TC8026
TC8026 is an allosteric-covalent inhibitor targeting protein disulfide isomerase (PDI), with an IC50 of 7 μM against human PDI. TC8026 induces endoplasmic reticulum stress-mediated apoptosis. TC8026 is a hit compound with PDI inhibitory activity identified via high-throughput screening, and it can be used for the research of glioblastoma.
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- Formule: C14H12ClN3O2
- Masse moléculaire:289.72
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Compound 30z (120-180 mg/kg; i.p.; single dose) exhibits no acute toxicity in male C57BL/6 mice, with no observable liver or kidney injury[1].
Compound 30z (40 mg/kg; i.p.; once daily) significantly inhibits subcutaneous U251 glioblastoma xenograft growth in female athymic nude mice with good in vivo tolerability[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male, 8 weeks old)[1]
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Dosage:10-40 mg/kg
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Administration:i.p.; once daily; 7 consecutive days
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Result:Exhibited normal body weight gain comparable to vehicle controls.
Maintained serum alanine aminotransferase (ALT), aspartate aminotransferase (AST), and blood urea nitrogen (BUN) levels within normal ranges with no significant differences from vehicle controls.
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Animal Model:C57BL/6 (male, 8 weeks old)[1]
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Dosage:120-180 mg/kg
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Administration:i.p.; single dose
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Result:Showed no mortality or adverse clinical signs over the 7-day monitoring period.
Had body weight changes comparable to vehicle controls.
Maintained serum ALT, AST, and BUN levels within normal ranges with no significant differences from vehicle controls.
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Animal Model:athymic nude (nu/nu) (female, 6 weeks old; subcutaneous glioblastoma xenograft model)[1]
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Dosage:40 mg/kg
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Administration:i.p.; once daily
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Result:Significantly suppressed subcutaneous U251 glioblastoma tumor growth compared to vehicle controls, as measured by reduced tumor volume over time and lower terminal tumor weights.
Had body weight changes comparable to vehicle controls, indicating good tolerability.
Chemical Information
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Masse moléculaire 289.72
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Formule C14H12ClN3O2
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SMILES
O=C(N1CC#CC(NCC)=O)C2=C(N=C1Cl)C=CC=C2
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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)