GSPT1 degrader-4
GSPT1 degrader-4 is a GSPT1 molecular glue degrader that recruits cereblon (CRBN), with a DC50 of 25.4 nM. GSPT1 degrader-4 inhibits the proliferation of cancer cells. GSPT1 degrader-4 is applicable to breast cancer-related research.
For research use only. We do not sell to patients.
- CAS No.: 3034764-32-1
- Formula: C24H21ClN4O5
- Molecular Weight:480.90
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Eukaryotic Release Factor (eRF) Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
eRF3a/GSPT1 25.4 nM (DC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CAL-51 | IC50 |
39 nM
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Concentration-dependent inhibition of cell proliferation in a CAL51 breast cancer 3D cell culture model.
Concentration-dependent inhibition of cell proliferation in a CAL51 breast cancer 3D cell culture model.
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WO2024067792A1 |
In Vitro
GSPT1 degrader-4 (compound 3) (6 h) induces concentration-dependent degradation of GSPT1 protein in CAL51 breast cancer cells, with a DC50 of 25.4 nM and a maximum degradation rate of 98.3%[1].
GSPT1 degrader-4 (0.1 nM-10 μM; 3 days) inhibits cell proliferation in a concentration-dependent manner in the CAL51 breast cancer 3D cell culture model, with an IC50 of 39 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:CAL51 breast cancer 3D cell culture model
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Concentration:0.1, 1, 10, 100, 1000 and 10000 nm
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Incubation Time:3 days
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Result:It inhibited cell proliferation in a concentration-dependent manner, with an IC50 of 39 nM.
Chemical Information
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CAS No. 3034764-32-1
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Molecular Weight 480.90
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Formula C24H21ClN4O5
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SMILES
CC1=CC=C(NC(OCC2=CC=C3C(C=C(CN4C5C(NC(CC5)=O)=O)N3C4=O)=C2)=O)C=C1Cl
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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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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)