GDC-0810(ARN-810)
GDC-0810(ARN-810) Basic information
- Product Name:
- GDC-0810(ARN-810)
- Synonyms:
-
- (E)-3-(4-((E)-2-(2-CHLORO-4-FLUOROPHENYL)-1-(1H-INDAZOL-5-YL)BUT-1-EN-1-YL)PHENYL)ACRYLIC ACID
- GDC-0810 (Brilanestrant)
- GDC-0810(ARN-810)
- GDC-0810
- (E)-3-[4-[(E)-2-(2-Chloro-4-fluorophenyl)-1-(1H-indazol-5-yl)but-1-en-1-yl]phenyl]-2-propenoic acid
- ARN-810
- ARN-810;BRILANESTRANT
- CS-2080
- CAS:
- 1365888-06-7
- MF:
- C26H20ClFN2O2
- MW:
- 446.9
- Mol File:
- 1365888-06-7.mol
GDC-0810(ARN-810) Chemical Properties
- 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
GDC-0810(ARN-810) Usage And Synthesis
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.
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[1].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[2].
GDC-0810(ARN-810)Supplier
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