Ganetespib [888216-25-9]
Cat# HY-15205-10mg
Size : 10mg
Brand : MedChemExpress
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- Antibody-drug Conjugate/ADC Related
- Apoptosis
- Autophagy
- Cell Cycle/DNA Damage
- Cytoskeleton
- Epigenetics
- GPCR/G Protein
- Immunology/Inflammation
- JAK/STAT Signaling
- MAPK/ERK Pathway
- Membrane Transporter/Ion Channel
- Metabolic Enzyme/Protease
- Neuronal Signaling
- NF-κB
- PI3K/Akt/mTOR
- PROTAC
- Protein Tyrosine Kinase/RTK
- Stem Cell/Wnt
- TGF-beta/Smad
- Vitamin D Related/Nuclear Receptor
- Others
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
Select the appropriate dissolution method based on your experimental animal and administration route.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
- Protocol 1
Add each solvent one by one: 15% Cremophor EL 85% Saline
Solubility: 10 mg/mL (27.44 mM); Suspended solution; Need ultrasonic
- Protocol 2
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.86 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution. - Protocol 3
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.86 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear. - Protocol 4
Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.86 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Dosage
mg/kgAnimal weight
(per animal)
Dosing volume
(per animal)
Number of animals
-
[1]. Shimamura T, et al. 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. Clin Cancer Res. 2012 Jul 17. [Content Brief]
[2]. Ying W, et al. Ganetespib, a unique triazolone-containing Hsp90 inhibitor, exhibits potent antitumor activity and a superior safety profile for cancer therapy. Mol Cancer Ther. 2012 Feb;11(2):475-84. [Content Brief]
[3]. London CA, et al. Phase I evaluation of STA-1474, a prodrug of the novel HSP90 inhibitor ganetespib, in dogs with spontaneous cancer. PLoS One. 2011;6(11):e27018. [Content Brief]
[4]. Proia DA, et al. Multifaceted intervention by the Hsp90 inhibitor ganetespib (STA-9090) in cancer cells with activated JAK/STAT signaling. PLoS One. 2011 Apr 14;6(4):e18552. [Content Brief]
[5]. Stewart E, et al. Identification of Therapeutic Targets in Rhabdomyosarcoma through Integrated Genomic, Epigenomic, and Proteomic Analyses. Cancer Cell. 2018 Sep 10;34(3):411-426.e19. [Content Brief]
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
Cells are grown in 96-well plates based on optimal growth rates determined empirically for each line. Twenty-four hours after plating, cells are treated with the indicated compounds or controls for 72 hours. AlamarBlue is added (10% v/v) to the cells, and the plates are incubated for 3 hours and, then, subjected to fluorescence detection. For the comparative viability/apoptosis assay, NCI-H1975 cells are treated with escalating concentrations of ganetespib for the indicated time periods and subjected to viability analysis via CellTiter Fluor and apoptosis via Caspase Glo 3/7. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
Mice: NCI-H1975 or HCC827 cells are cultured as above and 0.5-1×107 cells are mixed with 50% RPMI 1640/50% Matrigel and subcutaneously injected into the flanks of SCID mice. For efficacy studies, animals with 100-200 mm3 tumors are then randomized into treatments groups of eight. Tumor volumes (V) are calculated by the equation V=0.5236×L×W×T (Length, width, and thickness). Animals are treated by intravenous bolus tail vein injection at 10 mL/kg with ganetespib formulated in 10/18 DRD (10% DMSO, 18% Cremophor RH 40, 3.6% dextrose and 68.4% water). As a measurement of in vivo efficacy, the relative size of treated and control tumors [(%T/C) value] is determined from the change in average tumor volumes of each drug-treated group relative to the vehicle-treated group, or itself in the case of tumor regression. Body weights are monitored daily. For biomarker studies, mice bearing NCI-H1975 xenografts are treated with either a single dose of vehicle or ganetespib, or with 5 daily doses of vehicle or ganetespib, in groups of 3 or 8, and harvested at various time points. Tumors are excised and flash frozen in liquid nitrogen for preparation of protein lysates or fixed in 10% neutral buffered formalin for immunohistochemistry. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
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[1]. Shimamura T, et al. 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. Clin Cancer Res. 2012 Jul 17.
[2]. Ying W, et al. Ganetespib, a unique triazolone-containing Hsp90 inhibitor, exhibits potent antitumor activity and a superior safety profile for cancer therapy. Mol Cancer Ther. 2012 Feb;11(2):475-84.
[3]. London CA, et al. Phase I evaluation of STA-1474, a prodrug of the novel HSP90 inhibitor ganetespib, in dogs with spontaneous cancer. PLoS One. 2011;6(11):e27018.
[4]. Proia DA, et al. Multifaceted intervention by the Hsp90 inhibitor ganetespib (STA-9090) in cancer cells with activated JAK/STAT signaling. PLoS One. 2011 Apr 14;6(4):e18552.
[5]. Stewart E, et al. Identification of Therapeutic Targets in Rhabdomyosarcoma through Integrated Genomic, Epigenomic, and Proteomic Analyses. Cancer Cell. 2018 Sep 10;34(3):411-426.e19.
* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
---|
DMSO | 1 mM | 2.7442 mL | 13.7212 mL | 27.4424 mL | 68.6059 mL |
5 mM | 0.5488 mL | 2.7442 mL | 5.4885 mL | 13.7212 mL | |
10 mM | 0.2744 mL | 1.3721 mL | 2.7442 mL | 6.8606 mL | |
15 mM | 0.1829 mL | 0.9147 mL | 1.8295 mL | 4.5737 mL | |
20 mM | 0.1372 mL | 0.6861 mL | 1.3721 mL | 3.4303 mL | |
25 mM | 0.1098 mL | 0.5488 mL | 1.0977 mL | 2.7442 mL | |
30 mM | 0.0915 mL | 0.4574 mL | 0.9147 mL | 2.2869 mL | |
40 mM | 0.0686 mL | 0.3430 mL | 0.6861 mL | 1.7151 mL | |
50 mM | 0.0549 mL | 0.2744 mL | 0.5488 mL | 1.3721 mL | |
60 mM | 0.0457 mL | 0.2287 mL | 0.4574 mL | 1.1434 mL | |
80 mM | 0.0343 mL | 0.1715 mL | 0.3430 mL | 0.8576 mL | |
100 mM | 0.0274 mL | 0.1372 mL | 0.2744 mL | 0.6861 mL |
- Cell Cycle/DNA Damage Metabolic Enzyme/Protease Apoptosis
- HSP Apoptosis
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Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
Keywords:
Ganetespib888216-25-9STA-9090STA9090STA 9090HSPApoptosisHeat shock proteinsInhibitorinhibitorinhibit
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- Product Name:
- Ganetespib
- Cat. No.:
- HY-15205
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