AT13387, discovered by a high-throughput x-ray craystallography fragment-based platform, is a non-geldanamycin heat shock proterin 90 (HPS90), a molecule chaperone regulating signal transduction pathways for cell growth and survival, inhibitor reportedly resulting in client protein degradation, suppres...
AT13387是Hsp90抑制剂,对A375细胞的IC50为18nM,具有长效的抗肿瘤活性。注:本品仅可用于科研实验,严禁用于临床医疗及其他用途!CAS号:912999-49-6别名:Onalespib纯度:99.64%分子式:C24H31N3O3分子量:409.52结构式:储存条件:-20℃,有效期2年,溶入溶剂后-20℃请尽量在一个月内使用。相关搜索:Hsp90抑制剂(AT...
Onalespib is a synthetic, orally bioavailable, small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity. Onalespib selectively binds to Hsp90, thereby inhibiti
A novel Hsp90 inhibitor AT13387 induces senescence in EBV-positive nasopharyngeal carcinoma cells and suppresses tumor formation. Mol Cancer. 2013; 12: 128. Doi: 10. 1186/1476-4598-12-128.Chan KC, Ting CM, Chan PS, Lo MC, Lo KW, Curry JE, et al. A novel Hsp90 inhibitor AT13387 ...
The poly(ADP-ribose) polymerase inhibitor olaparib has shown antitumour activity in patients with platinum-sensitive, recurrent, high-grade serous ovarian cancer with or without BRCA1 or BRCA2 mutations. The aim of this study was to asse... Prof Amit M Oza FRCP a,Prof David Cibula MD b,...
Astex Therapeutics' AT13387, is a novel inhibitor of HSP90; a protein known to be involved in pancreatic tumorigenesis. Methods : In vivo studies were carried out in nude mice using a human pancreatic cancer cell line (miapaca2) xenograft model. Cell proliferation in pancreatic cancer cell-...
AT13387 is an orally bioavailable clinical candidate developed to inhibit heat shock protein 90 (Hsp90). This article describes a modified synthetic route for the multi-gram production of AT13387 in 46% overall yield. The modified synthetic route is short, avoids stringent reaction conditions and ...
The synthesis of C-5-substituted resorcinol amide AT13387, a known Hsp90 inhibitor currently in clinical trials, is reported without the use of phenolic protection in an overall yield of 13.4%. Biomimetic aromatization and Suzuki-Miyaura cross coupling approach were employed to synthesize the ...
Onalespib (AT13387) is a potent non-ansamycin HSP90 inhibitor. We hypothesised that the combination of onalespib and imatinib may be safe and effective in managing TKI-resistant GIST. Patients and methods In this dose-escalation study, we evaluated the safety and efficacy of combination once-...