Giredestrant tartrate
Based on 6 publication(s) in Google Scholar
Giredestrant tartrate (GDC-9545 tartrate) is an orally active, full, selective Estrogen receptor α (ERα) degrader and antagonist with a DC50 of 0.03 nM. Giredestrant tartrate promotes the degradation of ERα protein, including the ESR1Y537S mutant ERα. Giredestrant tartrate reduces uterine wet weight in immature rats and induces a low cuboidal phenotype in their endometrial epithelium. Giredestrant tartrate induces tumor regression in both ESR1Y537S mutant and wild-type ERα tumor models. Giredestrant tartrate can be used for the research of ER+ breast cancer.
For research use only. We do not sell to patients.
- CAS No.: 2407529-33-1
- Formula: C31H37F5N4O7
- Molecular Weight:672.64
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Giredestrant tartrate
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Biological Activity
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ERα 0.03 nM (DC50) |
Giredestrant tartrate potently inhibits ERα-mediated luciferase activity in T-47D wild-type breast cancer cells, with an IC50 of 0.05 nM[1].
Giredestrant tartrate potently degrades ERα in MCF-7 wild-type breast cancer cells, with a DC50 of 0.03 nM and a maximum degradation efficiency of 101%[1].
Giredestrant tartrate inhibits the proliferation of MCF-7 wild-type breast cancer cells, with an EC50 of 0.4 nM[1].
Giredestrant (0.1 nM-1 μM; 24 h) tartrate induces significant ERα degradation in ER+ breast cancer cell lines including CAMA-1, EFM-19, HCC1500, MCF-7, MDA-MB-134VI, MDA-MB-330 and T-47D starting at a concentration of 0.1 nM, and exhibits higher efficiency than GDC-0810 (HY-12864) and GDC-0927 (HY-111484)[1].
Giredestrant (1 nM; 0.5-24 h) tartrate promotes rapid degradation of ERα in MCF-7 breast cancer cells, with a half-life of 1.8 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:CAMA-1, EFM-19, HCC1500, MCF-7, MDA-MB-134VI, MDA-MB-330, T-47D ER+ breast cancer cell lines
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Concentration:0.1 nM, 1 nM, 10 nM, 100 nM, 1 μM
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Incubation Time:24 h
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Result:Promoted significant ERα degradation across all seven tested cell lines, starting at the lowest concentration of 0.1 nM.
Was a more efficient degrader than fulvestrant, GDC-0810, and GDC-0927 in all cell lines.
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Cell Line:MCF-7 wild-type breast cancer cells
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Concentration:1 nM
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Incubation Time:0.5, 1, 2, 4, 6, 24 h
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Result:Promoted rapid ERα turnover with a half-life of 1.8 h, which was faster than GDC-0927 (6.0 h) and GDC-0810 (16.5 h), and comparable to Fulvestrant (HY-13636) (2.2 h).
Induced the highest ERα degradation at 24 h among the tested compounds.
Giredestrant (0.1-1 mg/kg; p.o.; once daily; for 29 consecutive days) tartrate induces tumor regression in the ESR1Y537S-mutant ER+ breast cancer PDX model, even when administered at a daily oral dose as low as 0.1 mg/kg[1].
Giredestrant (3 mg/kg; p.o.; once daily; for 26 consecutive days) tartrate inhibits the growth of wild-type ER+ breast cancer xenografts by up to 79%; when combined with Palbociclib (HY-50767), it induces a maximum tumor regression of 108%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Immature female rats[1]
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Dosage:0.1 mg/kg; 10 mg/kg
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Administration:p.o.; daily; 4 days
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Result:Caused a statistically significant reduction in the ratio of uterine wet weight to body weight at 10 mg/kg, comparable to the positive control SERD 11.
Induced low cuboidal uterine epithelial cells at 10 mg/kg, consistent with inverse agonism.
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Animal Model:Immunocompromised mice (PDX model host)[1]
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Dosage:0.1 mg/kg; 1 mg/kg
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Administration:p.o.; daily; 29 days
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Result:Suppressed tumor growth at 0.1 mg/kg and 1 mg/kg.
Induced tumor regression at 1 mg/kg, comparable to the positive control SERD 11 at 100 mg/kg.
Achieved 1 mg/kg efficacy with 10-fold lower plasma concentration than SERD 11 at 100 mg/kg, while promoting 1.8-fold higher ERα turnover.
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Animal Model:Immunocompromised mice (xenograft model host)[1]
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Dosage:3 mg/kg (single agent); 3 mg/kg (in combination with palbociclib 50 mg/kg)
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Administration:p.o.; daily; 26 days
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Result:Inhibited tumor growth by 79% as a single agent at 3 mg/kg.
Induced tumor regression up to 108% after 24 days when combined with palbociclib at 3 mg/kg, outperforming the combination of fulvestrant and palbociclib.
Resulted in well-tolerated treatments across all groups.
Chemical Information
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CAS No. 2407529-33-1
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Molecular Weight 672.64
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Formula C31H37F5N4O7
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SMILES
C[C@H](C1)N(CC(F)(F)CO)[C@H](C2=C(F)C=C(NC3CN(CCCF)C3)C=C2F)C4=C1C5=C(N4)C=CC=C5.OC([C@H](O)[C@@H](O)C(O)=O)=O
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Synonyms
GDC-9545 tartrate; RG6171 tartrate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (6)
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Journal Impact Factor
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Most Recent
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Cancer Discov
2024 Feb 8;14(2):274-289. PMID: 37982575 -
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bioRxiv
Targeting Unique Ligand Binding Domain Structural Features Downregulates DKK1 in Y537S ESR1 Mutant Breast Cancer Cells. [Abstract]2024 Jun 2:2024.05.28.596307. PMID: 38854123 -
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Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Giredestrant tartrate Related Classifications
HY-135903 Related Classifications
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- Giredestrant
- 2407529-33-1
- GDC-9545
- RG6171
- GDC9545
- GDC 9545
- RG 6171
- RG-6171
- Estrogen Receptor/ERR
- immature rats
- human liver microsomes
- T-47D wild-type breast cancer cells
- MCF-7 wild-type breast cancer cells
- ER+ breast cancer cells
- ERα
- ESR1 Y537S mutant ERα
- hERG channels
- estrogen receptor alpha
- rat liver microsomes
- Inhibitor
- inhibitor
- inhibit