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Giredestrant (tartrate)

  Cat. No.:  DC60185   Featured
Chemical Structure
2407529-33-1
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Field of application
Giredestrant, also known as GDC-9545 and RG6171, is a SERD. GDC-9545 is an orally available selective estrogen receptor degrader/downregulator (SERD), with potential antineoplastic activity. Upon oral administration, SERD GDC-9545 specifically targets and binds to the estrogen receptor (ER) and induces a conformational change that promotes ER degradation.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 2407529-33-1
Chemical Name: Giredestrant tartrate
Synonyms: Giredestrant (tartrate);Giredestrant tartrate;GDC 9545;GDC9545;GDC-9545
SMILES: FC(C([H])([H])O[H])(C([H])([H])N1[C@]([H])(C([H])([H])[H])C([H])([H])C2C3=C([H])C([H])=C([H])C([H])=C3N([H])C=2[C@@]1([H])C1C(=C([H])C(=C([H])C=1F)N([H])C1([H])C([H])([H])N(C([H])([H])C([H])([H])C([H])([H])F)C1([H])[H])F)F.O([H])[C@@]([H])(C(=O)O[H])[C@]([H])(C(=O)O[H])O[H]
Formula: C31H37F5N4O7
M.Wt: 672.65
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: [1]. C Metcalfe, et al. Abstract P5-04-07: GDC-9545: A novel ER antagonist and clinical candidate that combines desirable mechanistic and pre-clinical DMPK attributes.
Description: Giredestrant tartrate (GDC-9545 tartrate), a non-steroidal ER ligand, is an orally active and selective estrogen receptor (ER) antagonist. Giredestrant tartrate potently competes with estradiol for binding and induces a conformational change within the ER ligand binding domain. Anti-tumor activity[1].
Target: Estrogen receptor
In Vivo: Giredestrant (GDC-9545) tartrate is an ER antagonist that combines desirable mechanistic and pre-clinical DMPK attributes. The highly potent in vivo efficacy of Giredestrant likely arises due to the particular combination of high binding potency, full suppression of ER signaling, and an improved DMPK profile[1].
In Vitro: Giredestrant (GDC-9545) tartrate consistently induces ER turnover and drives deep transcriptional suppression of ER, resulting in robust in vitro anti-proliferative activity[1].
References: [1]. C Metcalfe, et al. Abstract P5-04-07: GDC-9545: A novel ER antagonist and clinical candidate that combines desirable mechanistic and pre-clinical DMPK attributes.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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