Ganetespib [888216-25-9]
Referencia HY-15205-10mg
embalaje : 10mg
Marca : MedChemExpress
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Ganetespib (Synonyms: STA-9090)
- Cat. No.: HY-15205 Pureza: 99.84%
- COA Instrucciones de manejo
Ganetespib (STA-9090) is a heat shock protein 90 (HSP90) inhibitor which exhibits potent cytotoxicity in a wide variety of hematological and solid tumor cell lines. Ganetespib has antiangiogenic effects in colorectal cancer mediated through inhibition of HIF-1α and STAT3.
Para uso exclusivo en investigación. No vendemos a pacientes.
Ganetespib Estructura química
No. CAS : 888216-25-9
Tamaño | Precio | Stock | Cantidad |
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Muestra gratis (0.1 - 0.5 mg) | Solicite ahora | ||
Solid + Solvent | |||
10 mM * 1 mL
in DMSO
ready for reconstitution
|
USD 85 | En stock | |
Solution | |||
10 mM * 1 mL in DMSO | USD 85 | En stock | |
Solid | |||
5 mg | USD 77 | En stock | |
10 mg | USD 110 | En stock | |
50 mg | USD 209 | En stock | |
100 mg | USD 319 | En stock | |
200 mg | USD 539 | En stock | |
500 mg | USD 1078 | En stock | |
1 g | Obtener un presupuesto | ||
5 g | Obtener un presupuesto |
* Seleccione Cantidad antes de agregar artículos.
This product is a controlled substance and not for sale in your territory.
Revisión del cliente
Based on 40 publication(s) in Google Scholar
- •Cancer Cell. 2018 Sep 10;34(3):411-426.e19. [Abstract]
- •Nat Commun. 2020 Aug 7;11(1):3946. [Abstract]
- •J Control Release. 11 March 2022.
- •Theranostics. 2020 Jul 9;10(18):8415-8429. [Abstract]
- •Theranostics. 2019 Aug 12;9(20):5769-5783. [Abstract]
- •Theranostics. 2019 Jan 1;9(2):554-572. [Abstract]
- •Cell Death Dis. 2024 Jan 11;15(1):35. [Abstract]
- •Cell Rep. 2019 Jan 2;26(1):236-249.e4. [Abstract]
- •Cell Death Dis. 2018 Feb 7;9(2):165. [Abstract]
- •Elife. 2017 Sep 26;6:e28652. [Abstract]
- •J Biol Chem. 2024 Jan 8:105633. [Abstract]
- •Int J Mol Sci. 2023 Aug 23, 24(17), 13082.
- •Cancers (Basel). 2022 Mar 19;14(6):1575. [Abstract]
- •Hepatol Commun. 2022 Mar 3. [Abstract]
- •Front Pharmacol. 2021 Jul
- •J Virol. 2019 Oct 29;93(22):e01142-19. [Abstract]
- •Antimicrob Agents Chemother. 2018 Mar 27;62(4). pii: e01799-17. [Abstract]
- •Sci Rep. 2015 Aug 3;5:12728. [Abstract]
- •J Ultrasound Med. 2020 Jun;39(6):1223-1232. [Abstract]
- •Int J Biochem Cell Biol. 2019 Jan;106:35-45. [Abstract]
- •Cell Stress Chaperones. 2018 Sep;23(5):1137-1142. [Abstract]
- •ACS Chem Biol. 2016 Jan 15;11(1):200-10. [Abstract]
- •Anticancer Res. 2019 Apr;39(4):1767-1775. [Abstract]
- •University of Gothenburg. 2023 Jun 27.
- •McGill University. Massachusetts Institute of Technology. Department of Chemistry. 2022 Sep.
- •Faculty of Life Sciences, University College London. 2019 Oct.
- •Biomedical Sciences Group, Faculty of Medicine, Department of Cellular and Molecular Medicine. KU LEUVEN. 2019 Jun.
- •Massachusetts Institute of Technology, University of Texas at Dallas. 2018 Jun.
- •Oncotarget. 2015 Nov 24;6(37):39821-38. [Abstract]
- •Harvard Medical School LINCS LIBRARY
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Ganetespib purchased from MedChemExpress. Usage Cited in: Int J Biochem Cell Biol. 2019 Jan;106:35-45. [Abstract]
- Confocal immunofluorescence microscopy is performed on cultures that are immunoreacted with antibodies against HSP90β and phospho-Tyr705-STAT3 at 6-h recovery after heat shock with or without ganetespib (100 nM) and HSP90β esiRNA.
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Ganetespib purchased from MedChemExpress. Usage Cited in: Int J Biochem Cell Biol. 2019 Jan;106:35-45. [Abstract]
- Levels of HSP70, and phosphorylation and total protein of p38, ERK, JNK, JAK2, STAT3, IκB-α and p65 in total cell lysates are analysed using Western blotting with or without ganetespib (100 nM).
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Ganetespib purchased from MedChemExpress. Usage Cited in: Anticancer Res. 2019 Apr;39(4):1767-1775. [Abstract]
- Ganetespib suppresses epidermal growth factor receptor (EGFR) and its related downstream pathway molecules in non-small cell lung cancer cells with acquired resistance to EGFR-tyrosine kinase inhibitor. Cells are treated with the indicated concentration of ganetespib for 24 h, and lysates were analyzed by western blot. AKT: protein kinase B; EMT: epithelial-mesenchymal transition; MET: met proto-oncogene; amp: amplification; MAPK: mitogen-activated protein kinase.
