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LSZ-102

Name: LSZ-102
Brand: TargetMol
SKU: T15788
Price: 81 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T15788Cas No. 2135600-76-7

Alias LSZ102

LSZ-102 is an effective and selective degrader of estrogen receptor (IC50 = 0.2 nM) and can be used in studies about ERα positive breast cancer.

LSZ-102

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Purity: 98.56%

Catalog No. T15788Alias LSZ102Cas No. 2135600-76-7

LSZ-102 is an effective and selective degrader of estrogen receptor (IC50 = 0.2 nM) and can be used in studies about ERα positive breast cancer.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$81	-	In Stock
5 mg	$197	-	In Stock
10 mg	$318	-	In Stock
25 mg	$538	-	In Stock
50 mg	$723	-	In Stock
1 mL x 10 mM (in DMSO)	$198	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:98.56%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	LSZ-102 is an effective and selective degrader of estrogen receptor (IC50 = 0.2 nM) and can be used in studies about ERα positive breast cancer.
In vitro	LSZ-102 causes significant degradation of ERα after 24 h when given as a 10 μM solution to MCF-7 cells. LSZ-102 currently in Phase I/Ib trials for the treatment of ERα positive breast cancer. Robust inhibition of cell proliferation in MCF-7 cells is observed upon incubation with LSZ-102 with a half inhibitory concentration of 1.7 nM. Results show that LSZ-102 effectively inhibits the estrogen-induced activation of the ERE-luciferase reporter using charcoal-stripped serum treated with E2 (IC50: 0.3 nM)[1].
In vivo	In male Sprague-Dawley rats, LSZ-102 (3 mg/kg) causes 33% bioavailability and a dose-normalized exposure of 620 nM•h. In mice, LSZ-102 (20 mg/kg) causes significant tumor growth inhibition resulting in tumor stasis[1].
Synonyms	LSZ102

Chemical Properties

Molecular Weight	470.46
Formula	C₂₅H₁₇F₃O₄S
Cas No.	2135600-76-7
Smiles	CC(F)(F)c1cc(F)ccc1-c1sc2cc(O)ccc2c1Oc1ccc(\C=C\C(O)=O)cc1
Relative Density.	1.418 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 90 mg/mL (191.3 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.25 mM), Sonication is recommended.

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

	1mg	5mg	10mg	50mg
1 mM	2.1256 mL	10.6279 mL	21.2558 mL	106.2790 mL
5 mM	0.4251 mL	2.1256 mL	4.2512 mL	21.2558 mL
10 mM	0.2126 mL	1.0628 mL	2.1256 mL	10.6279 mL
20 mM	0.1063 mL	0.5314 mL	1.0628 mL	5.3139 mL
50 mM	0.0425 mL	0.2126 mL	0.4251 mL	2.1256 mL
100 mM	0.0213 mL	0.1063 mL	0.2126 mL	1.0628 mL

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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:

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 DMSO TargetMol | 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 DMSO TargetMol | reagent stock solution to 400 μL PEG300 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 ddH₂O TargetMol | 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.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

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