Giredestrant tartrate

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.

Product information

CAS Number: 2407529-33-1

Molecular Weight: 672.64

Formula: C31H37F5N4O7

Chemical Name: (2R,3R)-2,3-dihydroxybutanedioic acid; 3-[(1R,3R)-1-(2,6-difluoro-4-{[1-(3-fluoropropyl)azetidin-3-yl]amino}phenyl)-3-methyl-1H,2H,3H,4H,9H-pyrido[3,4-b]indol-2-yl]-2,2-difluoropropan-1-ol

Smiles: C[C@@H]1CC2=C(NC3=CC=CC=C23)[C@@H](C2C(F)=CC(=CC=2F)NC2CN(CCCF)C2)N1CC(F)(F)CO.OC(=O)[C@H](O)[C@@H](O)C(O)=O

InChiKey: QZOTWXMHTSEIJY-WULFPPIKSA-N

InChi: InChI=1S/C27H31F5N4O.C4H6O6/c1-16-9-20-19-5-2-3-6-23(19)34-25(20)26(36(16)14-27(31,32)15-37)24-21(29)10-17(11-22(24)30)33-18-12-35(13-18)8-4-7-28;5-1(3(7)8)2(6)4(9)10/h2-3,5-6,10-11,16,18,26,33-34,37H,4,7-9,12-15H2,1H3;1-2,5-6H,(H,7,8)(H,9,10)/t16-,26-;1-,2-/m11/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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.

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.

Products are for research use only. Not for human use.