1953133-47-5
Chemical Structure
Giredestrant
Synonym(s): GDC-9545; RG6171
- CAS No.: 1953133-47-5
- Formula:C27H31F5N4O
- Molecular Weight:522.55
IUPAC Name: 3-((1R,3R)-1-(2,6-difluoro-4-((1-(3-fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol
InChIKey: GQCXHIKRWBIQMD-AKJBCIBTSA-N
SMILES: OCC(F)(F)CN([C@@H]1C2=C(F)C=C(NC3CN(CCCF)C3)C=C2F)[C@H](C)CC4=C1NC5=C4C=CC=C5
Biological Activity: Giredestrant (GDC-9545) is an orally active, full, selective Estrogen receptor α (ERα) degrader and antagonist with a DC50 of 0.03 nM. Giredestrant promotes the degradation of ERα protein, including the ESR1Y537S mutant ERα. Giredestrant reduces uterine wet weight in immature rats and induces a low cuboidal phenotype in their endometrial epithelium. Giredestrant induces tumor regression in both ESR1Y537S mutant and wild-type ERα tumor models. Giredestrant can be used for the research of ER+ breast cancer[1].
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Giredestrant | 98.98% | Giredestrant (GDC-9545) is an orally active, full, selective Estrogen receptor α (ERα) degrader and antagonist with a DC50 of 0.03 nM. Giredestrant promotes the degradation of ERα protein, including the ESR1Y537S mutant ERα. Giredestrant reduces uterine wet weight in immature rats and induces a low cuboidal phenotype in their endometrial epithelium. Giredestrant induces tumor regression in both ESR1Y537S mutant and wild-type ERα tumor models. Giredestrant can be used for the research of ER+ breast cancer. | ||||||||||||||||||||
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Giredestrant (Standard) | ≥98% | Giredestrant (Standard) (GDC-9545 (Standard); RG6171 (Standard)) is the analytical standard of Giredestrant (HY-109176). This product is intended for research and analytical applications. Giredestrant (GDC-9545) is an orally active, full, selective Estrogen receptor α (ERα) degrader and antagonist with a DC50 of 0.03 nM. Giredestrant promotes the degradation of ERα protein, including the ESR1Y537S mutant ERα. Giredestrant reduces uterine wet weight in immature rats and induces a low cuboidal phenotype in their endometrial epithelium. Giredestrant induces tumor regression in both ESR1Y537S mutant and wild-type ERα tumor models. Giredestrant can be used for the research of ER+ breast cancer. | ||||||||||||||||||||
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