Description
NVP-AUY922 | 27026 | Gentaur US, UK & Europe Disrtribition
Category: Inhibitors / Activators/Other
Application: N/A
Background: Heat shock protein 90 (HSP90) is a molecular chaperone essential for the stability of key regulators of cell growth and survival. HSP90 is involved in protein folding and functions as a chaperone for numerous client proteins, many of which are important in cancer pathogenesis. Hsp90 enables cancer cell survival by maintaining the function of their mutated client proteins including the KIT and PDGFRA proteins. AUY922 inhibits Hsp90, resulting in proteasomal degradation of oncogenic client proteins, inhibition of cell proliferation, and elevation of HSP72 levels in a wide range of human tumor cell lines.
Description: NVP-AUY922 potently inhibits HSP90 with IC50 values of 7.8 nM and 21 nM, and Ki values of 9 nM and 8.2 nM for HSP90α and HSP90β, respectively. NVP-AUY922 shows a very high binding affinity to HSP90β with a Kd of 1.7 nM. NVP-AUY922 inhibits the proliferation of human tumor cells in vitro with GI50 values of approximately 2 to 40 nM, inducing G1-G2 arrest and apoptosis. Human endothelial cells are very sensitive to NVP-AUY922 with GI50s of 2.5-3.9 nM. NVP-AUY922 also exhibits potent antitumor efficacy in human tumor xenografts including BT474 breast, A2780 ovarian, U87MG glioblastoma, PC3 prostate, and WM266.4 melanoma.
Product Type: Inhibitor
Shippement Condition: -20°C
