Rintodestrant

• CAT Number: I035591
• CAS Number: 2088518-51-6
• Molecular Formula: C26H19FO5S
• Molecular Weight: 462.49
• Purity: 98%
• Synonyms: Rintodestrant; G1T48; G1T 48; G1T-48; G1 T48; G1-T 48; G1-T-48
• Solubility: Soluble in DMSO
• Storage: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
• IUPAC Name: (E)-3-(4-((2-(4-fluoro-2,6-dimethylbenzoyl)-6-hydroxybenzo[b]thiophen-3-yl)oxy)phenyl)acrylic acid
• InChI: 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+
• InChIKey: KOAITBOFZOEDOC-BJMVGYQFSA-N
• SMILES: OC1=CC=C2C(SC(C(C3=C(C=C(C=C3C)F)C)=O)=C2OC4=CC=C(C=C4)/C=C/C(O)=O)=C1

Rintodestrant（Cat No.:I035591） is a non-steroidal selective estrogen receptor degrader (SERD) that can be used in the treatment of breast cancer. It acts by binding to the estrogen receptor and targeting it for degradation, leading to reduced tumor growth. It is effective in preclinical studies against breast cancer that is resistant to current therapies, including tamoxifen and aromatase inhibitors. Rintodestrant has been granted orphan drug designation by the US FDA for the treatment of advanced estrogen receptor-positive breast cancer.

Reference

Andreano KJ, Wardell SE, Baker JG, et al. G1T48, an oral selective estrogen receptor degrader, and the CDK4/6 inhibitor lerociclib inhibit tumor growth in animal models of endocrine-resistant breast cancer. Breast Cancer Res Treat. 2020;180(3):635–646. doi:10.1007/s10549-020-05575-9