Asulacrine isethionate

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 205769

CAS#: 80841-48-1 (isethionate)

Description: Asulacrine, also known as CI-921; NSC-343499; SN-21407, is a topoisomerase ll inhibitor with antineoplastic properties. Asulacrine inhibits the enzyme topoisomerase ll, thereby blocking DNA replication and RNA and protein synthesis.

Chemical Structure

Asulacrine isethionate
CAS# 80841-48-1 (isethionate)

Theoretical Analysis

MedKoo Cat#: 205769
Name: Asulacrine isethionate
CAS#: 80841-48-1 (isethionate)
Chemical Formula: C26H30N4O7S2
Exact Mass: 0.00
Molecular Weight: 574.669
Elemental Analysis: C, 54.34; H, 5.26; N, 9.75; O, 19.49; S, 11.16

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales or click below button.
Note: Price will be listed if it is available in the future.

Request quote for custom synthesis

Related CAS #: 80841-48-1 (isethionate)   80841-47-0 (free base)    

Synonym: Amsalog; Asulacrine isethionate; CI921; CI-921; CI 921; NSC-343499; NSC343499; NSC 343499; SN21407; SN21407; SN 21407;

IUPAC/Chemical Name: 9-((2-methoxy-4-(methylsulfonamido)phenyl)amino)-N,5-dimethylacridine-4-carboxamide ethanesulfonate


InChi Code: InChI=1S/C24H24N4O4S.C2H6O3S/c1-14-7-5-8-16-21(14)27-23-17(9-6-10-18(23)24(29)25-2)22(16)26-19-12-11-15(13-20(19)32-3)28-33(4,30)31;1-2-6(3,4)5/h5-13,28H,1-4H3,(H,25,29)(H,26,27);2H2,1H3,(H,3,4,5)

SMILES Code: O=C(C1=CC=CC2=C(NC3=CC=C(NS(=O)(C)=O)C=C3OC)C4=CC=CC(C)=C4N=C12)NC.CCS(=O)(O)=O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >5 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info: Related CAS# 80841-47-0 (Asulacrine) 80841-48-1 (Asulacrine isethionate)   

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 574.67 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.


Dilution Calculator

Calculate the dilution required to prepare a stock solution.

1: Jin Y, Wu Z, Wu C, Zi Y, Chu X, Liu J, Zhang W. Size-adaptable and ligand (biotin)-sheddable nanocarriers equipped with avidin scavenging technology for deep tumor penetration and reduced toxicity. J Control Release. 2020 Apr 10;320:142-158. doi: 10.1016/j.jconrel.2020.01.040. Epub 2020 Jan 21. PMID: 31978442.

2: Zhang W, Li C, Jin Y, Liu X, Wang Z, Shaw JP, Baguley BC, Wu Z, Liu J. Multiseed liposomal drug delivery system using micelle gradient as driving force to improve amphiphilic drug retention and its anti-tumor efficacy. Drug Deliv. 2018 Nov;25(1):611-622. doi: 10.1080/10717544.2018.1440669. PMID: 29493300; PMCID: PMC6058678.

3: Jin Y, Wu Z, Li C, Zhou W, Shaw JP, Baguley BC, Liu J, Zhang W. Optimization of Weight Ratio for DSPE-PEG/TPGS Hybrid Micelles to Improve Drug Retention and Tumor Penetration. Pharm Res. 2018 Jan 4;35(1):13. doi: 10.1007/s11095-017-2340-y. PMID: 29302821.

4: Afzal A, Sarfraz M, Wu Z, Wang G, Sun J. Integrated scientific data bases review on asulacrine and associated toxicity. Crit Rev Oncol Hematol. 2016 Aug;104:78-86. doi: 10.1016/j.critrevonc.2016.05.013. Epub 2016 May 26. PMID: 27321375.

5: Zang X, Zhang J, Zhou Y, Chen Q, Peng Y, Sun J, Liu J, Liu W, Wang G, Zhou F. Quantitative determination of intracellular Asulacrine in MCF-7 breast cancer cells by liquid chromatography-mass spectrometry and its application to cellular pharmacokinetic studies of P188 modified liposomes. Biomed Chromatogr. 2016 Dec;30(12):1908-1914. doi: 10.1002/bmc.3762. Epub 2016 Jul 5. PMID: 27187844.

6: Afzal A, Zhong Y, Sarfraz M, Peng Y, Sheng L, Wu Z, Sun J, Wang G. Identification and characterization of in vivo metabolites of asulacrine using advanced mass spectrophotometry technique in combination with improved data mining strategy. J Chromatogr A. 2016 Apr 29;1444:74-85. doi: 10.1016/j.chroma.2016.03.068. Epub 2016 Mar 26. PMID: 27040513.

