Cas Number: | 2088518-51-6 |
Pubchem: | 129205616 |
Chemspiderid: | 76743881 |
Unii: | W3Y784Y0ES |
Kegg: | D11736 |
Chembl: | 4059888 |
Synonyms: | G1T48 |
Iupac Name: | (E)-3-[4-[2-(4-fluoro-2,6-dimethyl-benzoyl)-6-hydroxy-benzothiophen-3-yl]oxyphenyl]prop-2-enoic acid |
C: | 26 |
H: | 19 |
F: | 1 |
O: | 5 |
S: | 1 |
Smiles: | CC1=CC(=CC(=C1C(=O)C2=C(C3=C(S2)C=C(C=C3)O)OC4=CC=C(C=C4)/C=C/C(=O)O)C)F |
Stdinchi: | InChI=1S/C26H19FO5S/c1-14-11-17(27)12-15(2)23(14)24(31)26-25(20-9-6-18(28)13-21(20)33-26)32-19-7-3-16(4-8-19)5-10-22(29)30/h3-13,28H,1-2H3,(H,29,30)/b10-5+ |
Stdinchikey: | KOAITBOFZOEDOC-BJMVGYQFSA-N |
Rintodestrant is an orally bioavailable selective estrogen receptor degrader (SERD) developed by G1 Therapeutics for the treatment of estrogen receptor-positive (ER+) breast cancer. Structurally inspired by the 6-OH-benzothiophene scaffold used in arzoxifene and raloxifene, rintodestrant selectively binds to the estrogen receptor and inhibits ER signaling, demonstrating efficacy in endocrine-resistant tumors.[1]
A phase I clinical trial evaluated rintodestrant as monotherapy and in combination with the CDK4/6 inhibitor palbociclib in patients with ER+/HER2- advanced breast cancer.