CAS: 1061318-81-7 | 分子式: C22H30N6O2S | 分子量: 443 | EINECS号: |
沸点
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654.8±65.0 °C(Predicted)
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密度
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1.32±0.1 g/cm3(Predicted)
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溶解度
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DMSO:33.0(Max Conc. mg/mL);74.56(Max Conc. mM)
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形态
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A crystalline solid
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酸度系数(pKa)
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10.02±0.19(Predicted)
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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.
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