LSZ-102 - Moligand™,10mM in DMSO , CAS No.2135600-76-7

CAS: 2135600-76-7 Cat. No.: L654690 Summenformel: C₂₅H₁₇F₃O₄S Molekulargewicht: 470.46 PubChem CID: 118574930

GRADE & PURITY Moligand™, 10mM in DMSO

Storage

Argon charged,Store at -80°C

Shipped In

Dry ice packs + Cold packs

Übersicht

LSZ-102 is a potent, orally bioavailable selective estrogen receptor degrader with an IC 50 of 0.2 nM.

In Vitro

LSZ-102 is a potent, orally bioavailable selective estrogen receptor degrader with an IC 50 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 IC 50 of 0.3 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

IC50& Target:estrogen receptor

Specifications

Spezifikationen & Reinheit

Moligand™,10mM in DMSO

Biochemische und physiologische Mechanismen

LSZ-102 is a potent, orally bioavailable selective estrogen receptor degrader with an IC 50 of 0.2 nM.

Storage

Argon charged,Store at -80°C

Verschickt in

Dry ice packs + Cold packs

Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.

Note

Moligand™

Aktionsart

DEGRADER

Namen und Kennungen

• Isomere SMILES: CC(C1=C(C=CC(=C1)F)C2=C(C3=C(S2)C=C(C=C3)O)OC4=CC=C(C=C4)/C=C/C(=O)O)(F)F
• Alternative CAS-Nummer: 2135600-76-7
• PubChem CID: 118574930
• MeSH-Eintrag: (E)-3-(4-((2-(2-(1,1-Difluoroethyl)-4-fluorophenyl)-6-hydroxybenzo(b)thiophen-3-yl)oxy)phenyl)acrylic acid;LSZ-102;LSZ102
• Molekulargewicht: 470.46

Zugehörige Ziele (menschlich)

ESR1 Tclin Estrogen receptor (0 Activities)

Discover Target: ESR1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Häufig gestellte Fragen

What is Moligand??

Moligand? is one of Aladdin Scientific's premium product lines, formulated for high-purity applications across multiple workflows. Compared to standard grades in the same workflow, Moligand? products typically offer tighter specifications, more rigorous QC, and stronger lot-to-lot consistency.

How should this product be stored?

Store at ?80 °C under argon. It is supplied under an argon blanket; reseal under inert gas after each use.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 2135600-76-7, the molecular formula is C25H17F3O4S, and the molecular weight is 470.46 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.