Giredestrant (Synonyms: GDC-9545) |
Catalog No.GC39630
One-Click Copy Product Info
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Giredestrant is an oral selective estrogen receptor (ER) degrader. Giredestrant can induce an inactive conformation of the estrogen receptor ligand binding domain and promoting proteasome-mediated degradation of the receptor protein. Giredestrant is used to treat estrogen receptor-positive (ER+) breast cancer.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1953133-47-5
Sample solution is provided at 25 µL, 10mM.
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Giredestrant is an oral selective estrogen receptor (ER) degrader. Giredestrant can induce an inactive conformation of the estrogen receptor ligand binding domain and promoting proteasome-mediated degradation of the receptor protein. Giredestrant is used to treat estrogen receptor-positive (ER+) breast cancer [1-5].
Giredestrant significantly degraded ERα protein and inhibited proliferation at low nanomolar concentrations (0.1nM, 1nM, 10nM, 100nM and 1μM, 24h) in a variety of ER+ breast cancer cell lines (MCF-7, T-47D, CAMA-1 and HCC1500) [5]. In T47D cells, treatment with Giredestrant (50nM, 6d) reduced T47D cell viability [6].
In the HCI-013PDX animal model, Giredestrant (1mg/kg, po, 29d) can strongly induce tumor regression, showing excellent anti-tumor potential [5]. In the HCI-013 PDX model, Giredestrant (30mg/kg, po, 28d) suppressed the mutant ERα-PR proliferation in the mammary gland more so than the standard-of-care agents, tamoxifen and fulvestrant [7]. In the transgenic Esr1 animal model, Giredestrant (30mg/kg, po, 4d) exhibited an antiproliferative response against ESR1 mutant tumors [8].
References:
[1]. Malhi V, Agarwal P, Gates MR, et al. Optimizing Early-stage Clinical Pharmacology Evaluation to Accelerate Clinical Development of Giredestrant in Advanced Breast Cancer. Cancer Research Communications. 2023 Dec 15; 3(12): 2551-2559.
[2]. Martín M, Lim E, Chavez-MacGregor M, et al. Giredestrant for estrogen receptor–positive, HER2-negative, previously treated advanced breast cancer: Results from the randomized, phase II acelERA breast cancer study. Journal of Clinical Oncology. 2024 Jun 20; 42(18): 2149-2160.
[3]. Jhaveri KL, Bellet M, Turner NC, et al. Phase Ia/b study of giredestrant±palbociclib and±luteinizing hormone-releasing hormone agonists in estrogen receptor–positive, HER2-negative, locally advanced/metastatic breast cancer. Clinical Cancer Research. 2024 Feb 16; 30(4): 754-766.
[4]. Pathak N, Oliveira M. New Oral Selective Estrogen Receptor Degraders Redefine Management of Estrogen Receptor–Positive Breast Cancer. Annual Review of Medicine. 2025 Jan 27; 76(1): 243-255.
[5]. Liang J, Zbieg JR, Blake RA, et al. GDC-9545 (Giredestrant): a potent and orally bioavailable selective estrogen receptor antagonist and degrader with an exceptional preclinical profile for ER+ breast cancer. Journal of Medicinal Chemistry. 2021 Jul 12; 64(16): 11841-11846.
[6]. Herrera-Abreu MT, Guan J, Khalid U, et al. Inhibition of GPX4 enhances CDK4/6 inhibitor and endocrine therapy activity in breast cancer. Nature Communications. 2024 Nov 5; 15(1): 9550.
[7]. Liang J, Ingalla ER, Yao X, et al. Giredestrant reverses progesterone hypersensitivity driven by estrogen receptor mutations in breast cancer. Science Translational Medicine. 2022 Sep 21; 14(663): eabo5959.
[8]. Liang J, Yao X, Aouad P, et al. ERα dysfunction caused by ESR1 mutations and therapeutic pressure promotes lineage plasticity in ER+ breast cancer. Nature Cancer. 2025 Jan 13: 1-5.
| Cell experiment [1]: | |
Cell lines | MCF-7 cells |
Preparation Method | MCF-7 cells were cultured in RPMI 1640 containing 10% FBS, in poly-lysine coated 384 well tissue culture plates for 24h and then treated with different concentrations of Giredestrant for 24h. |
Reaction Conditions | 0.1nM, 1nM, 10nM, 100nM and 1μM; 24h |
Applications | Giredestrant significantly degraded ERα protein and inhibited proliferation at low nanomolar concentrations (0.1nM, 1nM, 10nM, 100nM and 1μM, 24h) in MCF-7. |
| Animal experiment [2]: | |
Animal models | HCI-013 PDX model |
Preparation Method | Giredestrant was administered by oral gavage in HCI-013 PDX model at a dose of 30mg/kg once daily in a volume of 100μL per mouse for 28d. |
Dosage form | 30mg/kg; po; 28d |
Applications | Giredestrant suppressed the mutant ERα-PR proliferation in the mammary gland more so than the standard-of-care agents, tamoxifen and fulvestrant. |
References: | |
| Cas No. | 1953133-47-5 | SDF | |
| Synonyms | GDC-9545 | ||
| Canonical SMILES | OCC(F)(F)CN([C@@H]1C2=C(F)C=C(NC3CN(CCCF)C3)C=C2F)[C@H](C)CC4=C1NC5=C4C=CC=C5 | ||
| Formula | C27H31F5N4O | M.Wt | 522.55 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9137 mL | 9.5685 mL | 19.1369 mL |
| 5 mM | 382.7 μL | 1.9137 mL | 3.8274 mL |
| 10 mM | 191.4 μL | 956.8 μL | 1.9137 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 21 reference(s) in Google Scholar.)