1061318-81-7
中文名稱
DEBIO 0932
英文名稱
Debio 0932 ,CUDC-305
CAS
1061318-81-7
分子式
C22H30N6O2S
分子量
442.58
MOL 文件
1061318-81-7.mol
更新日期
2024/12/18 18:02:15
1061318-81-7 結(jié)構(gòu)式
基本信息
中文別名
德比奧 0932BIO 0932
化合物 T15088
HSP90抑制劑(DEBIO 0932)
英文別名
CS-1423bio 0932
CUDC-305
Debio 0932
Debio 0932 ,CUDC-305
CUDC-305 (DEBIO-0932 )
1H-Imidazo[4,5-c]pyridine-1-ethanamine, 4-amino-2-[[6-(dimethylamino)-1,3-benzodioxol-5-yl]thio]-N-(2,2-dimethylpropyl)-
所屬類別
生物化工：激動(dòng)劑抑制劑物理化學(xué)性質(zhì)
沸點(diǎn)654.8±65.0 °C(Predicted)
密度1.32±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO:33.0(Max Conc. mg/mL);74.56(Max Conc. mM)
酸度系數(shù)(pKa)10.02±0.19(Predicted)
形態(tài)結(jié)晶固體
顏色White to yellow
應(yīng)用領(lǐng)域
用途1
一種HSP90(熱休克蛋白90)抑制劑，對(duì) HSP90α和 HSP90β的IC50值分別為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.