Cat. No.: HY-118942

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.

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

Purity: 99.94%
CAS No.: 500214-53-9
Formula: C₂₃H₂₃N₃O₅
Molecular Weight:421.45

Storage:

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

Topovale Chemical Structure

CAS No.: 500214-53-9

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

Topoisomerase I

All Topoisomerase Isoforms :

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	IC₅₀	0.005 μM Compound: 1	Concentration required to inhibit cell proliferation in KBV-1 tumor cell line; overexpress MDR1 Concentration required to inhibit cell proliferation in KBV-1 tumor cell line; overexpress MDR1	[PMID: 15482929]
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 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, 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 after MTT assay Cytotoxicity against human KB3-1 cells after 4 days after MTT assay	[PMID: 19299037]
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	Concentration required to inhibit cell proliferation in KB3-1 tumor cell line Concentration required to inhibit cell proliferation in KB3-1 tumor cell line	[PMID: 15482929]
KB 3-1	IC₅₀	0.005 μM Compound: 3	Inhibitory concentration against KB/V-1 cells overexpress MDR1 Inhibitory concentration against KB/V-1 cells overexpress MDR1	[PMID: 15689163]
KB 3-1	IC₅₀	0.005 μM Compound: 3	Inhibitory concentration against KB3-1 cell line was determined Inhibitory concentration against KB3-1 cell line was determined	[PMID: 15689163]
KB 3-1	IC₅₀	0.006 μM Compound: 1	Concentration required to inhibit cell proliferation in KBH5.0 tumor cell line; overexpress BCRP Concentration required to inhibit cell proliferation in KBH5.0 tumor cell line; overexpress BCRP	[PMID: 15482929]
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	Cytotoxicity against human KBV1 cells by MTT method Cytotoxicity against human KBV1 cells by MTT method	[PMID: 18771930]
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	0.015 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	Cytotoxicity against mouse P388 cells by MTT method Cytotoxicity against mouse P388 cells by MTT method	[PMID: 18771930]
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, 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 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 method Cytotoxicity against mouse P388 cells after 4 days by MTT method	[PMID: 19303306]
P388	IC₅₀	0.001 nM Compound: 1, ARC-111	Cytotoxicity against human P388 cells Cytotoxicity against human P388 cells	[PMID: 18511275]
P388	IC₅₀	0.001 μM Compound: 1	Concentration required to inhibit cell proliferation in P388 tumor cell line Concentration required to inhibit cell proliferation in P388 tumor cell line	[PMID: 15482929]
P388	IC₅₀	0.001 μM Compound: 3	Inhibitory concentration against P388 cell line in mouse leukemia was determine Inhibitory concentration against P388 cell line in mouse leukemia was determine	[PMID: 15689163]
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]
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, 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: 3	Inhibitory concentration against camptothecin-resistant variant of P388 cell line was determined Inhibitory concentration against camptothecin-resistant variant of P388 cell line was determined	[PMID: 15689163]
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	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	0.002 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, 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, 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 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 method Cytotoxicity against human RPMI8402 cells after 4 days by MTT method	[PMID: 19303306]
RPMI 8402	IC₅₀	0.002 μM Compound: 1	Concentration required to inhibit cell proliferation in RPM18402 tumor cell line Concentration required to inhibit cell proliferation in RPM18402 tumor cell line	[PMID: 15482929]
RPMI 8402	IC₅₀	0.002 μM Compound: 3	Inhibitory concentration against lymphoblast RPMI 8402 cell line was determined Inhibitory concentration against lymphoblast RPMI 8402 cell line was determined	[PMID: 15689163]
RPMI 8402	IC₅₀	0.002 μM Compound: 3a	Cytotoxicity against human lymphoblast tumor cell line RPM18402 Cytotoxicity against human lymphoblast tumor cell line RPM18402	[PMID: 12392745]
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]
RPMI 8402	IC₅₀	0.9 μM Compound: 1	Concentration required to inhibit cell proliferation in CPT-K5 tumor cell line; camptothecin resistant Concentration required to inhibit cell proliferation in CPT-K5 tumor cell line; camptothecin resistant	[PMID: 15482929]
RPMI 8402	IC₅₀	0.9 μM Compound: 3	Cytotoxicity against camptothecin-resistant RPMI 8402 Cytotoxicity against camptothecin-resistant RPMI 8402	[PMID: 15689163]

Chemical Information

CAS No. 500214-53-9
Appearance Solid
Molecular Weight 421.45
Formula C₂₃H₂₃N₃O₅
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
Synonyms

ARC 111
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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3728 mL

11.8638 mL

23.7276 mL

5 mM

0.4746 mL

2.3728 mL

4.7455 mL

10 mM

---

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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

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

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Topovale

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-Lung Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

All Topoisomerase Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Topovale

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-Lung Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

All Topoisomerase Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Topovale Related Classifications

HY-118942 Related Classifications