Top1 inhibitor 1

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

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Top1 inhibitor 1 Chemical Structure

CAS No. : 2302772-05-8

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Description

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

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]

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].

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

Molecular Weight

426.47

Formula

C₂₄H₂₂N₆O₂

CAS No.

2302772-05-8

SMILES

COC(C=C1)=CC=C1C2=CC=C(N=CC(C3=NN=CO3)=C4NCCCN5C=NC=C5)C4=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Kundu B, et al. Discovery and Mechanistic Study of Tailor-Made Quinoline Derivatives as Topoisomerase 1 Poison with Potent Anticancer Activity. J Med Chem. 2019 Apr 11; 62(7):3428-3446. [Content Brief]

Top1 inhibitor 1 Related Classifications

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The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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

Keywords:

Top1 inhibitor 12302772-05-8TopoisomeraseADC CytotoxinADC PayloadInhibitorinhibitorinhibit

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