2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. LSZ-102

LSZ-102 is a potent, orally bioavailable selective estrogen receptor degrader with an IC50 of 0.2 nM.

For research use only. We do not sell to patients.

LSZ-102 Chemical Structure

LSZ-102 Chemical Structure

CAS No. : 2135600-76-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 248 In-stock
Solution
10 mM * 1 mL in DMSO USD 248 In-stock
Solid
5 mg USD 240 In-stock
10 mg USD 385 In-stock
25 mg USD 650 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

LSZ-102 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE LSZ-102

View All Estrogen Receptor/ERR Isoform Specific Products:

View All Isoforms
Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

LSZ-102 is a potent, orally bioavailable selective estrogen receptor degrader with an IC50 of 0.2 nM.

IC50 & Target

estrogen receptor[1]
In Vitro

LSZ-102 is a potent, orally bioavailable selective estrogen receptor degrader with an IC50 of 0.2 nM and currently in Phase I/Ib trials for the treatment of ERα positive breast cancer. LSZ-102 induces significant degradation of ERα after 24 h, when given as a 10 μM solution to MCF-7 cells. 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 demonstrate that LSZ-102 effectively inhibits the estrogen-induced activation of the ERE-luciferase reporter using charcoal-stripped serum treated with E2 with IC50 of 0.3 nM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

LSZ-102 Related Antibodies
In Vivo

Treatment of the mice with LSZ-102 once daily at 20 mg/kg results in significant tumor growth inhibition as compare to the control group treated with vehicle alone, resulting in tumor stasis (mean change in tumor volume of LSZ-102 vs control=%ΔT/ΔC of 2.4% on day 48, p<0.05). Dosing of 3 mg/kg solution of LSZ-102 in male Sprague-Dawley rats results in 33% bioavailability and a dose-normalized exposure of 620 nM•h[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

470.46

Formula

C25H17F3O4S
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(O)/C=C/C1=CC=C(OC2=C(C3=CC=C(F)C=C3C(F)(F)C)SC4=CC(O)=CC=C42)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (212.56 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1256 mL 10.6279 mL 21.2558 mL
5 mM 0.4251 mL 2.1256 mL 4.2512 mL
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.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.67 mg/mL (3.55 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1.67 mg/mL (3.55 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

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
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

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.
Purity & Documentation

Purity: 99.94%

COA (255 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
References
Kinase Assay
[1]

Growth factors depleted MCF-7 ERE-luc cells are used and seeded (10 000 cells/well) in 96-well plates in CSS medium. After overnight incubation, cells are treated with LSZ-102 in the presence of estradiol (0.1 nM) for 24 h. Cells are then lysed and quantified for luciferase activity using Bright-Glo assay[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Female athymic nude mice are used for tumor xenograft studies. MCF-7 cells are subcutaneously injected (200 μL/animal) in the right axillary mammary fat pad area. Tumor volume and body weights are measured twice weekly. When tumors reach an average volume of ~200 mm3, mice are randomized into different groups. Animals are orally administered vehicle alone or 20 mg/kg LSZ-102 daily or 60 mg/kg tamoxifen 5 days per week[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

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, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1256 mL 10.6279 mL 21.2558 mL 53.1395 mL
5 mM 0.4251 mL 2.1256 mL 4.2512 mL 10.6279 mL
10 mM 0.2126 mL 1.0628 mL 2.1256 mL 5.3139 mL
15 mM 0.1417 mL 0.7085 mL 1.4171 mL 3.5426 mL
20 mM 0.1063 mL 0.5314 mL 1.0628 mL 2.6570 mL
25 mM 0.0850 mL 0.4251 mL 0.8502 mL 2.1256 mL
30 mM 0.0709 mL 0.3543 mL 0.7085 mL 1.7713 mL
40 mM 0.0531 mL 0.2657 mL 0.5314 mL 1.3285 mL
50 mM 0.0425 mL 0.2126 mL 0.4251 mL 1.0628 mL
60 mM 0.0354 mL 0.1771 mL 0.3543 mL 0.8857 mL
80 mM 0.0266 mL 0.1328 mL 0.2657 mL 0.6642 mL
100 mM 0.0213 mL 0.1063 mL 0.2126 mL 0.5314 mL
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LSZ-102 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    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:

LSZ-1022135600-76-7LSZ102LSZ 102Estrogen Receptor/ERRInhibitorinhibitorinhibit

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