NVP-AUY922

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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¡ Ó 0.5nmol/ L[ 3] . The IC50 values for NVP-AUY922 against the HSP90 family members GRP94 and TRAP-1 were 535 A¡ Ó 51 nmol/ L ( Ki = 108 nmol/ L) and 85A¡ Ó 8 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¡ Ó 1.8 to 13.7 A¡ Ó 1.4 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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