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Chemical Structure : GDC-0810
CAS No.: 1365888-06-7
Catalog No.: PC-43264Not For Human Use, Lab Use Only.
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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $85 | In stock | |
| 25 mg | $225 | In stock | |
| 100 mg | $545 | In stock | |
| 500 mg | Get quote |
Bulk size, bulk discount!
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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; 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
| M.Wt | 446.9006 | |
| Formula | C26H20ClFN2O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
DMSO: ≥ 30 mg/mL |
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| Chemical Name/SMILES |
2-Propenoic acid, 3-[4-[(1E)-2-(2-chloro-4-fluorophenyl)-1-(1H-indazol-5-yl)-1-buten-1-yl]phenyl]-, (2E)- |
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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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