Research Area
Product Type
United States ( Change Country )
17-AAG (Geldanamycin) Chemical Structure
Elesclomol
HSP-70 Inducer
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Biological Activity
17-AAG (Geldanamycin) is a less toxic analogue of the geldanamycin which binds to Hsp90 and alters its function. HSP90 client proteins play important roles in the regulation of the cell cycle, cell growth, cell survival, apoptosis, and oncogenesis. [1]
This agent displays a 100-fold higher affinity for HSP90 derived from tumor cells compared to HSP90 from normal cells. 17-AAG (Geldanamycin) binds into the ATP binding pocket in Hsp90 and induces the degradation of proteins that require this chaperone for conformational maturation. 17-AAG (Geldanamycin) inhibits Akt activation and expression in tumors and synergizes with a number of antitumor agents such as taxol, cisplatin, and UCN-014. [2]
References on 17-AAG (Geldanamycin)
- [1] Clin Cancer Res 2007;13:1591-1600
- [2] Blood 2003;102: 1824-1832
Product Information
| Molecular Weight (WM): | 585.69 |
|---|---|
| Formula: | C31H43N3O8 |
| CAS No.: | 75747-14-7 |
| Synonyms: |
Tanespimycin
|
| Dissolve in (25°C): | DMSO ≥20mg/mL |
| Water <1mg/mL | |
| Ethanol ≥5mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
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Selleck's high quality products have been used in several published research findings, including the following:
Therapeutic strategies to overcome crizotinib resistance in non-small cell lung cancers harboring the fusion oncogene EML4-ALK
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The Hsp90 inhibitor 17-AAG can overcome crizotinib resistance in H3122 CR cells. (A) Cell lines were seeded in 96-well plates and treated with 10 nM of 17-AAG for 72 h. Cell survival was analyzed using CellTiter-Glo. Both parental H3122 cells (red bar) and H3122 CR cells (blue bar) show sensitivity to 17-AAG. (B) Suppression of ALK signaling by 17-AAG in resistant H3122 CR cells. H3122 parental and resistant cells were exposed to increasing concentrations of 17-AAG for 6 h. Cell lysates were immunoblotted to detect the indicated proteins.
The Hsp90 inhibitor 17-AAG can overcome crizotinib resistance in H3122 CR cells. (A) Cell lines were seeded in 96-well plates and treated with 10 nM of 17-AAG for 72 h. Cell survival was analyzed using CellTiter-Glo. Both parental H3122 cells (red bar) and H3122 CR cells (blue bar) show sensitivity to 17-AAG. (B) Suppression of ALK signaling by 17-AAG in resistant H3122 CR cells. H3122 parental and resistant cells were exposed to increasing concentrations of 17-AAG for 6 h. Cell lysates were immunoblotted to detect the indicated proteins.
Data from [PNAS 2011 May;108:7535-40] 17-AAG (Geldanamycin) purchased from Selleck
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The Hsp90 inhibitor 17-AAG can overcome crizotinib resistance in H3122 CR cells. (A) Cell lines were seeded in 96-well plates and treated with 10 nM of 17-AAG for 72 h. Cell survival was analyzed using CellTiter-Glo. Both parental H3122 cells (red bar) and H3122 CR cells (blue bar) show sensitivity to 17-AAG. (B) Suppression of ALK signaling by 17-AAG in resistant H3122 CR cells. H3122 parental and resistant cells were exposed to increasing concentrations of 17-AAG for 6 h. Cell lysates were immunoblotted to detect the indicated proteins. |
Data from [PNAS 2011 May;108:7535-40]
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