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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C20H21N3O3
- 分子量:351.40
-
保管条件:
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]
-
生物活性
-
化学情報
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
生物活性
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.
-
Cell Line:MDA-MB-231, KYSE30, MCF-10A, Het1A
-
Concentration:50 μM
-
Incubation Time:72 h
-
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.
-
Animal Model:BALB/c nude (female)[1]
-
Dosage:10 mg/kg; 20 mg/kg
-
Administration:i.p.; daily; 3 weeks
-
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.
化学情報
-
分子量 351.40
-
分子式 C20H21N3O3
-
SMILES
COC1=C(C=C(C=C1)NC(C2=CC(CN3C=NC=C3C)=CC=C2)=O)OC
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
CL121 関連分類
HY-181797 関連分類
Powered by Bioz