Topo I/COX-2-IN-1 (1H-30) 是一种潜在的Topo I/COX-2抑制剂，抑制 COX-2 和 Topo I 活性的IC50值分别是 0.24 μM 和 4.42 μM。Topo I/COX-2-IN-1 可以诱导细胞凋亡 (apoptosis)，抑制癌细胞迁移，具有抗癌活性。
| 生物活性 | Topo I/COX-2-IN-1 (1H-30) is a potentialTopo I/COX-2inhibitor. Topo I/COX-2-IN-1 inhibitsCOX-2andTopo Iwith theIC50value of 0.24 μM and 4.42 μM, respectively. Topo I/COX-2-IN-1 can induceapoptosisand inhibit migration ofcancercells, has anti-cancer activity[1]. |
| IC50& Target[1] | Topoisomerase I 4.42 μM (IC50) |
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体外研究
(In Vitro) | Topo I/COX-2-IN-1 (1H-30) (0-100 μM, 24 h) has anti-tumor cell proliferation activity and can induce apoptosis by increasing caspase-3 activity in a dose-dependent manner[1].
Topo I/COX-2-IN-1 (1H-30) (0.04-0.37 μM, 48 h) shows a significant decrease in cell migration at 0.37 μM and reduces the expression of MMP-9 (matrix metalloproteinases) in HGC-27 and RKO cells[1].
Topo I/COX-2-IN-1 (1H-30) (10 μM, 48 h) can inhibit the activation of NF-κB pathway in cancer cells[1].
Cell Proliferation Assay[1] | Cell Line: | Colon cancer cell lines HGC-27, RKO, HT-29, SGC-7901, and CT26.WT | | Concentration: | 0-100 μM | | Incubation Time: | | | Result: | Inhibited the proliferation of CT26.WT, RKO, HT-29, HGC-27 and SGC-7901 cells with the IC50values of 3.04, 3.12, 16.93, 4.71 and 14.95 μM, respectively. |
Apoptosis Analysis[1] | Cell Line: | HGC-27, RKO cell lines | | Concentration: | 1.1 μM, 3.3 μM, 10 μM | | Incubation Time: | 24 hours | | Result: | Increased caspase-3 positive cells to 55.94% and 69.46 % at 10 μM comparing to 1.08% and 9.39% in the untreated group in RKO and HGC-27 cells respectively. |
Cell Cycle Analysis[1] | Cell Line: | HGC-27, RKO cell lines | | Concentration: | 1.1 μM, 3.3 μM, 10 μM | | Incubation Time: | | | Result: | Induced blocked in G2/M phase significantly. |
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体内研究
(In Vivo) | Topo I/COX-2-IN-1 (1H-30) (intraperitoneal injection, 100 mg/kg, twice a day, 14 days) may inhibit tumor growth by increasing the expression of caspase-3 and decreasing MMP-9 and COX-2 in tumor tissues to induce apoptosis in BALB/c mice model infected with CT26.WT colon cancer cells[1].
| Animal Model: | BALB/c mice model infected with CT26.WT colon cancer cells[1] | | Dosage: | 100 mg/kg | | Administration: | Intraperitoneal injection; twice a day; 14 days | | Result: | Significant reduction in tumor size and tumor weight and no significant differences in body weight, organs. |
| Animal Model: | SD rats[1] | | Dosage: | 100 mg/kg | | Administration: | Intraperitoneal injection; once | | Result: | b>The pharmacokinetic parameters of Topo I/COX-2-IN-1 (1H-30)
| Parameter | Topo I/COX-2-IN-1 (1H-30) | | t1/2 | 1.56 h | | Tmax | 0.67 h | | Cmax | 20.19 μg/mL | | AUC0-t | 18.20 mg/Loh | | AUC0-inf_obs | 18.60 mg/Loh | |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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