中文同义词:
HSP90抑制剂(DEBIO 0932)
英文名称:
Debio 0932 ,CUDC-305
英文同义词:
Debio 0932;Debio 0932 ,CUDC-305;CUDC-305 (DEBIO-0932 );CUDC-305;CS-1423;1H-Imidazo[4,5-c]pyridine-1-ethanamine, 4-amino-2-[[6-(dimethylamino)-1,3-benzodioxol-5-yl]thio]-N-(2,2-dimethylpropyl)-
沸点
654.8±65.0 °C(Predicted)
密度
1.32±0.1 g/cm3(Predicted)
酸度系数(pKa)
10.02±0.19(Predicted)
用途
一种HSP90(热休克蛋白90)抑制剂,对 HSP90α和 HSP90β的IC50值分别为100和103nM。Debio 0932 is a novel heat shock protein 90 (HSP90) inhibitor with strong affinity for HSP90 alpha/beta, high oral bioavailability and potent anti-proliferative activity against a broad range of cancer cell lines (with a mean IC50 of 220 nmol/L), including many non-small cell lung cancer (NSCLC) cell lines which are resistant to standard-of-care (SOC) agents. Debio 0932 potently inhibits tumour growth in subcutaneous xenograft models of a number of solid and haematological malignancies, including models of NSCLC which harbour mutations conferring acquired or primary erlotinib resistance.