Browsing by Author "Chen, C-W"

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BPR1J-097, a novel FLT3 kinase inhibitor, exerts potent inhibitory activity against AML
(2012-01-31)
Lin, W-H
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Jiaang, W-T
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Chen, C-W
;
Yen, K-J
;
Hsieh, S-Y
BACKGROUND: Activating mutations of Fms-like tyrosine kinase 3 (FLT3) constitute a major driver in the pathogenesis of acute myeloid leukaemia (AML). Hence, pharmacological inhibitors of FLT3 are of therapeutic interest for AML. METHODS: The effects of inhibition of FLT3 activity by a novel potent FLT3 inhibitor, BPR1J-097, were investigated using in vitro and in vivo assays. RESULTS: The 50% inhibitory concentration (IC50) of BPR1J-097 required to inhibit FLT3 kinase activity ranged from 1 to 10 nM, and the 50% growth inhibition concentrations (GC(50)s) were 21 +/- 7 and 46 +/- 14 nM for MOLM-13 and MV4-11 cells, respectively. BPR1J-097 inhibited FLT3/signal transducer and activator of transcription 5 phosphorylation and triggered apoptosis in FLT3-driven AML cells. BPR1J-097 also showed favourable pharmacokinetic property and pronounced dose-dependent tumour growth inhibition and regression in FLT3-driven AML murine xenograft models. CONCLUSION: These results indicate that BPR1J-097 is a novel small molecule FLT-3 inhibitor with promising in vivo anti-tumour activities and suggest that BPR1J-097 may be further developed in preclinical and clinical studies as therapeutics in AML treatments. British Journal of Cancer (2012) 106, 475-481. doi: 10.1038/bjc.2011.564 www.bjcancer.com Published online 20 December 2011 (C) 2012 Cancer Research UK
The Effect of Nanoparticle Morphology on the Measurement Accuracy of Mobility Particle Sizers
(2013-09-01)
Awasthi, A.
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Wu, B-S
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Liu, C-N
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Chen, C-W
;
Uang, S-N
The influence of particle morphology on the accuracy of nanoparticle size distributions measured by the engine exhaust particle sizer spectrometer (EEPS, TSI Model 3090) was studied using the scanning mobility particle sizer (SMPS, TSI Model 3936) as a reference. The EEPS shows higher total number concentrations with the maximum relative difference up to 67 % and smaller number median mobility diameters for polydisperse silver nanoparticles generated in the laboratory. To provide a quantitative explanation of the difference, generated polydisperse nanoparticles were classified as monodisperse particles with the initial equivalent mobility diameter (d (m1)) and sintered in the second furnace at different temperatures (room temperature to 600 A degrees C), to change their morphologies for the comparison tests. Without sintering (room temperature), results show that the measured mobility diameter (d (m2)) of the EEPS is smaller than that measured by the SMPS when d (m1) is larger than 30 nm and the difference increases as d (m1) is increased from 30 to 300 nm. But the difference decreases as the morphology of particles is changed from branched chain agglomerates to spheres for d (m1) less than 80 nm and the sintering temperature higher than 200 A degrees C. Theoretical analysis shows that the mean charge per agglomerates is more than that of spheres resulting in overestimation of the electrical mobility and underestimation of the d (m2) by the EEPS.