Successful, we will reply to you quickly.OK
Please select the quantity.OK
Your message is being sent, please wait.Close
Send mail failed, please send again!Close
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.
AT13387 is a selective potent Hsp90 inhibitor with IC50 of 18 nM in A375 cells, displays a long duration of anti-tumor activity.
BIIB021(CNF2024) is an orally available, fully synthetic small-molecule inhibitor of HSP90 with Ki and EC50 of 1.7 nM and 38 nM, respectively.
Celastrol(Tripterin) is a potent antioxidant and anti-inflammatory agent; It is a novel HSP90 inhibitor.
Dimethylenastron is an Eg5 inhibitor, which arrests cells with monopolar spindles to which all chromosomes attach in a syntelic manner.
Ganetespib(STA-9090) is a unique triazolone-containing Hsp90 inhibitor with an IC50 of 4 nM in OSA 8 cells.
Geldanamycin is a natural existing HSP90 inhibitor with Kd of 1.2 (mu)M.
ML346 is a novel activator of Hsp70 with EC50 of 4600 nM in HeLa cell toxicity assay.
NVP-BEP800(VER82576) is a novel, fully synthetic, oral Hsp90 inhibitor with an IC50 of 0.058 (plusmn) 0.006 (mu)M.
NVP-HSP990(HSP990) is an orally bioavailable inhibitor of Hsp90(IC50=13 nM; Hsp90(alpha)) with potential antineoplastic activity.
PU-WS13 is a potent, Grp94-specific Hsp90 inhibitor of the purine scaffold class.