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GDC-0810

  Cat. No.:  DC23161   Featured
Chemical Structure
1365888-06-7
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Field of application
GDC-0810 (ARN-810, Brilanestrant) is a non-steroidal, orally bioavailable selective estrogen receptor degrader (SERD) with IC50 of 0.7 nM (ER-α degradation), binds to ERα and ERβ with with Ki of 3.8 and 3.7 nM, respectively.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1365888-06-7
Chemical Name: 2-Propenoic acid, 3-[4-[(1E)-2-(2-chloro-4-fluorophenyl)-1-(1H-indazol-5-yl)-1-buten-1-yl]phenyl]-, (2E)-
Synonyms: ARN-810;Brilanestrant
SMILES: O=C(C=CC1C=CC(C(=C(CC)C2C(Cl)=CC(F)=CC=2)C2C=CC3NN=CC=3C=2)=CC=1)O
Formula: C26H20ClFN2O2
M.Wt: 446.9006
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: GDC-0810 is an orally bioavailable selective estrogen receptor degrader (SERD) with IC50 of 0.7 nM.
In Vivo: The pharmacokinetic profile of GDC-0810 shows it is a olw clearance molecule across species, with good bioavailability (40%-60%). GDC-0810 (3 mg/kg, p.o.) shows substantial tumor-growth inhibition in a tamoxifen-sensitive MCF-7 xenograft model, while at the highest dose of 100 mg/kg/day, all animals show tumor regression of more than 50% without weight loss[1]. GDC-0810 exhibits low clearance (11 mL/min/kg) and 61% oral bioavailability. GDC-0810 (1-100 mg/kg/day, p.o.) displays dose dependent efficacy in the MCF7 xenograft model[2].
In Vitro: GDC-0810 is a potent ER-α binder (IC50=6.1 nM), a full transcriptional antagonist with no agonism (3× ERE, IC50=2 nM), and displays good potency and efficacy in ER-α degradation (EC50=0.7 nM) and MCF-7 breast cancer cell viability (IC50=2.5 nM) assays[1]. GDC-0810 induces a distinct ERα conformation versus tamoxifen and other ER therapeutics, and does not exhibit tamoxifen-like ER agonism in MCF7 cells[2].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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