An ERα degrader
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LSZ-102

Item No. 41834

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[4-[[2E-[2-(1,1-difluoroethyl)-4-fluorophenyl]-6-hydroxybenzo[b]thien-3-yl]oxy]phenyl]-2-propenoic acid
CAS Number
2135600-76-7
Molecular Formula
C25H17F3O4S
Formula Weight
470.5
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Sparingly soluble: 1-10 mg/ml
SMILES
OC1=CC=C(C(OC2=CC=C(C=C2)/C=C/C(O)=O)=C(C3=C(C=C(C=C3)F)C(F)(F)C)S4)C4=C1
InChi Code
InChI=1S/C25H17F3O4S/c1-25(27,28)20-12-15(26)5-9-18(20)24-23(19-10-6-16(29)13-21(19)33-24)32-17-7-2-14(3-8-17)4-11-22(30)31/h2-13,29H,1H3,(H,30,31)/b11-4+
InChi Key
SJXNPGGVGZXKKI-NYYWCZLTSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

    $50

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    5 mg

    $236

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    10 mg

    $422

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    25 mg

    $990

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    Cayman Chemical
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    Product Description

    LSZ-102 is an estrogen receptor α (ERα) degrader (IC50 = 0.2 nM).1 It reduces 17β-estradiol-induced transcription in a reporter assay using MCF-7 breast cancer cells expressing ERα (IC50 = 6 nM). LSZ-102 decreases the proliferation of MCF-7 cells (IC50 = 1.7 nM). In vivo, LSZ-102 (20 mg/kg per day) reduces tumor volume in an MCF-7 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Tria, G.S., Abrams, T., Baird, J., 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. 61(7), 2837-2864 (2018).