Multicomponent System of NPS-1034, an Orally Administered Lung Cancer Drug Candidate, with Sulfonic Acids and Solid State Characterization
DC Field | Value | Language |
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dc.contributor.author | Lee, Jangmi | - |
dc.contributor.author | Park, Suzie | - |
dc.contributor.author | Yoon, Seon-Joo | - |
dc.contributor.author | Jung, Yong Woo | - |
dc.contributor.author | Byun, Youngjoo | - |
dc.contributor.author | Yuk, Soon Hong | - |
dc.contributor.author | Jeon, Min Keyong | - |
dc.contributor.author | Kang, Sung Kwon | - |
dc.contributor.author | Lee, Eun Hee | - |
dc.date.accessioned | 2021-09-05T22:17:50Z | - |
dc.date.available | 2021-09-05T22:17:50Z | - |
dc.date.created | 2021-06-14 | - |
dc.date.issued | 2013-09 | - |
dc.identifier.issn | 1528-7483 | - |
dc.identifier.uri | https://scholar.korea.ac.kr/handle/2021.sw.korea/102336 | - |
dc.description.abstract | NPS-1034 is a drug candidate targeted for the regulation of c-MET/AXL receptor tyrosin kinase activity. NPS-1034 was developed to improve efficacy and reduce toxicity by targeting c-MET/AXL related signaling pathways. However, NPS-1034 is practically insoluble in almost all organic solvents as well as aqueous media (pH 1, 4.5, and 7.5). We attempted to improve the physicochemical properties of NPS-1034 by forming multicomponent systems with a wide variety of sulfonic acids including methanesulfonic acid, 1,2-ethanedisulfonic acid, p-toluenesulfonic acid, and camphorsulfonic acid. Solid state characterization of NPS-1034 salts and amorphous with sulfonic acids was conducted, and the crystal structures of four salts and NPS-1034 were compared and investigated. Sulfonic acid salts of NPS-1034 decreased the melting point of NPS-1034 as much as -155.43 degrees C. Solubilities of NPS-1034 and salts of NPS-1034 were measured to develop lipid-based formulation for the GLP toxicity study. Solvents studied include oleic acid, poly(ethylene glycol) 400, and ethanol. Solubility of amorphous of NPS-1034 with camphorsulfonic acid showed a significant increase in all three solvents. This work will give some insight into how various types of sulfonic acids interact with pharmaceutically important compounds containing the pyrrolepyridine moiety. | - |
dc.language | English | - |
dc.language.iso | en | - |
dc.publisher | AMER CHEMICAL SOC | - |
dc.subject | SALT SELECTION | - |
dc.subject | INHIBITORS | - |
dc.subject | DISCOVERY | - |
dc.title | Multicomponent System of NPS-1034, an Orally Administered Lung Cancer Drug Candidate, with Sulfonic Acids and Solid State Characterization | - |
dc.type | Article | - |
dc.contributor.affiliatedAuthor | Jung, Yong Woo | - |
dc.contributor.affiliatedAuthor | Byun, Youngjoo | - |
dc.contributor.affiliatedAuthor | Yuk, Soon Hong | - |
dc.contributor.affiliatedAuthor | Lee, Eun Hee | - |
dc.identifier.doi | 10.1021/cg400651f | - |
dc.identifier.scopusid | 2-s2.0-84883666373 | - |
dc.identifier.wosid | 000330095800015 | - |
dc.identifier.bibliographicCitation | CRYSTAL GROWTH & DESIGN, v.13, no.9, pp.3958 - 3968 | - |
dc.relation.isPartOf | CRYSTAL GROWTH & DESIGN | - |
dc.citation.title | CRYSTAL GROWTH & DESIGN | - |
dc.citation.volume | 13 | - |
dc.citation.number | 9 | - |
dc.citation.startPage | 3958 | - |
dc.citation.endPage | 3968 | - |
dc.type.rims | ART | - |
dc.type.docType | Article | - |
dc.description.journalClass | 1 | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
dc.relation.journalResearchArea | Chemistry | - |
dc.relation.journalResearchArea | Crystallography | - |
dc.relation.journalResearchArea | Materials Science | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Multidisciplinary | - |
dc.relation.journalWebOfScienceCategory | Crystallography | - |
dc.relation.journalWebOfScienceCategory | Materials Science, Multidisciplinary | - |
dc.subject.keywordPlus | SALT SELECTION | - |
dc.subject.keywordPlus | INHIBITORS | - |
dc.subject.keywordPlus | DISCOVERY | - |
dc.subject.keywordAuthor | multicomponent system | - |
dc.subject.keywordAuthor | drug candidate | - |
dc.subject.keywordAuthor | sulfonic acid | - |
dc.subject.keywordAuthor | salt | - |
dc.subject.keywordAuthor | solid state characterization | - |
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