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  3. Giredestrant

Giredestrant (Synonyms: GDC-9545)

Cat. No.: HY-109176
Handling Instructions

Giredestrant (GDC-9545), a non-steroidal ER ligand, is an orally active and selective estrogen receptor (ER) antagonist. Giredestrant potently competes with estradiol for binding and induces a conformational change within the ER ligand binding domain. Giredestrant has anti-tumor activity.

For research use only. We do not sell to patients.

Giredestrant Chemical Structure

Giredestrant Chemical Structure

CAS No. : 1953133-47-5

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Description

Giredestrant (GDC-9545), a non-steroidal ER ligand, is an orally active and selective estrogen receptor (ER) antagonist. Giredestrant potently competes with estradiol for binding and induces a conformational change within the ER ligand binding domain. Giredestrant has anti-tumor activity[1].

IC50 & Target[1]

ER

 

In Vitro

Giredestrant (GDC-9545) is a novel ER antagonist and clinical candidate 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].

Molecular Weight

522.55

Formula

C₂₇H₃₁F₅N₄O

CAS No.

1953133-47-5

SMILES

OCC(F)(F)CN([[email protected]@H]1C2=C(F)C=C(NC3CN(CCCF)C3)C=C2F)[[email protected]](C)CC4=C1NC5=C4C=CC=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (191.37 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9137 mL 9.5685 mL 19.1369 mL
5 mM 0.3827 mL 1.9137 mL 3.8274 mL
10 mM 0.1914 mL 0.9568 mL 1.9137 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.78 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (4.78 mM); Suspended solution; Need ultrasonic

*All of the co-solvents are provided by MCE.
References
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Keywords:

GiredestrantGDC-9545GDC9545GDC 9545Estrogen Receptor/ERRnon-steroidalERligandorallyconformationalchangeanti-tumorInhibitorinhibitorinhibit

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Giredestrant
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