GSPT1 degrader-14
GSPT1 degrader-14 is a selective molecular glue GSPT1 degrader. GSPT1 degrader-14 exhibits antiproliferative activity against cancer cells in a CRBN- and GSPT1-dependent manner. GSPT1 degrader-14 can be used for leukemia research.
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- Formule: C26H32N4O6S
- Masse moléculaire:528.62
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Stockage:
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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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Voir tous les produits spécifiques à Isoform Eukaryotic Release Factor (eRF)
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Activité biologique
Description
IC50 & Target
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eRF3a/GSPT1 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BE(2)-C | EC50 |
42 μM
Compound: 3
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Antiproliferative activity against wild type human BE2C cells assessed as reduction in cell viability measured after 3 days by ATP-dependent luminescence assay
Antiproliferative activity against wild type human BE2C cells assessed as reduction in cell viability measured after 3 days by ATP-dependent luminescence assay
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[PMID: 38608634] |
| MOLT-4 | EC50 |
0.42 μM
Compound: 3
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Antiproliferative activity against wild type human MOLT-4 cells assessed as reduction in cell viability measured after 3 days by ATP-dependent luminescence assay
Antiproliferative activity against wild type human MOLT-4 cells assessed as reduction in cell viability measured after 3 days by ATP-dependent luminescence assay
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[PMID: 38608634] |
| MV4-11 | EC50 |
0.41 μM
Compound: 3
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Antiproliferative activity against wild type human MV4-11 cells assessed as reduction in cell viability measured after 3 days by ATP-dependent luminescence assay
Antiproliferative activity against wild type human MV4-11 cells assessed as reduction in cell viability measured after 3 days by ATP-dependent luminescence assay
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[PMID: 38608634] |
In Vitro
GSPT1 degrader-14 (compound 3) (3 days) exhibits anti-proliferative activity against cancer cells, with EC50s of 0.42 (MOLT4), 0.41 (MV4;11), and 42 μM (BE(2)-C)[1].
GSPT1 degrader-14 (3 h) shows GSPT1 degradation activity in MOLT4, MV4;11, and BE(2)-C cells, with EC50s of 0.70, 0.70, and 19 μM, respectively[1].
GSPT1 degrader-14 (3 μM, 3 h) degrades GSPT1 in wild-type MOLT4, MV4;11, and BE(2)-C cells, but its degradation activity is blocked by CRBN KO cells and G575N mutant cells, indicating that it degrades GSPT1 in a CRBN- and GSPT1-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route |
|---|---|---|
| Rat | 1 mg/kg | i.v. |
Chemical Information
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Masse moléculaire 528.62
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Formule C26H32N4O6S
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SMILES
CCC(CCNS(=O)(NC1=CC=C2C(N(CC2=C1)C3CCC(NC3=O)=O)=O)=O)(C4=CC=CC=C4OC)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GSPT1 degrader-14 Related Classifications
HY-177753 Related Classifications
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