Free shipping on all orders over $ 500

Luminespib (AUY922)

Cat. No. M1762
Luminespib (AUY922) Structure
Synonym:

NVP-AUY922; Luminespib

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 60  USD60 In stock
5mg USD 50  USD50 In stock
10mg USD 70  USD70 In stock
50mg USD 235  USD235 In stock
100mg USD 390  USD390 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

Luminespib (AUY922) is a small molecule Heat Shock Protein 90 (HSP90) inhibitor with IC50 values of 13 and 21 nM for HSP90α and HSP90β respectively. AUY922 (NVP-AUY922) potently inhibits HSP90 (Kd = 1.7 nmol/L) and proliferation of human tumor cells with GI50 values of approximately 2 to 40 nmol/L, inducing G1-G2 arrest and apoptosis. AUY922 (NVP-AUY922) inhibited proliferation, chemomigration, and tubular differentiation of human endothelial cells and antiangiogenic activity was reflected in reduced microvessel density in tumor xenografts.

Customer Product Validations & Biological Datas
Source PLoS One (2017). Figure 1. AUY922
Method FACS analysis
Cell Lines ATC cells
Concentrations 2.5, 5, 7.5, and 10 μM
Incubation Time 24, 48, and 72 h
Results Taken together, our results demonstrate that AUY922, compared with other hsp90 inhibitors, potently results in growth inhibition and death of ATC cells.
Protocol (for reference only)
Cell Experiment
Cell lines 41 human NSCLC cell lines in vitro: A427, A549, Calu-1, Calu-3, Calu-6, H23, H226, H358, H460, H520, H522, H596, H810, H838, H1155, H1299, H1385, H1435, H1437, H1563, H1568, H1581, H1651, H1703, H1755, H1793, H1836, H1944, H1975, H2030, H2073, H2106, H2110, H2135, H2172, H2228, H2286, H2342, H2405, HCC827, and SHP77
Preparation method Proliferation assays
Cells were seeded in duplicate at 5,000-10,000 cells per well. The day after plating (day 1), NVP-AUY922 was added at 1 µM and 2-fold dilutions over 12 concentrations. Data were compared to untreated controls. Cells were counted on the day drug was added and five days later and these two counts were compared. Cells were harvested by trypsinization and counted immediately using a Coulter Z2 particle counter (Beckman Coulter Inc, Fullerton, CA). Percent growth inhibition, defined as 100 × (1 - [generations in treated wells/generations in untreated controls]) was determined. Experiments were performed in duplicate. Error bars represent standard error for each experiment. Non-linear curve fitting was performed by fitting curves to data points using the Proc NLIN function in SAS for Windows version 9.2 (SAS Institute, Inc., Cary, NC) using a basic four-parameter sigmoid model. IC50 (concentration needed to prevent 50% of cell population doublings) and IC100 (complete inhibition of proliferation) were the summary outcome measures interpolated from the resulting curves.
Concentrations 0~100nM
Incubation time 5 days
Animal Experiment
Animal models BT-474 Breast cancer xenograft model Tumor Xenografts
Formulation formulated in 60 mM lactic acid or 2.5% ethanol, 20% 50 mM tartaric acid, 77.5% (5% glucose in water [D5W] containing 1% Tween 80) vol/vol
Dosages 25 to 58 mg/kg once per week
Administration intravenous
Chemical Information
Molecular Weight 465.54
Formula C26H31N3O5
CAS Number 747412-49-3
Solubility (25°C) DMSO 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Okui T et al. Curr Cancer Drug Targets. Novel HSP90 Inhibitor NVP-AUY922 enhances the anti-tumor effect of temsirolimus against oral squamous cell carcinoma.

[2] Moser C et al. Anticancer Res. Targeting HSP90 by the novel inhibitor NVP-AUY922 reduces growth and angiogenesis of pancreatic cancer.

[3] Best OG et al. Leuk Lymphoma. 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.

[4] Walsby E et al. Oncotarget. The Hsp90 inhibitor NVP-AUY922-AG inhibits NF-κB signaling, overcomes microenvironmental cytoprotection and is highly synergistic with fludarabine in primary CLL cells.

[5] Zaidi S et al. PLoS One. The HSP90 inhibitor NVP-AUY922 radiosensitizes by abrogation of homologous recombination resulting in mitotic entry with unresolved DNA damage.

[6] Ueno T et al. Lung Cancer. Strong anti-tumor effect of NVP-AUY922, a novel Hsp90 inhibitor, on non-small cell lung cancer.

Related HSP Products
Hsp70-derived octapeptide

Hsp70-derived octapeptide is a conserved octapeptide of the C-terminal end of Hsp70, which physically interacts with tetratricopeptide repeat (TPR) motifs.

p5 Ligand for Dnak and DnaJ

p5 Ligand for Dnak and DnaJ is a nonapeptide, which corresponds to the main binding site for the 23-residue part of the presequence of mitochondrial aspartate aminotransferase.

Tertomotide hydrochloride

Tertomotide hydrochloride is a peptide consisting of 16 amino acids containing sequences derived from human telomerase reverse transcriptase (TERT).Tertomotide penetrates cells and interacts with HSP70 and HSP90, as well as inhibiting amyloid beta and tau, and inhibiting aging-related signaling in the brain. pathways, which could be used in aging and Alzheimer's disease related studies.

BMS-986263

BMS-986263 is a small interfering RNA (siRNA) that targets Hsp47 and can be used in studies related to idiopathic pulmonary fibrosis (IPF).

AT-533

AT-533 is a potent Hsp90 and HSV inhibitor.

  Catalog
Abmole Inhibitor Catalog




Keywords: Luminespib (AUY922), NVP-AUY922; Luminespib supplier, HSP, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.