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LSZ-102

Catalog No. T15788 CAS 2135600-76-7

Synonyms: 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.

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LSZ-102, CAS 2135600-76-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 98.00
2 mg	In stock	$ 147.00
5 mg	In stock	$ 247.00
10 mg	In stock	$ 413.00
25 mg	In stock	$ 692.00
50 mg	In stock	$ 985.00
1 mL * 10 mM (in DMSO)	In stock	$ 256.00

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Purity: 97.84%

Biological Description

Chemical Properties

Storage & Solubility Information

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
Molecular Weight	470.46
Formula	C25H17F3O4S
CAS No.	2135600-76-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

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

References and Literature

1. Tria GS, et al. Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer. J Med Chem. 2018 Apr 12;61(7):2837-2864.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Compound Library

Related Products

Related compounds with same targets

Erteberel Dihydroresveratrol Genistin MPP hydrochloride Ethynyl estradiol Estriol Diethylstilbestrol Brilanestrant

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Keywords

LSZ-102 2135600-76-7 Endocrinology/Hormones Estrogen Receptor/ERR LSZ 102 LSZ102 inhibitor inhibit

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