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Ganetespib (STA-9090) is a potent synthetic small molecule inhibitor of Hsp90 with potential antineoplastic activity. Ganetespib (STA-9090) has shown strong activity in a broad range of preclinical solid and hematologic cancer models, including models highly resistant to treatment.
Int J Mol Sci. 2023 Sep 30;24(19):14776.
Annexin A2 Stabilizes Oncogenic JAG1 Intracellular Domain by Inhibiting Proteasomal Degradation in Glioblastoma Cells
Ganetespib purchased from AbMole
| Cell Experiment | |
|---|---|
| Cell lines | NCI-H1975 and HCC827 cell lines |
| Preparation method | Cell viability assays. Cells were grown in 96-well plates based on optimal growth rates determined empirically for each line. Twenty-four hours after plating, cells were treated with the indicated compounds or controls for 72 hours. AlamarBlue (Invitrogen) was added (10% v/v) to the cells, and the plates were incubated for 3 hours and, then, subjected to fluorescence detection. For the comparative viability/ apoptosis assay, NCI-H1975 cells were treated with escalating concentrations of ganetespib for the indicated time periods and subjected to viability analysis via CellTiter Fluor (Promega) and apoptosis via Caspase Glo 3/7 (Promega). |
| Concentrations | 0~10 μM |
| Incubation time | 6, 24, 48, and 72 hours |
| Animal Experiment | |
|---|---|
| Animal models | NCI-H1975 tumor xenograft-implanted SCID mice |
| Formulation | formulated in 10/18 DRD (10% dimethyl sulfoxide, 18% Cremophor RH 40, 3.6% dextrose, 68.4% water) |
| Dosages | 125 mg/kg for 6-72 hours |
| Administration | oral gavage |
| Molecular Weight | 364.4 |
| Formula | C20H20N4O3 |
| CAS Number | 888216-25-9 |
| Solubility (25°C) | DMSO 37 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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|---|
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BIIB021 (CNF2024) is an orally available synthetic non-ansamycin Hsp90 inhibitor with ki value of 1.7nM. |
| CUDC-305
CUDC-305 is a heat shock protein 90 (HSP90) inhibitor of the novel imidazopyridine class, with IC50 values of 100 and 103 nM for HSP90α and HSP90β, respectively. |
| Luminespib (AUY922)
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. |
| 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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