Alvespimycin TFA
Based on 9 publication(s) in Google Scholar
Alvespimycin (17-DMAG) TFA is a potent inhibitor of Hsp90, binding to Hsp90 with an EC50 of 62 nM.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98.97%
- Formel: C34H49F3N4O10
- Molecular Weight:730.77
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Speicherung:
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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Publications Citing Use of MedChemExpress (MCE) Alvespimycin TFA
More- Theranostics. 2020 Jul 9;10(18):8415-8429. [Abstract]
- Adv Sci (Weinh). 2025 Jul 29:e01977. [Abstract]
- Cell Death Dis. 2022 Jan 21;13(1):73. [Abstract]
- Pharmacol Res. 2020 Jan:151:104512. [Abstract]
- NPJ Precis Oncol. 2023 May 18;7(1):44. [Abstract]
- ACS Biomater Sci Eng. 2021 Nov 8;7(11):5154-5164. [Abstract]
- Sci Rep. 2021 May 26;11(1):11057. [Abstract]
- Exp Ther Med. 2022 Apr;23(4):273. [Abstract]
- Friedrich-Alexander University Erlangen-Nuremberg. 2016 Sep 14.
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Biologische Aktivität
Beschreibung
In Vitro
Alvespimycin (17-DMAG) TFA inhibits the growth of the human cancer cell lines SKBR3 and SKOV3, which overexpress Hsp90 client protein Her2, and causes down-regulation of Her2 as well as induction of Hsp70 consistent with Hsp90 inhibition, for Her2 degradation with EC50 of 8 nM and 46 nM in SKBR3 and SKOV3 cells, respectively; for Hsp70 induction with EC50 of 4 nM and 14 nM in SKBR3 and SKOV3 cells, respectively[1].
Compared with the vehicle control, Alvespimycin (17-DMAG) TFA dose-dependent apoptosis (P<0.001 averaged across 24- and 48-hour time points) at concentrations of 50 nM to 500 nM, which represent pharmacologically attainable doses. Similar to many other agents, Alvespimycin (17-DMAG) TFA also demonstrates time-dependent apoptosis (P <0.001, averaged across all doses) in chronic lymphocytic leukemia (CLL) cells with extended exposure from 24 to 48 hours. In addition,Alvespimycin (17-DMAG) TFA is much more potent after 24 and 48 hours of treatment than 17-AAG[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Appearance Solid
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Molecular Weight 730.77
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Formel C34H49F3N4O10
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Color Pale purple to purple
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SMILES
O=C(O)C(F)(F)F.C/C1=C\C=C/[C@@H]([C@H](/C(C)=C/[C@@H]([C@H]([C@H](C[C@@H](CC(C(C(NC1=O)=CC2=O)=O)=C2NCCN(C)C)C)OC)O[H])C)OC(N)=O)OC
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Synonyms
17-DMAG TFA; KOS-1022 TFA; NSC 707545 TFA
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (9)
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Journal Impact Factor
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Most Recent
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Theranostics
Hsp90 inhibitor HSP990 in very low dose upregulates EAAT2 and exerts potent antiepileptic activity. [Abstract]2020 Jul 9;10(18):8415-8429. PMID: 32724478
Alvespimycin TFA purchased from MedChemExpress. Usage Cited in: Theranostics. 2020 Jul 9;10(18):8415-8429. [Abstract]
Western blot analysis of three proteins of interest in astrocytes treated with the Alvespimycin (17DMAG) for 24 h. Alvespimycin treatment increases EAAT2 and Hsp70 levels in a dose-dependent manner.
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Adv Sci (Weinh)
2025 Jul 29:e01977. PMID: 40729735 -
Cell Death Dis
RNA binding protein NKAP protects glioblastoma cells from ferroptosis by promoting SLC7A11 mRNA splicing in an m6A-dependent manner. [Abstract]2022 Jan 21;13(1):73. PMID: 35064112 -
Pharmacol Res
Destabilization of ROR1 enhances activity of Ibrutinib against chronic lymphocytic leukemia in vivo. [Abstract]2020 Jan:151:104512. PMID: 31726100 -
NPJ Precis Oncol
2023 May 18;7(1):44. PMID: 37202469 -
ACS Biomater Sci Eng
2021 Nov 8;7(11):5154-5164. PMID: 34636537 -
Sci Rep
Functional characterization of a loss-of-function mutant I324M of arginine vasopressin receptor 2 in X-linked nephrogenic diabetes insipidus. [Abstract]2021 May 26;11(1):11057. PMID: 34040143 -
Exp Ther Med
2022 Apr;23(4):273. PMID: 35251339 -
Alvespimycin TFA purchased from MedChemExpress. Usage Cited in: Friedrich-Alexander University Erlangen-Nuremberg. 2016 Sep 14.
pJAK2 and JAK2 expression upon TGFβ stimulation and JAK inhibitors incubation. pJAK2 and JAK2 expression in healthy human fibroblasts after stimulation with TGFβ for 3 days and incubation with TG101209, 17-DMAG or Ruxolitinib.
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : ≥ 100 mg/mL (136.84 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Ge J, et al. Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90. J Med Chem. 2006 Jul 27;49(15):4606-15. [Content Brief]
[2]. Hertlein E, et al. 17-DMAG targets the nuclear factor-kappaB family of proteins to induce apoptosis in chronic lymphocytic leukemia: clinical implications of HSP90 inhibition. Blood. 2010 Jul 8;116(1):45-53. [Content Brief]
[3]. Henke A, et al. Reduced Contractility and Motility of Prostatic Cancer-Associated Fibroblasts after Inhibition of Heat Shock Protein 90. Cancers (Basel). 2016 Aug 24;8(9). pii: E77. [Content Brief]
Complete Stock Solution Preparation Table
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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.3684 mL | 6.8421 mL | 13.6842 mL | 34.2105 mL |
| 5 mM | 0.2737 mL | 1.3684 mL | 2.7368 mL | 6.8421 mL | |
| 10 mM | 0.1368 mL | 0.6842 mL | 1.3684 mL | 3.4210 mL | |
| 15 mM | 0.0912 mL | 0.4561 mL | 0.9123 mL | 2.2807 mL | |
| 20 mM | 0.0684 mL | 0.3421 mL | 0.6842 mL | 1.7105 mL | |
| 25 mM | 0.0547 mL | 0.2737 mL | 0.5474 mL | 1.3684 mL | |
| 30 mM | 0.0456 mL | 0.2281 mL | 0.4561 mL | 1.1403 mL | |
| 40 mM | 0.0342 mL | 0.1711 mL | 0.3421 mL | 0.8553 mL | |
| 50 mM | 0.0274 mL | 0.1368 mL | 0.2737 mL | 0.6842 mL | |
| 60 mM | 0.0228 mL | 0.1140 mL | 0.2281 mL | 0.5702 mL | |
| 80 mM | 0.0171 mL | 0.0855 mL | 0.1711 mL | 0.4276 mL | |
| 100 mM | 0.0137 mL | 0.0684 mL | 0.1368 mL | 0.3421 mL |
Alvespimycin TFA Related Classifications
HY-10389A Related Classifications
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