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17-AAG, Hsp90 inhibitor

Cat No.
CEI-0984
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.
Abbr
17-AAG, Hsp90 inhibitor
Appearance
White to off-white solid.
CAS No.
747412-49-3
Molecular Weight
465.5 Da
Purity
>99%
Stability
Store at or below –20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.
Synonyms
AUY922, VER-52296
Targets
HSP90, HSP90α, HSP90β
IC50
HSP90:7.8 nM and 21 nM
Molecular Formula
C26H31N3O5
Solubility
Soluble in DMSO at 100 mg/ml; soluble in ethanol at 100 mg/ml; very poorly soluble in water; maximum solubility in plain water is estimated to be about 25-50 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility.
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