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GDC-0927

Chemical Structure : GDC-0927

CAS No.: 1642297-01-5

GDC-0927 (GDC0927, SRN-927, RG6047)

Catalog No.: PC-63294Not For Human Use, Lab Use Only.

GDC-0927 (SRN-927, RG6047) is a potent, orally bioavailable, selective estrogen receptor degrader (SERD) with IC50 of 0.1 nM (ER-α degradation) and Emax=97%.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

GDC-0927 (SRN-927, RG6047) is a potent, orally bioavailable, selective estrogen receptor degrader (SERD) with IC50 of 0.1 nM (ER-α degradation) and Emax=97%.
GDC-0927 exhibits IC50 value of 0.1 nM in MCF-7 proliferation assays.
GDC-0927 (100 mg/kg, po) demonstrated tumor regression, together with robust reduction intratumoral ER-α levels in tamoxifen-resistant breast cancer xenograft models.

Physicochemical Properties

M.Wt 461.533
Formula C28H28FNO4
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-2-(4-(2-(3-(fluoromethyl)azetidin-1-yl)ethoxy)phenyl)-3-(3-hydroxyphenyl)-4-methyl-2H-chromen-6-ol

References

1. Kahraman M, et al. ACS Med Chem Lett. 2018 Dec 6;10(1):50-55.

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