CL121
CL121 is a Glutaminyl Cyclase inhibitor with an IC50 of 0.07 μM against human sQC and an IC50 of 0.54 μM against human gQC. CL121 reduces the level of pyroglutamate (pE)-modified CD47 on the surface of cancer cells. CL121 exhibits anti-tumor activity against triple-negative breast cancer.
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- Formule: C20H21N3O3
- Masse moléculaire:351.40
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
CL121 potently inhibits purified human sQC with an IC50 of 0.07 μM and human gQC with an IC50 of 0.54 μM[1].
CL121 (10-40 μM; 72 h) reduces surface pE-CD47 modification in a dose-dependent manner on MDA-MB-231 cells without affecting total CD47 expression[1].
CL121 (10-40 μM) enhances macrophage-mediated phagocytosis of KYSE30 cells, with the most potent effect at 20 μM, while higher concentrations (40 μM) show reduced activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231, KYSE30, MCF-10A, Het1A
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Concentration:50 μM
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Incubation Time:72 h
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Result:Resulted in cell viability above 75% across all tested cell lines.
| Species | Dose | Route | Cmax | Tmax | T1/2 | CLz/F | Vz/F | AUC0-∞ |
|---|---|---|---|---|---|---|---|---|
| Rat[1] | 10 mg/kg | i.p. | 4976 ± 889 μg/L | 0.25 h | 2.48 ± 2.15 h | 1.9 ± 0.4 L/h/kg | 6 ± 3.84 L/kg | 5431 ± 1253 μg/L·h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (female)[1]
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Dosage:10 mg/kg; 20 mg/kg
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Administration:i.p.; daily; 3 weeks
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Result:Reduced average tumor volume to 154 mm3 (from 227 mm3 in controls) and average tumor weight to 129.05 mg (from 191.49 mg in controls) at 10 mg/kg, with statistically significant tumor weight reduction (P < 0.01).
Reduced average tumor volume to 195 mm3 and average tumor weight to 173.69 mg at 20 mg/kg, with no statistically significant difference compared to controls.
Significantly reduced intratumoral pE-CD47 expression relative to controls at both doses, with 10 mg/kg showing statistically significant reduction (P < 0.05) and 20 mg/kg showing stronger statistically significant reduction (P < 0.01).
Showed no significant differences in body weight between treatment groups and controls, indicating low systemic toxicity.
Chemical Information
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Masse moléculaire 351.40
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Formule C20H21N3O3
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SMILES
COC1=C(C=C(C=C1)NC(C2=CC(CN3C=NC=C3C)=CC=C2)=O)OC
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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)
CL121 Related Classifications
HY-181797 Related Classifications
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