WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 206041
CAS#: 1365888-06-7
Description: Brilanestrant, also known as GDC-0810, ARN-810 and RG6046, 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.
MedKoo Cat#: 206041
Name: Brilanestrant
CAS#: 1365888-06-7
Chemical Formula: C26H20ClFN2O2
Exact Mass: 446.11973
Molecular Weight: 446.9064
Elemental Analysis: C, 69.88; H, 4.51; Cl, 7.93; F, 4.25; N, 6.27; O, 7.16
Synonym: GDC0810; GDC 0810; GDC-0810; ARN810; ARN 810; ARN-810; RG6046; RG-6046; RG 6046; Brilanestrant
IUPAC/Chemical Name: (E)-3-(4-((E)-2-(2-chloro-4-fluorophenyl)-1-(1H-indazol-5-yl)but-1-en-1-yl)phenyl)acrylic acid
InChi Key: BURHGPHDEVGCEZ-KJGLQBJMSA-N
InChi Code: InChI=1S/C26H20ClFN2O2/c1-2-21(22-10-9-20(28)14-23(22)27)26(18-8-11-24-19(13-18)15-29-30-24)17-6-3-16(4-7-17)5-12-25(31)32/h3-15H,2H2,1H3,(H,29,30)(H,31,32)/b12-5+,26-21+
SMILES Code: O=C(O)/C=C/C1=CC=C(C=C1)/C(C2=CC3=C(NN=C3)C=C2)=C(CC)\C4=CC=C(C=C4Cl)F
1: Lai A, Kahraman M, Govek S, Nagasawa J, Bonnefous C, Julien J, Douglas K, Sensintaffar J, Lu N, Lee KJ, Aparicio A, Kaufman J, Qian J, Shao G, Prudente R, Moon MJ, Joseph JD, Darimont B, Brigham D, Grillot K, Heyman R, Rix PJ, Hager JH, Smith ND. Identification of GDC-0810 (ARN-810), an orally bioavailable Selective Estrogen Receptor Degrader (SERD) that demonstrates robust activity in tamoxifen-resistant breast cancer xenografts. J Med Chem. 2015 Apr 16. [Epub ahead of print] PubMed PMID: 25879485.
