Giredestrant tartrate

SKU: orb1709734

Description

Giredestrant tartrate is a potent, orally bioavailable, non-steroidal estrogen receptor (ER) antagonist that induces ER degradation and blocks transcriptional activity. It is a research tool for studying ER-positive cancers, with applications in both in vitro mechanistic studies and in vivo xenograft models of breast tumorigenesis.

Research Area

Metabolism Research

Key Properties

• CAS Number: 2407529-33-1
• MW: 672.64
• Purity: 98.01%
• Formula: C₃₁H₃₇F₅N₄O₇
• SMILES: [C@@H]([C@H](C(O)=O)O)(C(O)=O)O.C(C(CO)(F)F)N1[C@@H](C2=C(C=3C(N2)=CC=CC3)C[C@H]1C)C4=C(F)C=C(NC5CN(CCCF)C5)C=C4F
• Target: Estrogen Receptor/ERR
• Solubility: DMSO:55 mg/mL (81.77 mM)

Bioactivity

• In Vitro:
  Estrogen receptor antagonist 1 shows weak metabolism dependent inhibition of CYP2C9.Estrogen receptor antagonist 1 directly inhibits CYP3A4 with IC50 values of 6.5 µM (midazolam 1'-hydroxylation) and 26 µM (testosterone 6β-hydroxylation); IC50 for CYP2B6 and CYP2C8 inhibition were 13 µM and 21 µM, respectively.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Estrogen receptor, Estrogen Receptor, Estrogen Receptor/ERR, Estrogen receptor antagonist 1, EstrogenReceptor, Giredestrant Tartrate, ERR

Compound Identifiers

PubChem CID

146026191