1. Cell Cycle/DNA Damage
    Metabolic Enzyme/Protease
    Autophagy
  2. HSP
    Autophagy

NVP-AUY922 (Synonyms: Luminespib; AUY922; VER-52296; NVP-AUY 922; AUY-922; VER 52296; VER52296)

Cat. No.: HY-10215 Purity: 98.17%
Data Sheet SDS Handling Instructions

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.

For research use only. We do not sell to patients.
NVP-AUY922 Chemical Structure

NVP-AUY922 Chemical Structure

CAS No. : 747412-49-3

Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO $55 In-stock
5 mg $50 In-stock
10 mg $70 In-stock
25 mg $140 In-stock
100 mg $350 In-stock
200 mg $600 In-stock
500 mg $1100 In-stock
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Description

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].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT01854034 Massachusetts General Hospital Non Small Cell Lung Cancer July 2013 Phase 2
NCT01668173 Memorial Sloan Kettering Cancer Center|Novartis Myeloproliferative Neoplasms August 2012 Phase 2
NCT01485536 M.D. Anderson Cancer Center|Novartis Lymphoma August 2012 Phase 2
NCT01484860 University Health Network, Toronto|Novartis Pharmaceuticals Adenocarcinoma of the Pancreas|Metastatic Disease January 2012 Phase 2
NCT01389583 National Health Research Institutes, Taiwan|National Taiwan University Hospital|Taipei Veterans General Hospital, Taiwan|Mackay Memorial Hospital|Taichung Veterans General Hospital|China Medical University Hospital|National Cheng-Kung University Hospital|Chang Gung Memorial Hospital Gastrointestinal Stromal Tumor October 2011 Phase 2
NCT01602627 Dale Shepard, MD, PhD|National Cancer Institute (NCI)|Case Comprehensive Cancer Center Unspecified Adult Solid Tumor, Protocol Specific September 2011 Phase 1
NCT01361945 Texas Tech University Health Sciences Center, El Paso Breast Cancer|Metastatic Breast Cancer|HER-2 Positive Breast Cancer|ER Positive Breast Cancer July 2011 Phase 1|Phase 2
NCT00526045 Novartis Pharmaceuticals|Novartis Breast Cancer|Hematologic Neoplasms July 2007 Phase 1|Phase 2
NCT01402401 Novartis Pharmaceuticals|Novartis Advanced Gastric Cancer November 2011 Phase 2
NCT00708292 Novartis Pharmaceuticals|Novartis Relapsed or Refractory Multiple Myeloma July 2008 Phase 1|Phase 2
NCT01404650 SCRI Development Innovations, LLC|Novartis Gastrointestinal Stromal Tumor December 2011 Phase 2
NCT01294826 Swedish Medical Center|Novartis Pharmaceuticals Recurrent Colon Cancer|Recurrent Rectal Cancer|Stage IV Colon Cancer|Stage IV Rectal Cancer|Adenocarcinoma of the Colon|Adenocarcinoma of the Rectum February 2011 Phase 1
NCT01613950 Novartis Pharmaceuticals|Novartis Stomach Neoplasms Esophageal Neoplasms Metastatic Gastric Cancer Mutated PI3KCA Protein Overexpressed HER2 Protein December 2012 Phase 1
NCT01132625 Novartis Pharmaceuticals|Novartis Advanced Solid Tumors November 2008 Phase 1
NCT01752400 Massachusetts General Hospital Non Small Cell Lung Cancer January 2013 Phase 2
NCT01271920 Novartis Pharmaceuticals|Novartis Advanced HER2-positive Breast Cancer September 2010 Phase 2
NCT01124864 Novartis Pharmaceuticals|Novartis Non-small-cell Lung Cancer October 2010 Phase 2
NCT01772797 Novartis Pharmaceuticals|Novartis Anaplastic Lymphoma Kinase (ALK)|Non-small Cell Lung Cancer June 2013 Phase 1
NCT01922583 National Taiwan University Hospital Non-small Cell Lung Cancer (NSCLC) January 2014 Phase 2
NCT01784640 Jonsson Comprehensive Cancer Center|National Cancer Institute (NCI) Recurrent Non-small Cell Lung Cancer|Squamous Cell Lung Cancer|Stage IV Non-small Cell Lung Cancer January 2014 Phase 1
NCT01646125 Novartis Pharmaceuticals|Novartis Advanced Non Small Cell Lung Cancer (NSCLC) November 2012 Phase 2
NCT01084330 Novartis Pharmaceuticals|Novartis Advanced Gastric Cancer|Gastro-esophageal Junction Cancer April 2010 Phase 2
NCT01259089 Northwestern University|Robert H. Lurie Cancer Center Adenocarcinoma of the Lung|Non-small Cell Lung Cancer March 2011 Phase 1|Phase 2
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 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
Cell Assay
[2]

Cell lines are grown in DMEM/10% FCS, 2 mM glutamine, and nonessential amino acids in a humidified atmosphere of 5% CO2 in air as described. All lines are free of Mycoplasma. Cell proliferation is determined using the sulforhodamine B (SRB) assay for tumor cells and prostate epithelial cells, the WST-1 assay for MCF10A and HB119, or an alkaline phosphatase assay for HUVEC and HDMEC. GI50 is the compound concentration inhibiting cell proliferation by 50% compared with vehicle controls. Cell cycle analysis is as described. Active caspase-3/7 is measured using a homogenous caspase assay kit.

Animal Administration
[2]

NVP-AUY922 is dissolved in DMSO and diluted in sterile saline/Tween 20.

For efficacy studies, human tumor xenografts are established s.c. in athymic mice. WM266.4 cells are also injected i.v. to generate experimental lung metastases and PC3LN3 prostate carcinoma cells are implanted into the prostates of male mice. Dosing with NVP-AUY922 commences when tumors are well established using schedules described. Tumor growth is monitored and at study end samples are harvested for analysis.

References
M.Wt

465.54

Formula

C₂₆H₃₁N₃O₅

CAS No.

747412-49-3

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 62 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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NVP-AUY922
Cat. No.:
HY-10215
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