化合物 Topo I/COX-2-IN-1 T61939

Product Introduction
Bioactivity


英文名: Topo I/COX-2-IN-1

描述: Topo I/COX-2-IN-1 (1H-30) 是有效的 Topo I/COX-2抑制剂。Topo I/COX-2-IN-1抑制 COX-2 和 Topo I 的 IC50分别是 0.24 μM 和 4.42 μM。Topo I/COX-2-IN-1 能够诱导细胞凋亡 (apoptosis)，抑制癌细胞迁移，显示出抗癌活性

体外活性: 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 IC 50 values 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.

体内活性: 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) t 1/2 1.56 h T max 0.67 h C max 20.19 μg/mL AUC 0-t 18.20 mg/L h AUC 0 inf_obs 18.60 mg/L h

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途