An ERα antagonist
Technical Support & Resources

Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.

Visit our FAQ

Contact Us

Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888

Request Technical Support

Technical Support Request

To streamline the process attach the appropriate questionnaire to your inquiry.

Download IHC QuestionnaireDownload WB Questionnaire

View Our Privacy Statement for details on how we use and protect your data. In addition, this site is protected by hCaptcha and its Privacy Policy and Terms of Service apply.

Palazestrant

Item No. 41843

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(1R,3R)-2-(2-fluoro-2-methylpropyl)-2,3,4,9-tetrahydro-3-methyl-1-[4-[(1-propyl-3-azetidinyl)oxy]phenyl]-1H-pyrido[3,4-b]indole
CAS Number
2092925-89-6
Synonyms
  • OP-1250
Molecular Formula
C28H36FN3O
Formula Weight
449.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/mlDMSO: Slightly soluble: 0.1-1 mg/ml
SMILES
C[C@H](CC1=C2NC3=CC=CC=C31)N(CC(F)(C)C)[C@@H]2C4=CC=C(OC5CN(CCC)C5)C=C4
InChi Code
InChI=1S/C28H36FN3O/c1-5-14-31-16-22(17-31)33-21-12-10-20(11-13-21)27-26-24(23-8-6-7-9-25(23)30-26)15-19(2)32(27)18-28(3,4)29/h6-13,19,22,27,30H,5,14-18H2,1-4H3/t19-,27-/m1/s1
InChi Key
LBSFUBLFDCAEKV-XHCCPWGMSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Recommended Products

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

Download most recent Certificate of Analysis for this product

    500 µg

    $32

    Add

    1 mg

    $61

    Add

    5 mg

    $208

    Add
    Cayman Chemical
    Visit Our Cancer Resource Center
    Find Tools & Resources to Study the Hallmarks of Cancer
    • Cancer cell signaling & regulation
    • Cancer metabolism
    • Tumor microenvironment
    EXPLORE NOW
    Product Description

    Palazestrant is an antagonist of estrogen receptor α (ERα ; IC50 = 6.4 nM).1 It also induces degradation of ERα in MCF-7 breast cancer cells (EC50 = 0.52 nM). Palazestrant decreases the proliferation of MCF-7 and CAMA-1 breast cancer cells (IC50s = 1.8 and 1.7 nM, respectively). It inhibits estradiol-induced cell cycle progression in the same cells when used at a concentration of 100 nM. In vivo, palazestrant (10 mg/kg per day), alone and in combination with ribociclib (LEE011; Item Nos. 17666 | 36414), reduces tumor growth and increases survival in an estradiol-stimulated patient-derived xenograft (PDX) mouse model of breast cancer.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Parisian, A.D., Barratt, S.A., Hodges-Gallagher, L., et al. Palazestrant (OP-1250), a complete estrogen receptor antagonist, inhibits wild-type and mutant ER-positive breast cancer models as monotherapy and in combination. Mol. Cancer Ther. 23(3), 285-300 (2024).