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The cheapest Giredestrant (GDC-9545, CAS No.: 1953133-47-5) is for research use only. Significant discount for bulk order of Giredestrant (GDC-9545). Condition of sample preparation and optimal sample dilution should be determined experimentally by the investigator.
Price/availability/specifications subject to change without notice. Unless otherwise indicated, our catalog and customized products are for research use only and not intended for human or animal diagnostic or therapeutic use.
Phone: 1-617-401-8149
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CAS No.: 1953133-47-5 (CAS No. 2407529-33-1 for giredestrant tartrate)
IUPAC/Chemical 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
Molecular Formula: C27H31F5N4O
Molecular Weight: 522.55
Purity: >99.5% purity
QC: HPLC-MS, chiral HPLC and quantitative elemental analysis.
Solubility: Soluble in DMSO
Storage: Store at 0 °C (short term), -20 °C (long term), Desiccated
Note: Please contact us for COA, Spectra, and SDS information.
Background:
Giredestrant (GDC-9545, CAS No.: 1953133-47-5), a non-steroidal estrogen receptor (ER) ligand, is an orally active and selective estrogen receptor degrader/downregulator (SERD) with potential antineoplastic activity. Giredestrant potently competes with Estradiol for binding and induces a conformational change within the ER ligand binding domain. Upon oral administration, GDC-9545 specifically targets and binds to ER and induces a conformational change to promote ER degradation, which prevents ER-mediated signaling and inhibits both the growth and survival of ER-expressing cancer cells.
Orally given, giredestrant delivers a strong clinical efficacy and safety profile and has shown superior pre-clinical potency over other SERDs in development. The oral administration of giredestrant has the potential to transform the treatment experience for patients, offering greater convenience and a less painful option compared to therapies administered via intramuscular injection.
Giredestrant has a comprehensive development programme across a broad range of settings and treatment combinations for patients with HR-positive, HER2-negative breast cancer. A standardised once-daily 30mg dose has been selected for the giredestrant development programme, both as a monotherapy and in combination studies.
Selective estrogen receptor degrader Giredestrant (GDC-9545) was synthesized in a longest linear sequence of six steps in 37% overall yield with 99% HPLC purity without chromatographic purification. The synthesis features a Friedel–Crafts indole functionalization, a strain-release aminoazetidine formation, a diastereoselective Pictet–Spengler reaction (98% yield, 95:5 dr) to assemble the tetrahydrocarboline core, and a highly efficient Pd-catalyzed C–N coupling (90% yield) using [t-BuBrettPhos Pd(allyl)]OTf as the catalyst and DBU as the base.[5]
Target: estrogen receptor (ER)
In Vitro: Giredestrant (GDC-9545) is a novel estrogen receptor (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]
How to make giredestrant stock solutions in vitro?
Reference:
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