GDC-0927 Racemate
GDC-0927 Racemate (SRN-927 Racemate) is an estrogen receptor (ER) degrader that can effectively inhibit the activity of ER-α with an IC50 value of 0.2 nM and can be used in diseases related to estrogen receptors.
For research use only. We do not sell to patients.
- CAS No.: 1443983-36-5
- Formula: C28H28FNO4
- Molecular Weight:461.52
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
IC50: 0.2 nM (ER-α)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | IC50 |
0.2 nM
Compound: 17h
|
Antiproliferative activity against human MCF7 cells after 5 days by CellTiter-Glo assay
Antiproliferative activity against human MCF7 cells after 5 days by CellTiter-Glo assay
|
[PMID: 30655946] |
| MCF7 | IC50 |
0.2 nM
Compound: 42
|
Antiproliferative activity against human MCF7 cells
Antiproliferative activity against human MCF7 cells
|
[PMID: 35567964] |
| MCF7 | IC50 |
0.3 nM
Compound: 17h
|
Induction of ERalpha degradation in human MCF7 cells assessed as decrease in ERalpha protein level after 4 hrs by InCell Western assay
Induction of ERalpha degradation in human MCF7 cells assessed as decrease in ERalpha protein level after 4 hrs by InCell Western assay
|
[PMID: 30655946] |
In Vitro
GDC-0927 Racemate (Example 1) is a degrader of estrogen receptor, potently inhibits ER-α activity, with an IC50 of 0.2 nM, and is used in the research of ER-related diseases. GDC-0927 Racemate reduces the viability of MCF7 cells with an IC50 of 0.21 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 1443983-36-5
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Molecular Weight 461.52
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Formula C28H28FNO4
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SMILES
OC1=CC=C2C(C(C)=C(C3=CC=CC(O)=C3)C(C4=CC=C(OCCN5CC(CF)C5)C=C4)O2)=C1
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Synonyms
SRN-927 Racemate
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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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)