3-(2,4-Dihydroxy-5-isopropylphenyl)-4-(1-methylindol-5-yl)-5-hydroxy-4H-1,2,4-triazole
Ganetespib
CAS: 888216-25-9
Molecular Formula: C20H20N4O3
3-(2,4-Dihydroxy-5-isopropylphenyl)-4-(1-methylindol-5-yl)-5-hydroxy-4H-1,2,4-triazole - Names and Identifiers
3-(2,4-Dihydroxy-5-isopropylphenyl)-4-(1-methylindol-5-yl)-5-hydroxy-4H-1,2,4-triazole - Physico-chemical Properties
| Molecular Formula | C20H20N4O3 |
| Molar Mass | 364.4 |
| Density | 1.39 |
| Solubility | Soluble in DMSO (up to at least 25 mg/ml) |
| Appearance | solid |
| Color | White |
| pKa | 7.38±0.20(Predicted) |
| Storage Condition | -20°C |
| Stability | Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| In vitro study | The 50% inhibitory concentration (IC50) of Ganetespib against Malignant mast cell lines was 10-15 times lower than that of 17-AAG, indicating that the triazolone-class HSP90 inhibitors may have higher potency than the geldamycin-class inhibitors. Ganetespib inhibits the MG63 cell line with an IC50 of 43 nM. Ganetespib binds to the N-terminal ATP binding domain of Hsp90 by causing multiple tumorigenic Hsp90 receptor proteins, including HER2/neu, mutant EGFR,Akt,c-Kit,IGF-1R,PDGFR α,Jak1, the degradation of Jak2,STAT3,STAT5,HIF-1α,CDC2 and c-Met, as well as Wilms' tumor 1, became a potent inhibitor of HSP90. Ganetespib, at nanomolar low concentrations, effectively blocks cell proliferation and induces apoptosis in a wide range of human tumor cell lines, it also has effects on many receptor tyrosine kinase inhibitor-and tanespimycin-resistant cell lines. Ganetespib has shown potent cytotoxicity in a range of solid and hematologic tumor cell lines, including those expressing mutant kinases that are resistant to small molecule tyrosine kinase inhibitors. Treatment with Ganetespib rapidly causes degradation of the known Hsp90 receptor protein, exhibits higher potency than the ansamycin inhibitor 17-AAG, and also has sustained activity at shorter exposure times. In another study, Ganetespib induced apoptosis in a malignant canine mast cell line. Ganetespib effectively acts on C2 and BR canine Malignant mast cells at very low concentrations, with IC50 of 19 and 4 nM, respectively, while 17-AAG inhibited the IC50 of C2 and BR canine Malignant mast cells to 958 and 44 nM, respectively. After treatment with 100 nM Ganetespib for 24 hours, the expression of WT and mutant Kit was down-regulated in all treated cell lines, including C2 and BMCMCs cells. However, Ganetespib treatment did not affect PI3K or HSP90 expression. |
| In vivo study | Administration of Ganetespib resulted in significant tumor shrinkage in mice in several tumor xenograft models and appeared to be less toxic. In addition, Ganetespib had better tumor permeability than tanespimcin. Ganetespib inhibits tumor growth in vivo in Malignant mast cell and OSA xenograft models. Ganetespib(25 mg/kg/day,3 days) repeated two cycles significantly inhibited tumor growth,%T/C value was 18. Ganetespib was well tolerated with a +0.3 and -8.1% change in mean body weight at day 17 for the vehicle control and Ganetespib groups, respectively, relative to the start of the study. |
3-(2,4-Dihydroxy-5-isopropylphenyl)-4-(1-methylindol-5-yl)-5-hydroxy-4H-1,2,4-triazole - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.744 ml | 13.721 ml | 27.442 ml |
| 5 mM | 0.549 ml | 2.744 ml | 5.488 ml |
| 10 mM | 0.274 ml | 1.372 ml | 2.744 ml |
| 5 mM | 0.055 ml | 0.274 ml | 0.549 ml |
Last Update：2024-01-02 23:10:35
3-(2,4-Dihydroxy-5-isopropylphenyl)-4-(1-methylindol-5-yl)-5-hydroxy-4H-1,2,4-triazole - Reference Information
| biological activity | Ganetespib (STA-9090) is an HSP90 inhibitor with an IC50 of 4 nM in 8 OSA cells, induces apoptosis of OSA cells without affecting normal osteoblasts; Is STA-1474 active metabolite. Phase 3. |
| Target | Value |
| HSP90 (OSA 8 cells) | 4 nM |
Last Update：2024-04-09 19:05:15
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Spot supply
Product Name: Ganetespib Visit Supplier Webpage Request for quotationCAS: 888216-25-9
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Spot supply
Product Name: Ganetespib (STA-9090) Visit Supplier Webpage Request for quotationCAS: 888216-25-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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