NVP-AUY922 | CAS:747412-49-3

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Name:NVP-AUY922; Luminespib; AUY922; VER-52296
Cat. No. :CS-0136
CAS No. :747412-49-3
Formula:C26H31N3O5
M. Wt. : 465.54
Solubility:DMSO: ≥ 62 mg/mL

NVP-AUY922 is a highly potent HSP90 inhibitor with IC50 of 13 nM/21 nM for for HSP90α/β, respectively, and has weaker potency against the HSP90 family members GRP94 and TRAP-1.IC50 & Target: IC50: 13 nM (HSP90α), 21 nM (HSP90β)In Vitro: AUY922 significantly attenuates changes in immunophenotype and signal transducer and activator of transcription 3 (STAT3) signaling induced by CD40L-fibroblast co-culture but has no effect on the viability of CLL cells. AUY922 in combination with fludarabine is significantly more effective at inducing apoptosis in cells in co-culture than either drug alone, an effect that is irrespective of ATM/TP53 dysfunction[1]. NVP-AUY922 binds to the NH2-terminal nucleotide site in HSP90. NVP-AUY922 inhibits HSP90 family members GRP94 and TRAP-1 with IC50 values of 535 nM and 85 nM, respectively. NVP-AUY922 induces marked accumulation in either GEC1 or G1 plus G2-M phases in most cell lines[2]. NVP-AUY922 shows great inhibition of pancreatic cancer cells with IC50 of at 10 nM. VP-AUY922 (10 nM for 20 h) reduces the expression and the epidermal growth factor (EGF)-mediated (40 ng/mL) activation of EGFR and substantially disrupts EGF signaling in terms of diminishing downstream phosphorylation of ERKThr202/Tyr204. NVP-AUY922 (10 nM) significantly blocks pancreatic cancer cell migration and invasion both in the absence and presence of EGF[3]. In Vivo: NVP-AUY922 (50, 75 mg/kg, i.p.) significantly inhibits tumor growth rate, reducing the mean weights of tumors on day 11[2]. NVP-AUY922 (50 mg/kg/week, 3×25 mg/kg/week) significantly reduces tumor growth rates and lowers tumor weights in the L3.6pl pancreatic cancer cell-bearing mice model[3].

Moser C, et al. 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, et al. 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 J Eccles, Suzanne A., et al. NVP-AUY922: A Novel Heat Shock Protein 90 Inhibitor Active against Xenograft Tumor Growth, Angiogenesis, and Metastasis. Cancer Research (2008), 68(8), 2850-2860.