A selective estrogen receptor degrader
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ARN810

Item No. 29595

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2E)-3-[4-[(1E)-2-(2-chloro-4-fluorophenyl)-1-(1H-indazol-5-yl)-1-buten-1-yl]phenyl]-2-propenoic acid
CAS Number
1365888-06-7
Synonyms
  • GDC-0810
  • RG-6046
Molecular Formula
C26H20ClFN2O2
Formula Weight
446.9
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 10mg/mLDMSO: 15mg/mLEthanol: 20mg/mLEthanol:PBS (pH 7.2) (1:4): 0.2mg/mL
SMILES
ClC1=C(/C(CC)=C(C2=CC=C(/C=C/C(O)=O)C=C2)/C3=CC(C=NN4)=C4C=C3)C=CC(F)=C1
InChi Code
InChI=1S/C26H20ClFN2O2/c1-2-21(22-10-9-20(28)14-23(22)27)26(18-8-11-24-19(13-18)15-29-30-24)17-6-3-16(4-7-17)5-12-25(31)32/h3-15H,2H2,1H3,(H,29,30)(H,31,32)/b12-5+,26-21+
InChi Key
BURHGPHDEVGCEZ-KJGLQBJMSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

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    25 mg

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    Cayman Chemical
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    Product Description

    ARN810 is a selective estrogen receptor degrader (SERD) that binds to ERα and ERβ (IC50s = 6.1 and 8.8 nM, respectively) and induces degradation of ERα in MCF-7 cells (EC50 = 0.7 nM).1 It inhibits ERα transcriptional activity induced by 17β-estradiol (Item No. 10006315) in a reporter assay and reduces MCF-7 breast cancer cell viability (IC50 = 2 nM). ARN810 (1 mg/kg, p.o.) inhibits 17β-estradiol-induced uterine weight gain in rats. It reduces tumor volume in tamoxifen-sensitive and -resistant MCF-7 mouse xenograft models in a dose-dependent manner.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Lai, A., Kahraman, M., Govek, S., et al. Identification of GDC-0810 (ARN-810), an orally bioavailable selective estrogen receptor degrader (SERD) that demonstrates robust activity in tamoxifen-resistant breast cancer xenografts. J. Med. Chem. 58(12), 4888-4904 (2015).