Topo I/COX-2-IN-1

Name: Topo I/COX-2-IN-1
Brand: TargetMol
SKU: T61939
Rating: 4.5 (1 reviews)

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产品编号 T61939

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

Topo I/COX-2-IN-1

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产品编号 T61939

规格	价格	库存
25 mg	¥ 10,600	10-14周
50 mg	¥ 13,800	10-14周
100 mg	¥ 17,500	10-14周

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产品描述	Topo I/COX-2-IN-1 (1H-30) is a potent Topo I/COX-2 inhibitor with the IC50 of 0.24 μM and 4.42 μM for COX-2 and Topo I, respectively. Topo I/COX-2-IN-1 induces apoptosis and inhibits migration of cancer cells, shows anti-cancer activity.
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