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 |
| 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.
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