Topovale (Synonyms: ARC 111)

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Topovale (ARC 111) is a topoisomerase I inhbitor. Topovale is an antitumor agent, and shows low nM cytotoxicity against a panel of cancer cells. Topovale induces reversible topoisomerase I (TOP1) cleavage complexes in tumor cells.

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Topovale Chemical Structure

CAS No. : 500214-53-9

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Topoisomerase Topo I Topo II

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

Topoisomerase I

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	GI₅₀	0.177 μM Compound: ARC-111	Growth inhibition of human HCT-116 cells by Cell-titer96 assay Growth inhibition of human HCT-116 cells by Cell-titer96 assay	[PMID: 33492141]
KB 3-1	IC₅₀	0.005 μM Compound: 1, ARC-111	Cytotoxicity against human KB3-1 cells after MTT assay Cytotoxicity against human KB3-1 cells after MTT assay	[PMID: 18829334]
KB 3-1	IC₅₀	0.005 μM Compound: 1, ARC-111	Cytotoxicity against human KB3-1 cells after 4 days by MTT method Cytotoxicity against human KB3-1 cells after 4 days by MTT method	[PMID: 19303306]
KB 3-1	IC₅₀	0.005 μM Compound: 1, ARC-111	Cytotoxicity against human KB3-1 cells after 4 days by MTT assay Cytotoxicity against human KB3-1 cells after 4 days by MTT assay	[PMID: 18676151]
KB 3-1	IC₅₀	0.005 μM Compound: 1	Cytotoxicity against human KB3-1 cells by MTT method Cytotoxicity against human KB3-1 cells by MTT method	[PMID: 18771930]
KB 3-1	IC₅₀	0.005 μM Compound: 1, ARC-111	Cytotoxicity against human KB3-1 cells after 4 days after MTT assay Cytotoxicity against human KB3-1 cells after 4 days after MTT assay	[PMID: 19299037]
KB-V1	IC₅₀	0.002 μM Compound: 1, ARC-111	Cytotoxicity against MDR1 overexpressing human KBV1 cells after 4 days by MTT method Cytotoxicity against MDR1 overexpressing human KBV1 cells after 4 days by MTT method	[PMID: 19303306]
KB-V1	IC₅₀	0.005 μM Compound: 1, ARC-111	Cytotoxicity against multidrug resistant human KBV-1 cells overexpressing MDR1 after MTT assay Cytotoxicity against multidrug resistant human KBV-1 cells overexpressing MDR1 after MTT assay	[PMID: 18829334]
KB-V1	IC₅₀	0.005 μM Compound: 1, ARC-111	Cytotoxicity against multidrug resistant human KBV1 cells overexpressing MDR1 after 4 days by MTT assay Cytotoxicity against multidrug resistant human KBV1 cells overexpressing MDR1 after 4 days by MTT assay	[PMID: 19299037]
KB-V1	IC₅₀	0.005 μM Compound: 1	Cytotoxicity against human KBV1 cells by MTT method Cytotoxicity against human KBV1 cells by MTT method	[PMID: 18771930]
KB-V1	IC₅₀	0.015 μM Compound: 1, ARC-111	Cytotoxicity against human multidrug resistant MDR1 overexpressing human KBV1 cells after 4 days by MTT assay Cytotoxicity against human multidrug resistant MDR1 overexpressing human KBV1 cells after 4 days by MTT assay	[PMID: 18676151]
P388	IC₅₀	0.001 μM Compound: 1, ARC-111	Cytotoxicity against mouse P388 cells after MTT assay Cytotoxicity against mouse P388 cells after MTT assay	[PMID: 18829334]
P388	IC₅₀	0.001 μM Compound: 1, ARC-111	Cytotoxicity against mouse P388 cells after 4 days by MTT method Cytotoxicity against mouse P388 cells after 4 days by MTT method	[PMID: 19303306]
P388	IC₅₀	0.001 μM Compound: 1, ARC-111	Cytotoxicity against mouse P388 cells after 4 days by MTT assay Cytotoxicity against mouse P388 cells after 4 days by MTT assay	[PMID: 19299037]
P388	IC₅₀	0.001 μM Compound: 1, ARC-111	Cytotoxicity against mouse P388 cells after 4 days by MTT assay Cytotoxicity against mouse P388 cells after 4 days by MTT assay	[PMID: 18676151]
