Tamanho : 5mg
Telefone : +1 850 650 7790
Synonyms: STA-9090
| Description | Ganetespib (STA-9090) is a synthetic small-molecule inhibitor of heat shock protein 90 (Hsp90), exhibiting potential antineoplastic activity. |
| Targets & IC50 | HSP90:4 nM |
| 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. |
| Synonyms | STA-9090 |
| 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. |
| 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) |
| Molecular Weight | 364.4 |
| Formula | C20H20N4O3 |
| Cas No. | 888216-25-9 |
| Smiles | CC(C)c1cc(-c2n[nH]c(=O)n2-c2ccc3n(C)ccc3c2)c(O)cc1O |
| Relative Density. | 1.39 g/cm3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 83.33 mg/mL (228.68 mM), Sonication is recommended.  H2O: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.49 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
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