An ERα antagonist
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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
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
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    500 µg

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    1 mg

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    5 mg

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    Cayman Chemical
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    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).