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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

🥰Excellent

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	Availability
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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Batch Information

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Purity:98.56%

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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 mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

Dose Conversion

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