2. Cell Cycle/DNA Damage GPCR/G Protein Apoptosis
  3. Topoisomerase Prostaglandin Receptor Apoptosis
  4. Topo I/COX-2-IN-1

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。

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Topo I/COX-2-IN-1 Chemical Structure

Topo I/COX-2-IN-1 Chemical Structure

CAS No. : 3031418-84-2

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Topo I/COX-2-IN-1 相关抗体

Top Publications Citing Use of Products

查看 Topoisomerase 亚型特异性产品:

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Topoisomerase Topo I Topo II

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Topo I/COX-2-IN-1 (1H-30) is a potential Topo I/COX-2 inhibitor. Topo I/COX-2-IN-1 inhibits COX-2 and Topo I with the IC50 value of 0.24 μM and 4.42 μM, respectively. Topo I/COX-2-IN-1 can induce apoptosis and inhibit migration of cancer cells, 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Topo I/COX-2-IN-1 相关抗体:

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 IC50 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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/L•h
AUC0‑inf_obs 18.60 mg/L•h
分子量

400.83

Formula

C21H18ClFN2O3
CAS 号
Unlabeled Cas

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.
纯度 & 产品资料
参考文献

Topo I/COX-2-IN-1 相关分类

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Topo I/COX-2-IN-13031418-84-2TopoisomeraseProstaglandin ReceptorApoptosisTopo I/COX-2 inhibitorCOX-2,Topo Ianti-cancermigrationapoptosisInhibitorinhibitorinhibit

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