Debio 0932 (CUDC-305) 是一種可口服的 HSP90 抑制劑，對 HSP90α 和 HSP90β 的 IC50 值分別為 100 和 103 nM。
0932 (CUDC-305) binds to the tumor HSP90 complex with a mean IC50 of 48.8 nM. Debio 0932 (1 μM) promotes degradation of multiple HSP90 client proteins in cancer cell lines. Debio 0932 also shows inhibitory activities against the proliferation of 40 cancer cell lines (containing 34 solid and 6 hematologic tumor-derived lines) with an IC50 ranging from 40 to 900 nM (mean IC50, 220 nM)[1]. Debio 0932 strongly binds to cancer-derived HSP90 complex with an IC50 of 61.2 nM in H1975 cells and 74.2 nM in H1993 cells, respectively. Debio 0932 (CUDC-305, 1 μM) durably induces oncoprotein degradation in NSCLC cell lines with mutations that can confer resistance to erlotinib[3].
Debio 0932 (CUDC-305, 30 mg/kg, p.o.) exhibits favorable pharmacokinetic profiles in tumor-bearing nude mice. Debio 0932 (160 mg/kg, p.o.) causes degradation of HSP90 client proteins, suppresses tumor growth, and also prolongs survival in various animal models of U87MG glioblastoma. Debio 0932 (40, 80, or 160 mg/kg, p.o.) also dose-dependently inhibits tumor growth in the U87MG s.c. tumor model by every-other-day (q2d) dosing[1]. Debio 0932 (80 mg/kg, p.o.) significantly alleviates psoriasis by day 11 and decreases epidermal thickness in psoriasis xenograft transplantation model[2]. Debio 0932 (CUDC-305) is able to cross the blood-brain barrier. Debio 0932 (80, 120, and 160 mg/kg, p.o.) shows dose-dependent inhibition of tumor growth in the H1975 subcutaneous tumor model. Debio 0932 (160 mg/kg, p.o.) also promotes antitumor activity in the erlotinib-resistant H1975 subcutaneous tumor model[3].
關鍵字： 1061318-81-7;
廣州優(yōu)南科技有限公司，是一家集研發(fā)、生產(chǎn)、銷售于一體的高新技術(shù)企業(yè)，為全球生物醫(yī)藥企業(yè)、高校及科研院提供生命科學研究的產(chǎn)品與服務。
優(yōu)南擁有自主研發(fā)的品牌ULS，為客戶提供超過50000的工具化合物(小分子抑制劑/激動劑、標準品/對照品、熒光標記染料及探針)、醫(yī)藥原料及中間體、新型材料。