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Ganetespib purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2018 Sep 10;34(3):411-426.e19. [Abstract]
- Immunoblot of HSP70 expression in RD cells after treatment with Ganetespib (GSP) alone or CPT-11+NSC-67574.
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Ganetespib purchased from MedChemExpress. Usage Cited in: Cell Stress Chaperones. 2018 Sep;23(5):1137-1142. [Abstract]
- Western blot analysis of human bladder cancer cell lysates (T24) treated with DMSO, the Hsp90 inhibitor STA9090, the Hsp70 inhibitors VER155008, and MAL3-101 or combinations of the various inhibitors. The blot is probed with a keratin 9 mouse monoclonal antibody
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Ganetespib purchased from MedChemExpress. Usage Cited in: Massachusetts Institute of Technology, University of Texas at Dallas. 2018 Jun.
- Immunoblot of HEK293T-Rex cells upon treatment with increasing concentrations of the HSP90 inhibitor STA-9090.
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Ganetespib purchased from MedChemExpress. Usage Cited in: Massachusetts Institute of Technology, University of Texas at Dallas. 2018 Jun.
- Immunoblot of HEK293T-REx cells inducibly expressing dn-cHSF1 following pretreatment with vehicle or dox (18 h; 1 pg/mL) and then HSR activation by treatment with arsenite (6 h; 100 pM) or STA-9090 (6 h; 100 nM).
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Ganetespib purchased from MedChemExpress. Usage Cited in: ACS Chem Biol. 2016 Jan 15;11(1):200-10. [Abstract]
- Protein level by immunoblotting for HSR target proteins.
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Ganetespib purchased from MedChemExpress. Usage Cited in: Sci Rep. 2015 Aug 3;5:12728. [Abstract]
- Ganetespib decreases the DYRK1A protein level. 293T cells are transiently transfected with an expression vector for 3xFLAG-DYRK1A. At 24 h after transfection, the cells are treated with Ganetespib (100 nM) and collected 0 and 8 h after treatment. Total cell lysates are subjected to SDS-PAGE followed by Western blot analysis using antibodies against FLAG and GAPDH. In the control group (DMSO), expression of 3xFLAG-DYRK1A increases at 8 h compared to 0 h, and Ganetespib suppresses this increase of
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Ganetespib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2015 Nov 24;6(37):39821-38. [Abstract]
- J82 cells are treated with 1 μM STA9090 and 50 μM VER155008 as mono or dual therapy for the time indicated. Lysates are prepared and Western blots probed for cell cycle markers.
Ver todos los productos específicos de isoformas HSP:
Actividad biológica
Protocolo
Pureza y Documentación
Referencias
Revisión del cliente
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IC50 & Target[1] |
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In Vitro |
Ganetespib causes depletion of receptor tyrosine kinases, extinguishing of downstream signaling, inhibition of proliferation and induction of apoptosis with IC50 values ranging 2-30 nM in genomically-defined NSCLC cell lines. Ganetespib is also approximately 20-fold more potent in isogenic Ba/F3 pro-B cells rendered IL-3 independent by expression of EGFR and ERBB2 mutants[1]. Ganetespib exhibits potent in vitro cytotoxicity in a range of solid and hematologic tumor cell lines, induces the degradation of known Hsp90 client proteins, displays superior potency to the ansamycin inhibitor 17-allylamino-17-demethoxygeldanamycin (17-AAG)[2]. Ganetespib is a potent HSP90 inhibitor, and shown to kill canine tumor cell lines in vitro[3]. Ganetespib possesses superior JAK/STAT inhibitory activity to both P6 and 17-AAG in terms of potency or duration of response in the HEL92.1.7 cells[4]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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In Vivo |
Ganetespib (125 mg/kg, i.v.) accumulates in tumors relative to normal tissues and displays greater in vivo efficacy than 17-AAG without increased toxicity and inhibits proliferation and induces apoptosis in parallel with EGFR depletion in NCI-H1975 xenografts[1]. Ganetespib (100, 125, 150 mg/kg, i.v.) shows potent antitumor efficacy in solid and hematologic xenograft models of oncogene addiction, as evidenced by significant growth inhibition and/or regressions[2]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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Ensayo clínico |
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Peso molecular |
364.40 |
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Fòrmula |
C20H20N4O3 |
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No. CAS | |||||||||||||
Appearance |
Solid |
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Color |
White to yellow |
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SMILES |
CN1C2=CC=C(N3C(NN=C3C4=CC(C(C)C)=C(O)C=C4O)=O)C=C2C=C1 |
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Envío | Room temperature in continental US; may vary elsewhere. |
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Almacenamiento |
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Solvente y solubilidad |
In Vitro:
DMSO : ≥ 100 mg/mL (274.42 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) *"≥" means soluble, but saturation unknown. Preparing
Stock Solutions
View the 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.
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 In Vivo:
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 In Vitro approach and then sequentially add co-solvents:
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage mg/kgAnimal weight Dosing volume Number of animals Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO
+
%
+
%
Tween-80
+
%
Saline
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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Pureza y Documentación | |||||||||||||
Referencias |
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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, 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 |
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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 |
Ganetespib Related Classifications
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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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- Nombre del producto:
- Ganetespib
- Cat. No.:
- HY-15205
- Cantidad:
- MCE Japan Authorized Agent: