化学性质：                                                                                                             

产品描述：                                                                                                            

TAS-116 is an oral bioavailable, ATP-competitive, highly specific HSP90α/HSP90β inhibitor (Kis of 34.7 nM and 21.3 nM, respectively) without inhibiting other HSP90 family proteins such as GRP94[1]. TAS-116 demonstrates less ocular toxicity[2].

TAS-116 binds not only to the conventional-binding pockets as existing Hsp-90 inhibitors, but also to a novel-binding pocket. Such a unique binding mode makes TAS-116 highly specific for Hsp-90α/β without inhibiting other Hsp-90 family proteins such as GRP94 in endoplasmic reticulum or TRAP-1 in mitochondria[3].TAS-116 (0-5 μM, 48 hours) inhibits human retinal pigment epithelial ARPE-19 cell lines and NCI-H929 MM cells growth[2].More significant degradation of p-C-Raf and p-MEK1/2, HSP90 client proteins and key RAS/RAF/MEK pathway regulators, is triggered by TAS-116 (0.125-1 μM, 24 hours) than 17-AAG in INA6 and NCI-H929 MM cells[2].|| Cell Viability Assay[2]||Cell Line:|Human retinal pigment epithelial ARPE-19 cell lines and NCI-H929 MM cells|Concentration:|0-5 μM|Incubation Time:|48 hours|Result:|Inhibited NCI-H929 MM cells growth with an IC50 of 0.35 μM.|| Western Blot Analysis[2]||Cell Line:|MM cell lines INA6 and NCI-H929 cells|Concentration:|0.125-1 μM|Incubation Time:|24 hours|Result:|Targeted potently HSP90 client proteins including C-Raf and MEK1/2; as well as inhibited upregulation of HSP27 and overcomes 17-AAG resistance mechanisms.

特别提醒：