A degrader of ERα
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Estrogen Receptor Antagonist 2

Item No. 43587

Technical Information
Formal Name
N-[1-(3-fluoropropyl)-3-azetidinyl]-6-[(6S,8R)-6,7,8,9-tetrahydro-8-methyl-7-(2,2,2-trifluoroethyl)-3H-pyrazolo[4,3-f]isoquinolin-6-yl]-3-pyridinamine
CAS Number
2222844-89-3
Synonyms
  • AZD9833
Molecular Formula
C24H28F4N6
Formula Weight
Purity
≥95%
A solid
DMSO: Soluble: ≥ 10 mg/mlEthanol: Soluble: ≥ 10 mg/ml
SMILES
FCCCN(C1)CC1NC2=CC=C([C@@H]3C(C=CC4=C5C=NN4)=C5C[C@H](N3CC(F)(F)F)C)N=C2
InChi Code
InChI=1S/C24H28F4N6/c1-15-9-19-18(4-6-21-20(19)11-30-32-21)23(34(15)14-24(26,27)28)22-5-3-16(10-29-22)31-17-12-33(13-17)8-2-7-25/h3-6,10-11,15,17,23,31H,2,7-9,12-14H2,1H3,(H,30,32)/t15-,23+/m1/s1
InChi Key
WDHOIABIERMLGY-CMJOXMDJSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Estrogen receptor antagonist 2 is a degrader of estrogen receptor α (ERα).1 It induces degradation of ERα in MCF-7 breast cancer cells (IC50 = 0.16 nM). Estrogen receptor antagonist 2 inhibits estradiol-induced growth in MCF-7 cells (IC50 = 5.01 nM). In vivo, estrogen receptor antagonist 2 (0.5-50 mg/kg per day) decreases 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. Scott, J.S., Moss, T.A., Balazs, A., et alDiscovery of AZD9833, a potent and orally bioavailable selective estrogen receptor degrader and antagonist. J. Med. Chem. 63(23), 14530-14559 (2020).