Products

Enzymes for Research, Diagnostic and Industrial Use

AS703026

Cat No.
CEI-0153
Description
As a novel, selective, orally bioavailable inhibitor, AS703026 can inhibit MEK1/2 with IC50 of with IC50 of 5-11 nM.
Alias
MSC1936369B
CAS No.
1236699-92-5
Molecular Weight
431.2
Purity
>99%
Storage
2 years at -20 centigrade
Synonyms
MSC1936369B
Targets
MEK1/2
Molecular Formula
C15H15FIN3O3
Chemical Name
(S)-N-(2,3-dihydroxypropyl)-3-(2-fluoro-4-iodophenylamino)isonicotinamide
Solubility
DSMO 86 mg/mL Water
In vitro
As a novel, selective, orally bioavailable inhibitor, AS703026 can inhibit MEK1/2 with IC50 of with IC50 of 5-11 nM. For cell lines, (1)AS703026 effectively inhibited the growth of D-MUT cells in vitro and in vivo by specific inhibition of the key MEK downstream target kinase ERK. Inhibition of MEK by AS703026 suppressed cetuximab-resistant colorectal cancer cells attributed to K-ras mutation both in vitro and in vivo. (2)AS703026 also inhibit growth and survival of MM (human multiple myeloma) cells and cytokine-induced osteoclast differentiation more potently (9- to 10-fold) than AZD6244. Inhibition of proliferation induced by AS703026 was mediated by G0-G1 cell cycle arrest and was accompanied by reduction of MAF oncogene expression. AS703026 further induced apoptosis via caspase 3 and Poly ADP ribose polymerase (PARP) cleavage in MM cells, both in the presence or absence of bone marrow stromal cells (BMSCs).
In vivo
AS703026 sensitized MM cells to a broad spectrum of conventional (dexamethasone, melphalan), novel or emerging (lenalidomide, perifosine, bortezomib, rapamycin) anti-MM therapies. Significant tumour growth reduction in AS703026- vs. vehicle-treated mice bearing H929 MM xenograft tumours correlated with downregulated pERK1/2, induced PARP cleavage, and decreased microvessels in vivo. AS703026, at the concentration less than 200 nM, was cytotoxic against the majority of tumour cells tested from patients with relapsed and refractory MM, regardless of mutational status of RAS and BRAF genes.
Download Datasheet:



Inquiry
Realted Products
Catalog
ProductName
EC No.
CAS No.
Source
Price
CatalogCEI-0146
ProductNameTAK-733
EC No.
CAS No.1035555-63-5
Source
CatalogCEI-0147
ProductNameAZD8330
EC No.
CAS No.869357-68-6
Source
CatalogCEI-0155
ProductNamePD318088
EC No.
CAS No.391210-00-7
Source
CatalogCEI-0168
EC No.
CAS No.212631-79-3
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: