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Ganetespib

Cat. No. M1741
Ganetespib Structure
Synonym:

STA-9090

Size Price Availability Quantity
10mg USD 150 In stock
50mg USD 500 In stock
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Quality Control
Biological Activity

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.

Protocol
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 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.

Chemical Information
Molecular Weight 364.4
Formula C20H20N4O3
CAS Number 888216-25-9
Purity 98.24%
Solubility DMSO
Storage at -20°C
References

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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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Ganetespib, STA-9090 supplier, HSP90, inhibitors

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