1. Cell Cycle/DNA Damage Antibody-drug Conjugate/ADC Related
  2. Topoisomerase ADC Cytotoxin
  3. Top1 inhibitor 1

Top1 inhibitor 1 (化合物 28) 是一种有效的人拓扑异构酶 1 (Top1) 抑制剂,IC50 值为 29 nM。

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Top1 inhibitor 1 Chemical Structure

Top1 inhibitor 1 Chemical Structure

CAS No. : 2302772-05-8

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Top1 inhibitor 1 (compound 28) is a potent human topoisomerase I (Top1) inhibitor with an IC50 value of 29 nM[1].

IC50 & Target[1]

Camptothecins

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HCT-116 IC50
2.34 μM
Compound: 28
Cytotoxicity against human HCT116 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
Cytotoxicity against human HCT116 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
[PMID: 30897325]
HEK293 IC50
8.34 μM
Compound: 1
Cytotoxicity against HEK293 cells assessed as reduction in cell viability after 48 hr by MTT assay
Cytotoxicity against HEK293 cells assessed as reduction in cell viability after 48 hr by MTT assay
[PMID: 32682183]
HEK293 IC50
8.34 μM
Compound: 28
Cytotoxicity against HEK293 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
Cytotoxicity against HEK293 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
[PMID: 30897325]
HeLa IC50
2.61 μM
Compound: 28
Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
[PMID: 30897325]
MCF7 IC50
2.74 μM
Compound: 1
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hr by MTT assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hr by MTT assay
[PMID: 32682183]
MCF7 IC50
2.74 μM
Compound: 28
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
[PMID: 30897325]
MCF7 IC50
2.74 μM
Compound: 28
Poison activity at TOP1 in human MCF7 cells assessed as decrease in relaxed supercoiled pBS(SK+) DNA mobility measured after 30 mins by ethidium bromide staining based agarose gel electrophoresis
Poison activity at TOP1 in human MCF7 cells assessed as decrease in relaxed supercoiled pBS(SK+) DNA mobility measured after 30 mins by ethidium bromide staining based agarose gel electrophoresis
[PMID: 30897325]
MEF IC50
1.02 μM
Compound: 28
Cytotoxicity against TDP1-deficient MEF cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
Cytotoxicity against TDP1-deficient MEF cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
[PMID: 30897325]
MEF IC50
2.91 μM
Compound: 28
Cytotoxicity against TDP1-positive MEF cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
Cytotoxicity against TDP1-positive MEF cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
[PMID: 30897325]
Sf9 IC50
0.029 μM
Compound: 28
Poison activity at recombinant human TOP1 expressed in baculovirus infected Sf9 insect cells assessed as decrease in relaxed supercoiled pBS(SK+) DNA mobility measured after 30 mins by ethidium bromide staining based agarose gel electrophoresis
Poison activity at recombinant human TOP1 expressed in baculovirus infected Sf9 insect cells assessed as decrease in relaxed supercoiled pBS(SK+) DNA mobility measured after 30 mins by ethidium bromide staining based agarose gel electrophoresis
[PMID: 30897325]
体外研究
(In Vitro)

Top1 inhibitor 1 reveals cytotoxicity in cancerous cells including MCF7 (IC50: 2.74 µM), HeLa (IC50: 2.61 µM), HCT116 (IC50: 2.34 µM), NIH: OVCAR-3 (IC50: 2.35 µM) cells compared to the non-cancerous cells like HEK293 (IC50: 8.34 µM) [1].

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

分子量

426.47

Formula

C24H22N6O2

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
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

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Top1 inhibitor 1
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HY-126142
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