Biological Activity:

NVP-AUY922 has excellent potency against HSP90 in a fluorescence polarisation binding assay with an IC50 of 21 nmol/L against the I2-isoform and of 13 nmol/L for the I¡Ó-isoform. The IC50 for HCT116 cell is 16nmol/L[1]. ITC demonstrated a very high binding affinity to HSP90I2 with a Kd of 1.7A¡Ó0.5nmol/L[3]. The IC50 values for NVP-AUY922 against the HSP90 family members GRP94 and TRAP-1 were 535 A¡Ó51 nmol/L (Ki = 108 nmol/L) and 85A¡Ó8 nmol/L (Ki = 53 nmol/L), respectively, indicating weaker potency than for HSP90. The fluorescence polarization IC50 for binding to HSP90 in human cell lysates was in the range of 6.0A¡Ó1.8 to 13.7 A¡Ó1.4 with no clear differences between tumor cells (HCT116 and WM266.4) and nontumorigenic cells (HUVEC and PNT2 prostate epithelial cells)

Technical Data:
M.Wt: 465.54
Formula: C26H31N3O5
Solubility: Soluble in DMSO at 10 mM
Purity: >99%
Storage: Storage at -20C 2 years
CAS No: 747412-49-3 
 
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