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Cat. No.: HY-13552

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Asulacrine isethionate

(Synonyms: CI-921 isethionate; NSC 343499 isethionate)

Asulacrine isethionate (CI-921 isethionate) is a derivative of Amsacrine (HY-13551), a Topoisomerase II inhibitor and an anticancer agent. Asulacrine isethionate binds to DNA via intercalation, forming stable complexes with long residence times at DNA sites. Asulacrine isethionate mediates DNA breakage and DNA-protein cross-linking. Asulacrine isethionate exhibits anticancer activity against leukemia or lung cancer. Asulacrine isethionate can be used in research related to breast cancer, lung cancer, mouse solid tumors and leukemia.

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

CAS No.: 80841-48-1
Formula: C₂₆H₃₀N₄O₈S₂
Molecular Weight:590.67

Storage:

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

Asulacrine isethionate Chemical Structure

CAS No.: 80841-48-1

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Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

Topoisomerase-2

All Topoisomerase Isoforms :

All DNA/RNA Synthesis Isoforms :

In Vitro

The IC₅₀ values of Asulacrine isethionate against the T-47D breast cancer cell line and the murine leukemia P388/ADR cell line are 6.7 nM and 800 nM, respectively^[4].

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

Parmacokinetics

Species	Dose	Route	C_max	AUC_0-∞	MRT	T_1/2 (Distribution)	T_1/2β	CL	V_ss
Mice^[1]	30 mg/kg	i.v.	18.3 μg/mL	46.4 μg/mL·h	3.5 h	0.9 h	2.7 h	0.6 L/h/kg	2.5 L/kg

In Vivo

Asulacrine (isethionate) (30 mg/kg; i.v.; single dose) administered as a nanocrystalline suspension in male C57BL/6 mice results in reduced peak plasma concentrations, prolonged plasma residence time, and significantly higher drug exposure in liver, lung, and kidney compared to the Asulacrine solution^[1].

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

Chemical Information

CAS No. 80841-48-1
Molecular Weight 590.67
Formula C₂₆H₃₀N₄O₈S₂
SMILES

O=C(C1=CC=CC2=C1N=C3C(C=CC=C3C)=C2NC4=CC=C(NS(=O)(C)=O)C=C4OC)NC.O=S(O)(CCO)=O
Synonyms

CI-921 isethionate; NSC 343499 isethionate
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]. Ganta S, et al. Formulation and pharmacokinetic evaluation of an asulacrine nanocrystalline suspension for intravenous delivery. International journal of pharmaceutics. 2009 Feb 09;367(1-2):179-86. [Content Brief]

[2]. Hays S J, et al. Deuterium, tritium, and carbon‐14 labeling of 9‐[[2‐methoxy‐4‐[(methylsulfonyl) amino] phenyl] amino]‐N, 5‐dimethyl‐acridinecarboxamide (CI‐921), a new antitumor agent[J]. Journal of Labelled Compounds and Radiopharmaceuticals, 1984, 21(6): 575-586.

[3]. Gellerman G. Recent synthetic approaches to anti-cancer 9-anilinoacridines. A review[J]. Organic Preparations and Procedures International, 2012, 44(3): 187-221.

[4]. Teitelbaum A M. Pre-clinical Drug Development of 9-aminoacridines for Malignant Glioma and Meropenem Prodrugs for Drug-Resistant Tuberculosis[M]. University of Minnesota, 2012.

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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.

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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Asulacrine isethionate

All Topoisomerase Isoforms

All DNA/RNA Synthesis Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

Asulacrine isethionate Related Classifications

HY-13552 Related Classifications