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Luminespib

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Catalog No. T1989Cas No. 747412-49-3
Alias VER-52296, NVP-AUY922, AUY922

Luminespib (VER-52296) is an HSP90 inhibitor that inhibits HSP90α and HSP90β (IC50=7.8/21 nM). Luminespib has antitumor activity and is used in studies of head and neck tumors, among others.

Luminespib

Luminespib

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Purity: 99.25%
Catalog No. T1989Alias VER-52296, NVP-AUY922, AUY922Cas No. 747412-49-3
Luminespib (VER-52296) is an HSP90 inhibitor that inhibits HSP90α and HSP90β (IC50=7.8/21 nM). Luminespib has antitumor activity and is used in studies of head and neck tumors, among others.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
5 mg$52In StockIn Stock
10 mg$74In StockIn Stock
25 mg$148In StockIn Stock
50 mg$233In StockIn Stock
100 mg$382In StockIn Stock
200 mg$569-In Stock
500 mg$917-In Stock
1 mL x 10 mM (in DMSO)$57In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.25%
Color:White
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Product Introduction

Bioactivity
Description
Luminespib (VER-52296) is an HSP90 inhibitor that inhibits HSP90α and HSP90β (IC50=7.8/21 nM). Luminespib has antitumor activity and is used in studies of head and neck tumors, among others.
Targets&IC50
GRP94:535 nM, HSP90 β:21 nM (cell free), TRAP1:85 nM, HSP90 α:7.8 nM (cell free)
In vitro
METHODS: H. pylori infected GES-1 cells were treated with Patchouli alcohol (5-20 µg/mL) for 24 h. Apoptosis was detected by flow cytometry.
RESULTS: Patchouli alcohol treatment significantly reduced H. pylori-induced apoptosis. [1]
METHODS: H. pylori-infected GES-1 cells were treated with Patchouli alcohol (5-20 µg/mL) for 24 h. Cytokine levels were measured by ELISA.
RESULTS: Treatment with 5-20 µg/mL Patchouli alcohol significantly reduced the production of TNF-α and MCP-1. [1]
In vivo
METHODS: To study the effect on H. pylori-associated gastritis, Patchouli alcohol (5-20 mg/kg) was administered orally to H. pylori infected mice once daily for two weeks.
RESULTS: Patchouli alcohol treatment increased SH-NP content and CAT activity and significantly protected the gastric mucosa from H. pylori-induced damage. [1]
Cell Research
Cell lines were grown in DMEM/10% FCS, 2 mmol/L glutamine, and nonessential amino acids in a humidified atmosphere of 5% CO2 in air. All lines were free of Mycoplasma. Cell proliferation was determined using the sulforhodamine B (SRB) assay for tumor cells and prostate epithelial cells, the WST-1 assay for MCF10A and HB119, or an alkaline phosphatase assay for HUVEC and HDMEC. GI50 was the compound concentration inhibiting cell proliferation by 50% compared with vehicle controls. Cell cycle analysis was as described. Active caspase-3/7 was measured using a homogenous caspase assay kit [1].
Animal Research
In vivo, pharmacokinetic studies in female NCr athymic mice bearing WM266.4 human melanoma xenografts were essentially as described. NVP-AUY922 was dissolved in DMSO and diluted in sterile saline/Tween 20. A single dose of 50 mg/kg NVP-AUY922 was given i.v. or i.p. and groups of three animals were taken at intervals for pharmacokinetic analyses [1].
SynonymsVER-52296, NVP-AUY922, AUY922
Chemical Properties
Molecular Weight465.54
FormulaC26H31N3O5
Cas No.747412-49-3
SmilesCCNC(=O)c1noc(c1-c1ccc(CN2CCOCC2)cc1)-c1cc(C(C)C)c(O)cc1O
Relative Density.1.234 g/cm3
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 16.67 mg/mL (35.81 mM), Sonication is recommended.
Ethanol: 29 mg/mL (62.29 mM), Sonication is recommended.
H2O: < 1 mg/mL (insoluble or slightly soluble)
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 8.6 mg/mL (18.47 mM), Solution.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO/Ethanol
1mg5mg10mg50mg
1 mM2.1480 mL10.7402 mL21.4804 mL107.4022 mL
5 mM0.4296 mL2.1480 mL4.2961 mL21.4804 mL
10 mM0.2148 mL1.0740 mL2.1480 mL10.7402 mL
20 mM0.1074 mL0.5370 mL1.0740 mL5.3701 mL
Ethanol
1mg5mg10mg50mg
50 mM0.0430 mL0.2148 mL0.4296 mL2.1480 mL

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Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
% DMSO
%
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Dose Conversion

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

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