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References |
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.
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Molecular Formula |
C24H24N4O4S
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Molecular Weight |
464.54
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Exact Mass |
464.15
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Elemental Analysis |
C, 62.05; H, 5.21; N, 12.06; O, 13.78; S, 6.90
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CAS # |
80841-47-0
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Related CAS # |
80841-48-1 (isethionate);80841-47-0;
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Appearance |
Solid powder
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SMILES |
O=C(C1=CC=CC2=C(NC3=CC=C(NS(=O)(C)=O)C=C3OC)C4=CC=CC(C)=C4N=C12)NC
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InChi Key |
TWHSQQYCDVSBRK-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C24H24N4O4S/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/h5-13,28H,1-4H3,(H,25,29)(H,26,27)
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Chemical Name |
9-((2-methoxy-4-(methylsulfonamido)phenyl)amino)-N,5-dimethylacridine-4-carboxamide
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Synonyms |
Amsalog; Asulacrine isethionate; CI921; CI-921; CI 921; NSC-343499; NSC343499; NSC 343499; SN21407; SN21407; SN 21407;
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.1527 mL | 10.7633 mL | 21.5267 mL | |
5 mM | 0.4305 mL | 2.1527 mL | 4.3053 mL | |
10 mM | 0.2153 mL | 1.0763 mL | 2.1527 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.