Literature DB >> 23472049

Structural and Physicochemical Aspects of Dasatinib Hydrate and Anhydrate phases.

Saikat Roy1, Rosalynn Quiñones, Adam J Matzger.   

Abstract

Crystal structures for the commercial monohydrate form and an anhydrate form of dasatinib, an oral anti-cancer agent, are presented along with characterization by Raman spectroscopy, powder X-ray diffraction, differential scanning calorimetry, and thermogravimetric analysis. Solubility measurements conducted in water reveal the anhydrate has dramatically improved solubility compared to the commercial hydrate form. Finally, dasatinib is a rare example of a promiscuous solvate former and the basis for this behavior can now be understood by examining the poor packing efficiency in the unsolvated form.

Entities:  

Year:  2012        PMID： 23472049      PMCID： PMC3586737          DOI： 10.1021/cg300152p

Source DB:  PubMed          Journal:  Cryst Growth Des        ISSN： 1528-7483            Impact factor:   4.076


  14 in total

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Authors:  Louis J Lombardo; Francis Y Lee; Ping Chen; Derek Norris; Joel C Barrish; Kamelia Behnia; Stephen Castaneda; Lyndon A M Cornelius; Jagabandhu Das; Arthur M Doweyko; Craig Fairchild; John T Hunt; Ivan Inigo; Kathy Johnston; Amrita Kamath; David Kan; Herbert Klei; Punit Marathe; Suhong Pang; Russell Peterson; Sidney Pitt; Gary L Schieven; Robert J Schmidt; John Tokarski; Mei-Li Wen; John Wityak; Robert M Borzilleri
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6.  Packing interactions in hydrated and anhydrous forms of the antibiotic Ciprofloxacin: a solid-state NMR, X-ray diffraction, and computer simulation study.

Authors:  Luís Mafra; Sérgio M Santos; Renée Siegel; Inês Alves; Filipe A Almeida Paz; Dmytro Dudenko; Hans W Spiess
Journal:  J Am Chem Soc       Date:  2011-12-09       Impact factor: 15.419

7.  2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase inhibitor.

Authors:  Jagabandhu Das; Ping Chen; Derek Norris; Ramesh Padmanabha; James Lin; Robert V Moquin; Zhongqi Shen; Lynda S Cook; Arthur M Doweyko; Sidney Pitt; Suhong Pang; Ding Ren Shen; Qiong Fang; Henry F de Fex; Kim W McIntyre; David J Shuster; Kathleen M Gillooly; Kamelia Behnia; Gary L Schieven; John Wityak; Joel C Barrish
Journal:  J Med Chem       Date:  2006-11-16       Impact factor: 7.446

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Authors:  G L Amidon; H Lennernäs; V P Shah; J R Crison
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Authors:  Neil P Shah; Chris Tran; Francis Y Lee; Ping Chen; Derek Norris; Charles L Sawyers
Journal:  Science       Date:  2004-07-16       Impact factor: 47.728

10.  Conformational polymorphism in organic crystals.

Authors:  Ashwini Nangia
Journal:  Acc Chem Res       Date:  2008-03-19       Impact factor: 22.384
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  7 in total

1.  Remodeling the cancer epigenome: mutations in the SWI/SNF complex offer new therapeutic opportunities.

Authors:  Krystal A Orlando; Vinh Nguyen; Jesse R Raab; Tara Walhart; Bernard E Weissman
Journal:  Expert Rev Anticancer Ther       Date:  2019-05-13       Impact factor: 4.512

2.  Mechanisms of Crystal Plasticization by Lattice Water.

Authors:  Chenguang Wang; Changquan Calvin Sun
Journal:  Pharm Res       Date:  2022-03-17       Impact factor: 4.200

3.  Periodic DFT study of structural transformations of cocrystal NTO/TZTN under high pressure.

Authors:  Guo-Zheng Zhao; Dong-Fang Yang
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4.  Identification of Small-Molecule Inhibitors of Brucella Diaminopimelate Decarboxylase by Using a High-Throughput Screening Assay.

Authors:  Pengfei Bie; Xiaowen Yang; Cunrui Zhang; Qingmin Wu
Journal:  Front Microbiol       Date:  2020-01-21       Impact factor: 5.640

5.  Stable Fatty Acid Solvates of Dasatinib, a Tyrosine Kinase Inhibitor: Prediction, Process, and Physicochemical Properties.

Authors:  Venkata Narasayya Saladi; Bal Raju Kammari; Arthanareeswari Maruthapillai; Sudarshan Mahapatra; Ramanaiah Chennuru; Eswaraiah Sajja; Srinivasan Thirumalai Rajan; Vijayavitthal T Mathad
Journal:  ACS Omega       Date:  2022-02-15

6.  Pharmaceutical Cocrystal Formation of Pyrazinamide with 3-Hydroxybenzoic Acid: A Terahertz and Raman Vibrational Spectroscopies Study.

Authors:  Qiqi Wang; Jiadan Xue; Zhi Hong; Yong Du
Journal:  Molecules       Date:  2019-01-30       Impact factor: 4.411

7.  Dasatinib Nanoemulsion and Nanocrystal for Enhanced Oral Drug Delivery.

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Journal:  Pharmaceutics       Date:  2022-01-15       Impact factor: 6.321
  7 in total

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