7: Zhang W, Falconer JR, Baguley BC, Shaw JP, Kanamala M, Xu H, Wang G, Liu J, Wu Z. Improving drug retention in liposomes by aging with the aid of glucose. Int J Pharm. 2016 May 30;505(1-2):194-203. doi: 10.1016/j.ijpharm.2016.03.044. Epub 2016 Mar 25. PMID: 27021465.

8: Zhang W, Wang G, See E, Shaw JP, Baguley BC, Liu J, Amirapu S, Wu Z. Post- insertion of poloxamer 188 strengthened liposomal membrane and reduced drug irritancy and in vivo precipitation, superior to PEGylation. J Control Release. 2015 Apr 10;203:161-9. doi: 10.1016/j.jconrel.2015.02.026. Epub 2015 Feb 19. PMID: 25701612.

9: Zhang W, Wang G, Falconer JR, Baguley BC, Shaw JP, Liu J, Xu H, See E, Sun J, Aa J, Wu Z. Strategies to maximize liposomal drug loading for a poorly water- soluble anticancer drug. Pharm Res. 2015 Apr;32(4):1451-61. doi: 10.1007/s11095-014-1551-8. Epub 2014 Oct 30. PMID: 25355460.

10: See E, Zhang W, Liu J, Svirskis D, Baguley BC, Shaw JP, Wang G, Wu Z. Physicochemical characterization of asulacrine towards the development of an anticancer liposomal formulation via active drug loading: stability, solubility, lipophilicity and ionization. Int J Pharm. 2014 Oct 1;473(1-2):528-35. doi: 10.1016/j.ijpharm.2014.07.033. Epub 2014 Jul 28. PMID: 25079434.

11: Ganta S, Paxton JW, Baguley BC, Garg S. Formulation and pharmacokinetic evaluation of an asulacrine nanocrystalline suspension for intravenous delivery. Int J Pharm. 2009 Feb 9;367(1-2):179-86. doi: 10.1016/j.ijpharm.2008.09.022. Epub 2008 Sep 21. PMID: 18848873.

12: Ganta S, Paxton JW, Baguley BC, Garg S. Development and validation of bioanalytical method for the determination of asulacrine in plasma by liquid chromatography. J Pharm Biomed Anal. 2008 Jan 22;46(2):386-90. doi: 10.1016/j.jpba.2007.09.025. Epub 2007 Oct 2. PMID: 17981420.

13: Bayés M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2002 Nov;24(9):615-43. PMID: 12616707.

14: Fyfe D, Raynaud F, Langley RE, Newell DR, Halbert G, Gardner C, Clayton K, Woll PJ, Judson I, Carmichael J. A study of amsalog (CI-921) administered orally on a 5-day schedule, with bioavailability and pharmacokinetically guided dose escalation. Cancer Chemother Pharmacol. 2002 Jan;49(1):1-6. doi: 10.1007/s00280-001-0389-z. PMID: 11855748.

15: Fyfe D, Price C, Langley RE, Pagonis C, Houghton J, Osborne L, Woll PJ, Gardner C, Baguley BC, Carmichael J; Cancer Research Campaing Phase I/II Trials Committee. A phase I trial of amsalog (CI-921) administered by intravenous infusion using a 5-day schedule. Cancer Chemother Pharmacol. 2001 Apr;47(4):333-7. doi: 10.1007/s002800000216. PMID: 11345650.

16: Finlay GJ, Baguley BC. Effects of protein binding on the in vitro activity of antitumour acridine derivatives and related anticancer drugs. Cancer Chemother Pharmacol. 2000;45(5):417-22. doi: 10.1007/s002800051011. PMID: 10803926.

17: Finlay GJ, Atwell GJ, Baguley BC. Inhibition of the action of the topoisomerase II poison amsacrine by simple aniline derivatives: evidence for drug-protein interactions. Oncol Res. 1999;11(6):249-54. PMID: 10691026.

18: Kettle AJ, Robertson IG, Palmer BD, Anderson RF, Patel KB, Winterbourn CC. Oxidative metabolism of amsacrine by the neutrophil enzyme myeloperoxidase. Biochem Pharmacol. 1992 Nov 3;44(9):1731-8. doi: 10.1016/0006-2952(92)90066-r. PMID: 1333205.

19: Sklarin NT, Wiernik PH, Grove WR, Benson L, Mittelman A, Maroun JA, Stewart JA, Robert F, Doroshow JH, Rosen PJ, et al. A phase II trial of CI-921 in advanced malignancies. Invest New Drugs. 1992 Nov;10(4):309-12. doi: 10.1007/BF00944186. PMID: 1487405.

20: Robertson IG, Palmer BD, Paxton JW, Shaw GJ. Differences in the metabolism of the antitumour agents amsacrine and its derivative CI-921 in rat and mouse. Xenobiotica. 1992 Jun;22(6):657-69. doi: 10.3109/00498259209053128. PMID: 1441589.