Topovale (Synonyms: ARC 111)

Cat. No.: HY-118942 Purity: 99.94%: Data Sheet
SDS

COA
Handling Instructions
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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.

For research use only. We do not sell to patients.

Topovale Chemical Structure

CAS No. : 500214-53-9

Size	Stock	Quantity
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	Get quote
100 mg	Get quote

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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

Appearance

Solid

Color

White to off-white

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

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 4.03 mg/mL (9.56 mM; ultrasonic and adjust pH to 2 with TFA; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3728 mL	11.8638 mL	23.7276 mL
5 mM	0.4746 mL	2.3728 mL	4.7455 mL
10 mM	---	---	---

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

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Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.94%

Select Batch:

Data Sheet (273 KB) SDS (251 KB)

COA (252 KB) HNMR (258 KB) RP-HPLC (247 KB) MS (69 KB)

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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.3728 mL	11.8638 mL	23.7276 mL	59.3190 mL
DMSO	5 mM	0.4746 mL	2.3728 mL	4.7455 mL	11.8638 mL

Topovale Related Classifications

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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Topovale (Synonyms: ARC 111)

Topovale Related Antibodies

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References

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