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Topo I/COX-2-IN-1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Topo I/COX-2-IN-1图片
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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)

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.
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)
ParameterTopo I/COX-2-IN-1 (1H-30)
t1/21.56 h
Tmax0.67 h
Cmax20.19 μg/mL
AUC0-t18.20 mg/Loh
AUC0-inf_obs18.60 mg/Loh
分子量

400.83

Formula

C21H18ClFN2O3

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.