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.
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- 純度: 98.97%
- 分子式: C34H49F3N4O10
- 分子量:730.77
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保管条件:
-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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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 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.
Customer Validation & Images
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生物活性
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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性状 Solid
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分子量 730.77
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分子式 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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別名
17-DMAG TFA; KOS-1022 TFA; NSC 707545 TFA
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-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.
純度とドキュメンテーション
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データシート (276 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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取扱説明書 (2659 KB)
参考文献
[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]
Calculators
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Alvespimycin TFA 関連分類
HY-10389A 関連分類
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