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

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:

查看所有亚型
Topoisomerase Topo I Topo II

查看 Prostaglandin Receptor 亚型特异性产品:

查看所有亚型
DP EP FP IP TXA2/TP TXB2

  • 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)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CT26.WT IC50
3.04 μM
Compound: 1H-30
Antiproliferative activity against mouse CT26.WT cells assessed as reduction in cell proliferation incubated for 48 hrs by MTT assay
Antiproliferative activity against mouse CT26.WT cells assessed as reduction in cell proliferation incubated for 48 hrs by MTT assay
[PMID: 35868003]
HGC-27 IC50
4.71 μM
Compound: 1H-30
Antiproliferative activity against human HGC-27 cells assessed as reduction in cell proliferation incubated for 48 hrs by MTT assay
Antiproliferative activity against human HGC-27 cells assessed as reduction in cell proliferation incubated for 48 hrs by MTT assay
[PMID: 35868003]
HT-29 IC50
16.93 μM
Compound: 1H-30
Antiproliferative activity against human HT-29 cells assessed as reduction in cell proliferation incubated for 48 hrs by MTT assay
Antiproliferative activity against human HT-29 cells assessed as reduction in cell proliferation incubated for 48 hrs by MTT assay
[PMID: 35868003]
RKO IC50
3.12 μM
Compound: 1H-30
Antiproliferative activity against human RKO cells assessed as reduction in cell proliferation incubated for 48 hrs by MTT assay
Antiproliferative activity against human RKO cells assessed as reduction in cell proliferation incubated for 48 hrs by MTT assay
[PMID: 35868003]
SGC-7901 IC50
14.95 μM
Compound: 1H-30
Antiproliferative activity against human SGC-7901 cells assessed as reduction in cell proliferation incubated for 48 hrs by MTT assay
Antiproliferative activity against human SGC-7901 cells assessed as reduction in cell proliferation incubated for 48 hrs by MTT assay
[PMID: 35868003]
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
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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