GSPT1 degrader-2
GSPT1 degrader-2 is an orally active GSPT1 molecular glue degrader that promotes the degradation of intracellular GSPT1 protein, with DC50 values of 3 nM and 22 nM in NCI-H1155 and ABC-1 cells with high N-Myc expression, respectively. GSPT1 degrader-2 can be used in the research of N-Myc-driven cancers, such as lung cancer.
For research use only. We do not sell to patients.
- CAS No.: 2803879-60-7
- Formula: C22H20ClN3O5
- Molecular Weight:441.86
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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All Eukaryotic Release Factor (eRF) Isoforms
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Biological Activity
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eRF3a/GSPT1 |
GSPT1 degrader-2 (Compound 210) (0.1 nM-100 μM) reduces GSPT1 in N-Myc-overexpressing NCI-H1155 and ABC-1 cells in a concentration-dependent manner, with DC50 values of 3 nM and 22 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c nude mice, 6-8 weeks old[1]
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Dosage:1 mg/kg; 3 mg/kg; 6 mg/kg
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Administration:p.o.; once daily; 9 days off after 5 consecutive days of dosing
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Result:Completely degraded GSPT1 in mice at all three doses.
No weight loss was observed in any of the dosage groups.
Chemical Information
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CAS No. 2803879-60-7
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Molecular Weight 441.86
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Formula C22H20ClN3O5
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SMILES
O=C(NC(CC1)=O)C1N2CC(C=CC(COC(NC3=CC(Cl)=C(C)C=C3)=O)=C4)=C4C2=O
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GSPT1 degrader-2 Related Classifications
HY-156747 Related Classifications
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