ChemicalBook > CAS DataBase List > GDC-0810(ARN-810)
GDC-0810(ARN-810)
- Product Name
- GDC-0810(ARN-810)
- CAS No.
- 1365888-06-7
- Chemical Name
- GDC-0810(ARN-810)
- Synonyms
- RG6046;RG 6046;ARN-810;CS-2080;RG-6046;GDC-0810;Brilanestrant);GDC-0810(ARN-810);ARN-810;BRILANESTRANT;GDC-0810 (Brilanestrant)
- CBNumber
- CB93040499
- Molecular Formula
- C26H20ClFN2O2
- Formula Weight
- 446.9
- MOL File
- 1365888-06-7.mol
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GDC-0810(ARN-810) Property
- 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
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N-Bromosuccinimide Price
Cayman Chemical
- Product number
- 29595
- Product name
- ARN810
- Packaging
- 5mg
- Price
- $120
- Updated
- 2024/03/01
Cayman Chemical
- Product number
- 29595
- Product name
- ARN810
- Packaging
- 25mg
- Price
- $510
- Updated
- 2024/03/01
Cayman Chemical
- Product number
- 29595
- Product name
- ARN810
- Packaging
- 1mg
- Price
- $36
- Updated
- 2024/03/01
Cayman Chemical
- Product number
- 29595
- Product name
- ARN810
- Packaging
- 10mg
- Price
- $223
- Updated
- 2024/03/01
TRC
- Product number
- B677393
- Product name
- Brilanestrant
- Packaging
- 10mg
- Price
- $210
- Updated
- 2021/12/16
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GDC-0810(ARN-810) Chemical Properties,Usage,Production
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) Preparation Products And Raw materials
Raw materials
Preparation Products
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