Products

Enzymes for Research, Diagnostic and Industrial Use

BKM120 (NVP-BKM120)

Cat No.
CEI-0119
Description
BKM120 (NVP-BKM120) can inhibit p110-alpha, p110-beta, p110-delta and p110-gamma with IC50 of 52 nM, 166 nM, 166 nM and 262 nM.
CAS No.
944396-07-0
Molecular Weight
410.39
Purity
>99%
Storage
2 years at -20centigrade Powder
Targets
p110-alpha, p110-beta, p110-delta, p110-gamma
Molecular Formula
C18H21F3N6O2
Chemical Name
5-(2,6-dimorpholinopyrimidin-4-yl)-4-(trifluoromethyl)pyridin-2-amine
Solubility
DMSO 82 mg/mL Water
In vitro
2-morpholino pyrimidine derivative pan-PI3K inhibitor, NVP-BKM120, can inhibit all four class I PI3K isoforms with at least 50-fold selectivity against other protein kinases, but does not significantly inhibit the related class III (Vps34) and class IV (mTOR, DNA-PK) PI3K kinases. As a selective PI3K inhibitor, NVP-BKM120 can decreases the cellular levels of p-Akt in mechanistic models and relevant tumor cell lines and block the PI3K/Akt signaling cascade leading to a dose-dependent growth inhibition. BKM120 can cause cell death in various cellular systems, irrespective of their level of PI3K addiction. BKM120 also inhibited microtubule dynamics upon direct binding to tubulin. At 5 to 10-fold the concentration needed to half-maximally inhibit PI3K signaling, BKM120 treatment caused changes in expression of mitotic genes and the induction of a robust G2/M arrest. NVP-BKM120 and p53 There is a relationship between the cell lines sensitivity to NVP-BKM120 and p53 status in glioma cells with different p53 status. Actually, glioma cells containing wild-type p53 are more sensitive to NVP-BKM120 than cells with mutated or deleted p53.NVP-BKM120 showed differential forms of cell death on the basis of p53 status of the cells with p53 wild-type cells undergoing apoptotic cell death and p53 mutant/deleted cells having a mitotic catastrophe cell death.
In vivo
NVP-BKM120 inhibits the PI3K pathway in tumor-bearing animals and displays strong antitumor activity in vivo. Rat1-myr-p110alpha tumor-bearing animals were treated orally, once, at dose levels of either 30 or 60 mg/kg. Maximum inhibition of p-Akt levels in tumor tissue was achieved at the 1 hour time point.
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-0080
ProductNameAS-605240
EC No.
CAS No.648450-29-7
Source
CatalogCEI-0088
ProductNameAS-252424
EC No.
CAS No.900515-16-4
Source
CatalogCEI-0091
ProductNamePIK-90
EC No.
CAS No.677338-12-4
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: