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.
|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).|
|Incubation time||6, 24, 48, and 72 hours|
|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|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
Ganetespib (STA-9090), a Non-Geldanamycin HSP90 Inhibitor, has Potent Antitumor Activity in In Vitro and In Vivo Models of Non-Small Cell Lung Cancer.
Shimamura et al. Clin Cancer Res. 2012 Jul 17. PMID: 22806877.
Synergistic activity of the Hsp90 inhibitor ganetespib with taxanes in non-small cell lung cancer models.
Proia et al. Invest New Drugs. 2012 Jan 10. PMID: 22227828.
Ganetespib, a unique triazolone-containing Hsp90 inhibitor, exhibits potent antitumor activity and a superior safety profile for cancer therapy.
Ying et al. Mol Cancer Ther. 2012 Feb;11(2):475-84. PMID: 22144665.
Multifaceted intervention by the Hsp90 inhibitor ganetespib (STA-9090) in cancer cells with activated JAK/STAT signaling.
Proia et al. PLoS One. 2011 Apr 14;6(4):e18552.. PMID: 21533169.
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