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Estrogen receptor modulator 10

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Catalog No. T82439Cas No. 2991504-90-4

Compound G-5b, an estrogen receptor modulator 10, functions as an estrogen receptor (ER) antagonist (IC50=6.7 nM) and degrader (DC50=0.4 nM). It has the capability to induce apoptosis and block cells at the G1/G0 phase, making it applicable in cancer research [1].

Estrogen receptor modulator 10

Estrogen receptor modulator 10

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Catalog No. T82439Cas No. 2991504-90-4
Compound G-5b, an estrogen receptor modulator 10, functions as an estrogen receptor (ER) antagonist (IC50=6.7 nM) and degrader (DC50=0.4 nM). It has the capability to induce apoptosis and block cells at the G1/G0 phase, making it applicable in cancer research [1].
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
5 mgInquiry8-10 weeks8-10 weeks
50 mgInquiry8-10 weeks8-10 weeks
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction

Bioactivity
Description
Compound G-5b, an estrogen receptor modulator 10, functions as an estrogen receptor (ER) antagonist (IC50=6.7 nM) and degrader (DC50=0.4 nM). It has the capability to induce apoptosis and block cells at the G1/G0 phase, making it applicable in cancer research [1].
In vitro
The estrogen receptor modulator 10, at concentrations of 20-100 nM applied for 2-48 hours, significantly suppresses the activity of the estrogen receptor (ER) in T47D cells in a dose-dependent manner. In MCF-7 cells, it elicits a delayed reduction in the degradation level of cellular ER compared to T47D cells [1].
In vivo
Estrogen receptor modulator 10 (30 mg/kg, intramuscular (i.m.) injection, single dose) exhibited favorable pharmacokinetic properties in female Sprague-Dawley rats [1].
Chemical Properties
Molecular Weight728.71
FormulaC32H37F9N4O3S
Cas No.2991504-90-4
SmilesC(C(CO)(F)F)N1[C@@H](C2=C(C=3C(N2)=CC=CC3)C[C@H]1C)C4=C(F)C=C(NC5CN(CCCS(CCCC(C(F)(F)F)(F)F)(=O)=O)C5)C=C4F
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

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:
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Dose Conversion

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Tech Support

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

EstrogenReceptorEstrogen ReceptorERR
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