Latent pH-responsive ratiometric fluorescent cluster based on self-assembled photoactivated SNARF derivatives

We have developed a self-assembled fluorescent cluster comprising a seminaphthorhodafluor (SNARF) derivative protected by a photoremovable o-nitrobenzyl group. Prior to UV irradiation, a colorless and nonfluorescent cluster was spontaneously assembled in aqueous solution. After UV irradiation, the self-assembled cluster remained intact and showed a large enhancement in pH-responsive fluorescence. The unique pH responsive fluorescent cluster could be used as a dual-emissive ratiometric fluorescent pH probe not only in the test tube but also in HeLa cell cultures.</p

Table S2 from Aurora A Inhibitor TAS-119 Enhances Antitumor Efficacy of Taxanes <i>In Vitro</i> and <i>In Vivo</i>: Preclinical Studies as Guidance for Clinical Development and Trial Design

Combination Index scores (CI50 and CI75) are shown in the indicated cell lines.</p

Figure S4 from Aurora A Inhibitor TAS-119 Enhances Antitumor Efficacy of Taxanes <i>In Vitro</i> and <i>In Vivo</i>: Preclinical Studies as Guidance for Clinical Development and Trial Design

Optimization of dosing schedule of TAS-119 HCl salt in combination with docetaxel in a xenograft model in mice.</p

Table S1 from Aurora A Inhibitor TAS-119 Enhances Antitumor Efficacy of Taxanes <i>In Vitro</i> and <i>In Vivo</i>: Preclinical Studies as Guidance for Clinical Development and Trial Design

Material list</p

Synthesis of the New Mannosidase Inhibitors, Diversity-Oriented 5-Substituted Swainsonine Analogues, via Stereoselective Mannich Reaction

5α-Substituted swainsonine analogues were synthesized by Mannich reaction of an in situ generated (−)-swainsonine iminium ion intermediate. 5α-Substituted swainsonine analogues were epimerized to their 5β-isomers in protic solvent

Figure S5 from Aurora A Inhibitor TAS-119 Enhances Antitumor Efficacy of Taxanes <i>In Vitro</i> and <i>In Vivo</i>: Preclinical Studies as Guidance for Clinical Development and Trial Design

TAS-119 was compared to MK-5108 in in vivo HeLa-luc xenograft model.</p

Figure S3 from Aurora A Inhibitor TAS-119 Enhances Antitumor Efficacy of Taxanes <i>In Vitro</i> and <i>In Vivo</i>: Preclinical Studies as Guidance for Clinical Development and Trial Design

Four hours after oral administration of TAS-119 HCl salt, phosphorylation of histone H3 in tumor (a) and skin (b) tissues was monitored using western blotting.</p

Synthesis of the New Mannosidase Inhibitors, Diversity-Oriented 5-Substituted Swainsonine Analogues, via Stereoselective Mannich Reaction

5α-Substituted swainsonine analogues were synthesized by Mannich reaction of an in situ generated (−)-swainsonine iminium ion intermediate. 5α-Substituted swainsonine analogues were epimerized to their 5β-isomers in protic solvent

Fiugre S2 from Aurora A Inhibitor TAS-119 Enhances Antitumor Efficacy of Taxanes <i>In Vitro</i> and <i>In Vivo</i>: Preclinical Studies as Guidance for Clinical Development and Trial Design

(a) Structure of compound #1. (b) IC50 value of compound #1 for each recombinant Aurora kinase. (c) Fold enhancement of GI50 of paclitaxel by compound #1 in HeLa cells. (d) Expression changes of SAC-related genes</p

Supplementary Material & Method from Aurora A Inhibitor TAS-119 Enhances Antitumor Efficacy of Taxanes <i>In Vitro</i> and <i>In Vivo</i>: Preclinical Studies as Guidance for Clinical Development and Trial Design

Supplementary Material & Method</p