P388	IC₅₀	0.001 μM Compound: 1	Cytotoxicity against mouse P388 cells by MTT method Cytotoxicity against mouse P388 cells by MTT method	[PMID: 18771930]
P388	IC₅₀	0.23 μM Compound: 1, ARC-111	Cytotoxicity against camptothecin-resistant mouse P388 cells after 4 days by MTT method Cytotoxicity against camptothecin-resistant mouse P388 cells after 4 days by MTT method	[PMID: 19303306]
P388	IC₅₀	0.23 μM Compound: 1, ARC-111	Cytotoxicity against mouse CPT45-resistant topoisomerase 1-deficient P388 cells after 4 days by MTT assay Cytotoxicity against mouse CPT45-resistant topoisomerase 1-deficient P388 cells after 4 days by MTT assay	[PMID: 18676151]
P388	IC₅₀	0.23 μM Compound: 1	Cytotoxicity against camptothecin-resistant mouse P388 cells by MTT method Cytotoxicity against camptothecin-resistant mouse P388 cells by MTT method	[PMID: 18771930]
P388CPT45	IC₅₀	0.23 μM Compound: 1, ARC-111	Cytotoxicity against camptothecin-resistant and TOP1 deficient mouse P388/CPT45 cells after MTT assay Cytotoxicity against camptothecin-resistant and TOP1 deficient mouse P388/CPT45 cells after MTT assay	[PMID: 18829334]
P388CPT45	IC₅₀	0.23 μM Compound: 1, ARC-111	Cytotoxicity against mouse P388/CPT45 cells after 4 days by MTT assay Cytotoxicity against mouse P388/CPT45 cells after 4 days by MTT assay	[PMID: 19299037]
RPMI 8402	IC₅₀	0.002 μM Compound: 1, ARC-111	Cytotoxicity against human RPMI8402 cells after MTT assay Cytotoxicity against human RPMI8402 cells after MTT assay	[PMID: 18829334]
RPMI 8402	IC₅₀	0.002 μM Compound: 1, ARC-111	Cytotoxicity against human RPMI8402 cells after 4 days by MTT method Cytotoxicity against human RPMI8402 cells after 4 days by MTT method	[PMID: 19303306]
RPMI 8402	IC₅₀	0.002 μM Compound: 1, ARC-111	Cytotoxicity against human RPMI8402 cells after 4 days by MTT assay Cytotoxicity against human RPMI8402 cells after 4 days by MTT assay	[PMID: 19299037]
RPMI 8402	IC₅₀	0.002 μM Compound: 1, ARC-111	Cytotoxicity against human RPMI8402 cells after 4 days by MTT assay Cytotoxicity against human RPMI8402 cells after 4 days by MTT assay	[PMID: 18676151]
RPMI 8402	IC₅₀	0.002 μM Compound: 1	Cytotoxicity against human RPMI8402 cells by MTT method Cytotoxicity against human RPMI8402 cells by MTT method	[PMID: 18771930]
RPMI 8402	IC₅₀	0.002 μM Compound: 1	Cytotoxic activity against human lymphoblast tumor cell line RPMI8402 after 4 days of treatment Cytotoxic activity against human lymphoblast tumor cell line RPMI8402 after 4 days of treatment	[PMID: 12747798]
RPMI 8402	IC₅₀	0.9 μM Compound: 3a	Cytotoxicity using camptothecin-resistant variant of RPM18402 (CPT-K5) possessing functional, but mutant TOP-1 Cytotoxicity using camptothecin-resistant variant of RPM18402 (CPT-K5) possessing functional, but mutant TOP-1	[PMID: 12392745]

Molecular Weight

421.45

Formula

C₂₃H₂₃N₃O₅

CAS No.

500214-53-9

SMILES

COC1=C(C=C(C2=C1)C(N(C3=C2C=NC4=C3C=C5OCOC5=C4)CCN(C)C)=O)OC

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]. Li TK, et al. Characterization of ARC-111 as a novel topoisomerase I-targeting anticancer drug. Cancer Res. 2003 Dec 1;63(23):8400-7. [Content Brief]

Topovale Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

Mass		Concentration		Volume		Molecular Weight *
	=		×		×

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:

Topovale500214-53-9ARC 111ARC111ARC-111TopoisomeraseHCT-8colon tumorInhibitorinhibitorinhibit

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