2407529-33-1
Chemical Structure
Giredestrant tartrate
Synonym(s): GDC-9545 tartrate; RG6171 tartrate
- CAS No.: 2407529-33-1
- Formula:C31H37F5N4O7
- Molecular Weight:672.64
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 (2R,3R)-2,3-dihydroxysuccinate
InChIKey: QZOTWXMHTSEIJY-WULFPPIKSA-N
SMILES: C[C@H](C1)N(CC(F)(F)CO)[C@H](C2=C(F)C=C(NC3CN(CCCF)C3)C=C2F)C4=C1C5=C(N4)C=CC=C5.OC([C@H](O)[C@@H](O)C(O)=O)=O
Biological Activity: Giredestrant tartrate (GDC-9545 tartrate) is an orally active, full, selective Estrogen receptor α (ERα) degrader and antagonist with a DC50 of 0.03 nM. Giredestrant tartrate promotes the degradation of ERα protein, including the ESR1Y537S mutant ERα. Giredestrant tartrate reduces uterine wet weight in immature rats and induces a low cuboidal phenotype in their endometrial epithelium. Giredestrant tartrate induces tumor regression in both ESR1Y537S mutant and wild-type ERα tumor models. Giredestrant tartrate can be used for the research of ER+ breast cancer[1].
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Giredestrant tartrate | Giredestrant tartrate (GDC-9545 tartrate) is an orally active, full, selective Estrogen receptor α (ERα) degrader and antagonist with a DC50 of 0.03 nM. Giredestrant tartrate promotes the degradation of ERα protein, including the ESR1Y537S mutant ERα. Giredestrant tartrate reduces uterine wet weight in immature rats and induces a low cuboidal phenotype in their endometrial epithelium. Giredestrant tartrate induces tumor regression in both ESR1Y537S mutant and wild-type ERα tumor models. Giredestrant tartrate can be used for the research of ER+ breast cancer. | |||||||||||||||||||||
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Keywords
