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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.
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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. |
| 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 |
| 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 |
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| Ganetespib
Ganetespib (STA-9090) is a potent synthetic small molecule inhibitor of Hsp90 with potential antineoplastic activity. |
| NVP-HSP990
NVP-HSP990 is an orally bioavailable inhibitor of human heat-shock protein 90 (Hsp90) with IC50 values of 0.6, 0.8, and 8.5 nM for Hsp90α, Hsp90β, and Grp94, respectively. NVP-HSP990 has potential antineoplastic activity. |
| VER-82576
VER-82576 (NVP-BEP800) is a potent, orally available and selective inhibitor of Hsp90β with an IC50 of 58 nM. VER-82576 also slightly blocks Grp94 and Trap-1, with IC50s of 4.1 and 5.5 μM, respectively. |
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