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Products are for research use only. Not for human use. We do not sell to patients.
(Luminespib; AUY922; VER-52296; NVP-AUY 922; AUY-922; VER 52296; VER52296)
NVP-AUY922 Chemical Structure
|Product name: NVP-AUY922|
|Cat. No.: HY-10215|
AUY922 (NVP-AUY922) is a highly potent HSP90 inhibitor for HSP90α/β with IC50 of 13 nM /21 nM, weaker potency against the HSP90 family members GRP94 and TRAP-1.
IC50 Value: 13 nM(HSP90α); 21 nM(HSP90β)
in vitro: NVP-AUY922 inhibits proliferation of various human cancer cell lines in vitro, with an average GI50 of 9 nM.  The IC50 values of NVP-AUY922 fall in the range of 2 to 40 nM in these gastric cancer cell lines. IC50 value for the BEAS-2B cells is 28.49 nM. Treatment with NVP-AUY922 does not influence the expression of HSP90, but expression of HSP70 gets elevated by NVP-AUY922 treatment. NVP-AUY922 increases the binding of HSP70 to HSP90. NVP-AUY922 causes p23 dissociation from the HSP90 complex and can then recruit HSP70 to the HSP90 complex.
in vivo: Treatment with NVP-AUY922 causes a robust antitumor response and inhibits p-Akt and VEGF expression in an HSC-2 xenograft model. In BT474, NVP-AUY922 shows complete loss of ERBB2 and substantial depletion of ERα, in addition to reductions in CDK4 and phospho-ERK1/2.
|M.Wt||465.54||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
|1 mg||5 mg||10 mg|
|1 mM||2.1480 mL||10.7402 mL||21.4804 mL|
|5 mM||0.4296 mL||2.1480 mL||4.2961 mL|
|10 mM||0.2148 mL||1.0740 mL||2.1480 mL|
. Monazzam, Azita; Razifar, Pasha; Evaluation of the Hsp90 inhibitor NVP-AUY922 in multicellular tumour spheroids with respect to effects on growth and PET tracer uptake. Nuclear Medicine and Biology (2009), 36(3), 335-342.
. Eccles, Suzanne A.; Massey, Andy; Raynaud, Florence I.; NVP-AUY922: A Novel Heat Shock Protein 90 Inhibitor Active against Xenograft Tumor Growth, Angiogenesis, and Metastasis. Cancer Research (2008), 68(8), 2850-2860.
. Moser C, Lang SA, Hackl C, Wagner C, Scheiffert E, Schlitt HJ, Geissler EK, Stoeltzing O.Targeting HSP90 by the novel inhibitor NVP-AUY922 reduces growth and angiogenesis of pancreatic cancer.Anticancer Res. 2012 Jul;32(7):2551-61.
. Best OG, Mulligan SP.Heat shock protein-90 inhibitor, NVP-AUY922, is effective in combination with fludarabine against chronic lymphocytic leukemia cells cultured on CD40L-stromal layer and inhibits their activated/proliferative phenotype.Leuk Lymphoma. 2012 Jul 9.
. Walsby E, Pearce L, Burnett AK, Fegan C, Pepper C.The Hsp90 inhibitor NVP-AUY922-AG inhibits NF-κB signaling, overcomes microenvironmental cytoprotection and is highly synergistic with fludarabine in primary CLL cells.Oncotarget. 2012 May;3(5):525-34.
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