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Chemical Structure| 2135600-76-7 Chemical Structure| 2135600-76-7

Structure of LSZ-102
CAS No.: 2135600-76-7

Chemical Structure| 2135600-76-7

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LSZ102 is a potent ERα antagonist and degrader. LSZ102 showed ERα degradation IC50 = 0.2 nM. LSZ102 demonstrated IC50 for MCF-7 cells = 1.7 nM. Upon administration of LSZ102, this agent binds to the ER and induces the degradation of the receptor. This prevents ER activation and ER-mediated signaling, and inhibits the growth and survival of ER-expressing cancer cells.

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Product Details of LSZ-102

CAS No. :2135600-76-7
Formula : C25H17F3O4S
M.W : 470.46
SMILES Code : 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
MDL No. :N/A

Safety of LSZ-102

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02734615 Advanced or Metastatic ER+ Bre... More >>ast Cancer Less << Phase 1 Recruiting October 30, 2020 United States, Maryland ... More >> Novartis Investigative Site Recruiting Baltimore, Maryland, United States, 21287 United States, Massachusetts Massachusetts General Hospital Massachusetts General Hospital Recruiting Boston, Massachusetts, United States, 02114 Contact: Dejan Juric, MD    617-726-6500    Juric.Dejan@mgh.harvard.edu    Contact: Meghan Miles    617-726-6500    MEMILES@mgh.harvard.edu    Principal Investigator: Dejan Juric, MD          United States, New York Novartis Investigative Site Recruiting New York, New York, United States, 10021 Contact: Alexandra Burleigh    646-422-4394    burleiga@mskcc.org    Principal Investigator: Komal Jhaveri          United States, Texas Novartis Investigative Site Recruiting Houston, Texas, United States, 77030 Contact: Daniela Westerhold       diwesterhold@mdanderson.org    Principal Investigator: Rachel M Layman          Belgium Novartis Investigative Site Recruiting Bruxelles, Belgium, 1200 Canada, Ontario Novartis Investigative Site Recruiting Toronto, Ontario, Canada, M5G 2M9 France Novartis Investigative Site Recruiting Lyon Cedex, France, 69373 Italy Novartis Investigative Site Recruiting Milano, MI, Italy, 20133 Novartis Investigative Site Recruiting Milano, MI, Italy, 20141 Japan Novartis Investigative Site Recruiting Koto-ku, Tokyo, Japan, 135 8550 Singapore Novartis Investigative Site Recruiting Singapore, Singapore, 169610 Spain Novartis Investigative Site Recruiting Barcelona, Catalunya, Spain, 08036 Novartis Investigative Site Recruiting Madrid, Spain, 28007 Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.13mL

0.43mL

0.21mL

10.63mL

2.13mL

1.06mL

21.26mL

4.25mL

2.13mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
 

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