Danusertib (PHA-739358)是一种Aurora kinase抑制剂，作用于Aurora A/B/C时IC50为13 nM/79 nM/61 nM，适度有效作用于Abl， TrkA， c-RET和FGFR1，对Lck， VEGFR2/3， c-Kit， CDK2等作用效果稍弱。 Danusertib（PHA-739358），是吡咯并吡咯子系列的3-aminopyrazole衍生物，是aurora激酶家族的小分子抑制剂，显著抑制aurora B激酶(ABK)。这种pan-aurora激酶抑制剂还能够抑制其他的酪氨酸激酶，包括T315I突变体、RET、TRK-A和成纤维细胞生长因子受体-1（FGFR-1），这些酪氨酸激酶参与多种恶性肿瘤的形成，例如慢性髓性白血病（ CML）、急性淋巴细胞白血病（ALL）、甲状腺前列腺癌和乳腺癌。之前的研究表明，在不同的异种移植、自发的和转基因动物肿瘤模型中，danusertib具有显著的抗肿瘤活性，并具有有利的药代动力学和安全性。 Danusertib (PHA-739358)是一种Aurora kinase抑制剂，作用于Aurora A/B/C，无细胞试验中IC50为13 nM/79 nM/61 nM，适度有效作用于Abl，TrkA，c-RET和FGFR1，对Lck，VEGFR2/3，c-Kit，CDK2等作用效果稍弱。Danusertib 可诱导凋亡、细胞周期阻滞和自噬。 Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc.
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Danusertib (PHA-739358)
CAS number：827318-97-8 molecular formula：C26H30N6O3
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| Chinese alias | 达鲁舍替 | ||
| English alias | PHA739358 | DTXSID301002864 | AB05523 | Danusertib, PHA-739358 | Danusertib; PHA-739358 | N-(5-((2R)-2-methoxy-2-phenylacetyl)-1,4,5,6-tetrahydropyrrolo(3,4-c)pyrazol-3-yl)-4-(4-methylpiperazin-1-yl)benzamide | (R)-N-(5-(2-Methoxy-2-phenylacetyl)-1,4,5,6- | ||
| CAS number | 827318-97-8 | molecular formula | C26H30N6O3 |
| molecular weight | 474.55 g/mol | Exact mass | - |
| PSA | 93.800 Ų | logp | 1.8 |
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