Identification | Back Directory | [Name]
GDC-0810(ARN-810) | [CAS]
1365888-06-7 | [Synonyms]
RG6046 RG-6046 RG 6046 ARN-810 CS-2080 GDC-0810 Brilanestrant) GDC-0810(ARN-810) ARN-810;BRILANESTRANT GDC-0810 (Brilanestrant) Brilanestrant (GDC-0810, ARN-810) (E)-3-(4-((E)-2-(2-CHLORO-4-FLUOROPHENYL)-1-(1H-INDAZOL-5-YL)BUT-1-EN-1-YL)PHENYL)ACRYLIC ACID GDC0810; GDC 0810; GDC-0810; ARN810; ARN 810; ARN-810; RG6046; RG-6046; RG 6046; BRILANESTRANT (E)-3-[4-[(E)-2-(2-Chloro-4-fluorophenyl)-1-(1H-indazol-5-yl)but-1-en-1-yl]phenyl]-2-propenoic acid 2-Propenoic acid, 3-[4-[(1E)-2-(2-chloro-4-fluorophenyl)-1-(1H-indazol-5-yl)-1-buten-1-yl]phenyl]-, (2E)- | [Molecular Formula]
C26H20ClFN2O2 | [MDL Number]
MFCD28902190 | [MOL File]
1365888-06-7.mol | [Molecular Weight]
446.9 |
Chemical Properties | Back Directory | [Boiling point ]
622.8±55.0 °C(Predicted) | [density ]
1.342±0.06 g/cm3(Predicted) | [solubility ]
DMSO:89.0(Max Conc. mg/mL);199.15(Max Conc. mM) Ethanol:89.0(Max Conc. mg/mL);199.15(Max Conc. mM) | [form ]
A solid | [pka]
13.94±0.40(Predicted) | [color ]
White to off-white |
Hazard Information | Back Directory | [Uses]
Brilanestrant is an orally bioavailable Selective Estrogen Receptor Degrader (SERD) that demonstrates robust activity in tamoxifen-resistant breast cancer xenografts. GDC-0810 functions by binding to the estrogen receptor, inducing a conformational change resulting in the degradation of the receptor. GDC-0810 or ARN-810 demonstrates robust activity in models of tamoxifen-sensitive and tamoxifen-resistant breast cancer, and is currently in clinical trials in women with locally advanced or metastatic estrogen receptor-positive breast cancer. |
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