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^[1][2][3][4].

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.

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.

590.67

C₂₆H₃₀N₄O₈S₂

80841-48-1

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

Room temperature in continental US; may vary elsewhere.

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

• [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.