
GDC-0810
CAS No. 1365888-06-7
GDC-0810( ARN-810 | Brilanestrant )
Catalog No. M11510 CAS No. 1365888-06-7
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).
Purity : >98% (HPLC)






Size | Price / USD | Stock | Quantity |
2MG | 63 | In Stock |
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5MG | 97 | In Stock |
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10MG | 138 | In Stock |
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25MG | 246 | In Stock |
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50MG | 405 | In Stock |
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100MG | 582 | In Stock |
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Biological Information
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Product NameGDC-0810
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NoteResearch use only, not for human use.
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Brief DescriptionGDC-0810 (ARN-810, Brilanestrant) is a non-steroidal, orally bioavailable selective estrogen receptor degrader (SERD) with IC50 of 0.7 nM (ER-α degradation).
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DescriptionGDC-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; dually antagonizes and induces proteasome-dependent degradation of ERα, exhibits robust in vitro activity against a variety of human breast cancer cell lines (MCF7 cell IC50=25 nM); demonstrates robust activity in models of tamoxifen-sensitive and tamoxifen-resistant breast cancer models.Breast Cancer Phase 1 Discontinued(In Vitro):Brilanestrant (ARN-810; 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.Brilanestrant (ARN-810; GDC-0810) induces a distinct ERα conformation versus tamoxifen and other ER therapeutics, and does not exhibit tamoxifen-like ER agonism in MCF7 cells.(In Vivo):The pharmacokinetic profile of Brilanestrant (ARN-810) shows it is a olw clearance molecule across species, with good bioavailability (40%-60%). Brilanestrant (ARN-810) (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.Brilanestrant (ARN-810) exhibits low clearance (11 mL/min/kg) and 61% oral bioavailability. Brilanestrant (ARN-810) (1-100 mg/kg/day, p.o.) displays dose dependent efficacy in the MCF7 xenograft model.
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In VitroBrilanestrant (ARN-810; 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.Brilanestrant (ARN-810; GDC-0810) induces a distinct ERα conformation versus tamoxifen and other ER therapeutics, and does not exhibit tamoxifen-like ER agonism in MCF7 cells.
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In VivoThe pharmacokinetic profile of Brilanestrant (ARN-810) shows it is a olw clearance molecule across species, with good bioavailability (40%-60%). Brilanestrant (ARN-810) (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.Brilanestrant (ARN-810) exhibits low clearance (11 mL/min/kg) and 61% oral bioavailability. Brilanestrant (ARN-810) (1-100 mg/kg/day, p.o.) displays dose dependent efficacy in the MCF7 xenograft model.
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SynonymsARN-810 | Brilanestrant
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PathwayEndocrinology/Hormones
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TargetEstrogen Receptor/ERR
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RecptorERα
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Research AreaCancer
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IndicationBreast Cancer
Chemical Information
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CAS Number1365888-06-7
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Formula Weight446.9006
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Molecular FormulaC26H20ClFN2O2
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Purity>98% (HPLC)
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SolubilityDMSO: ≥ 30 mg/mL
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SMILESCCC(=C(C1=CC=C(C=C1)C=CC(=O)O)C2=CC3=C(C=C2)NN=C3)C4=C(C=C(C=C4)F)Cl
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Chemical Name2-Propenoic acid, 3-[4-[(1E)-2-(2-chloro-4-fluorophenyl)-1-(1H-indazol-5-yl)-1-buten-1-yl]phenyl]-, (2E)-
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Lai A, et al. J Med Chem. 2015 Jun 25;58(12):4888-904.
2. Joseph JD, et al. Elife. 2016 Jul 13;5. pii: e15828.
3. Wang Y, et al. Clin Cancer Res. 2017 Jun 15;23(12):3053-3060.
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