEZ235 ( 6 nM ). GSK2126458 also a low picomolar inhibitor of the common activating mutants of p110 R ( E542K, E545K, and H1047R ) with Ki of 0.008 nM, 0.008 nM and 0.009 nM in human cancer. In mechanistic cellular assays, GSK2126458 caused a significant reduction in the levels of pAKT-S473 with remarkable potency. Consistent with its activity against both PI3K R and mTOR, GSK2126458 also inhibits phosphorylation of AKT-T308 and p70S6K at low nanomolar concentrations. GSK2126458 induces a G1 cell cycle arrest and inhibits cell proliferation in a large panel of cell lines, including T47D and BT474 breast cancer lines.
Download Datasheet:



Inquiry
Realted Products
Catalog
ProductName
EC No.
CAS No.
Source
Price
CatalogCEI-0078
ProductNameCAY10505
EC No.
CAS No.1218777-13-9
Source
CatalogCEI-0079
ProductNameWYE-687
EC No.
CAS No.1062161-90-3
Source
CatalogCEI-0080
ProductNameAS-605240
EC No.
CAS No.648450-29-7
Source
CatalogCEI-0086
ProductNameWYE-354
EC No.
CAS No.1062169-56-5
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: