| Name | Ganetespib |
| Description | Ganetespib (STA-9090) is a synthetic small-molecule inhibitor of heat shock protein 90 (Hsp90), exhibiting potential antineoplastic activity. |
| Cell Research | A total of 1.5 × 103 OSA cells are seeded in 96-well plates in 10% serum-containing complete medium and incubated overnight to determine the 50% inhibitory concentrations. Plates are, harvested at day 5 following 0.001, 0.005, 0.01, 0.05, 0.1, 0.5 and 1 μM Ganetespib, treatment and analyzed. Fluorescence measurements are made using a plate reader with excitation at 485 nm and emission detection at 530 nm. Relative cell number is calculated as a percentage of the control wells: absorbance of sample/absorbance of DMSO treated cells × 100.(Only for Reference) |
| Kinase Assay | Exponentially growing cells are processed in lysis buffer (20 mM HEPES, pH 7.4, 1 mM EDTA, 5 mM MgCl2, 100 mM KCl) and incubated with increasing concentrations of 17-AAG or ganetespib for 30 min at 4°C, and incubated with biotin-GM linked to Dynabeads MyOne Streptavidin T1 magnetic beads for 1 h at 4°C. Beads are washed three times in lysis buffer and heated for 5 min at 95°C in SDS-PAGE sample buffer. Samples are resolved on 4-12% Bis-Tris gradient gel and Western blots are performed using an anti-HSP90 antibody. |
| In vitro | Ganetespib was able to exhibit cytotoxicity at the nanomolar level, inhibiting cell proliferation while inducing apoptosis in a variety of human anti-receptor tyrosine kinase inhibitor and tapepermycin-resistant cancer cell lines. In MG63 cell line (IC50=43 nM), Ganetespib inhibited cell growth. In C2 (IC50=19 nM) and BR canine malignant mast cells (IC50=4 nM), Ganetespib induced apoptosis. |
| In vivo | Ganetespib was able to exhibit cytotoxicity at the nanomolar level, inhibiting cell proliferation while inducing apoptosis in a variety of human anti-receptor tyrosine kinase inhibitor and tapepermycin-resistant cancer cell lines. In MG63 cell line (IC50=43 nM), Ganetespib inhibited cell growth. In C2 (IC50=19 nM) and BR canine malignant mast cells (IC50=4 nM), Ganetespib induced apoptosis. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | Ethanol : < 1 mg/mL (insoluble or slightly soluble)
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.49 mM), Sonication is recommended.
DMSO : 83.33 mg/mL (228.68 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
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| Keywords | STA9090 | STA 9090 | Inhibitor | inhibit | HSP90 | HSP | HIF-1α | Heat shock proteins | Ganetespib | Apoptosis |
| Inhibitors Related | Ethoxyquin | Stavudine | Aceglutamide | Urea | Tamoxifen | Cysteamine hydrochloride | Metronidazole | Citric Acid Triammonium | Formamide | Dimethyl phthalate | Alginic acid | Sildenafil citrate |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Bioactive Compound Library | Endoplasmic Reticulum Stress Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library | Transcription Factor-Targeted Compound Library |
United States
