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Medchemexpress LLC Brilanestrant | 1365888-06-7 | 99.9% | 50 MG
Supplier: Medchemexpress LLC HY1286450MG
Brilanestrant is an orally bioavailable selective estrogen receptor degrader (SERD) with an IC50 of 0.7 nM. It acts as a potent ER-α binder (IC50=6.1 nM) and a full transcriptional antagonist with no agonism (3x ERE, IC50=2 nM). It demonstrates good potency and efficacy in ER-α degradation (EC50=0.7 nM) and MCF-7 breast cancer cell viability (IC50=2.5 nM) assays.
- Orally bioavailable selective estrogen receptor degrader (SERD)
- Potent ER-α binder (IC50=6.1 nM)
- Full transcriptional antagonist with no agonism
- Induces a distinct ERα conformation
- Does not show tamoxifen-like ER agonism in MCF7 cells
- Low clearance and good bioavailability (40%-60%)
- Substantial tumor-growth inhibition in tamoxifen-sensitive MCF-7 xenograft model
- Displays dose-dependent efficacy in MCF7 xenograft model
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