VX-680 (Tozasertib, MK-0457)是一种pan-Aurora抑制剂,对Aurora A作用最强,Kiapp为0.6 nM,而对Aurora B/Aurora C的作用稍弱,对Aurora A选择性比其他55种激酶强高100倍。A potent and selective pan-ARK inhibitor VX-680 (Tozasertib, MK-0457) is a pan-Aurora inhibitor, mostly against Aurora A with Kiapp of 0.6 nM, less potent towards Aurora B/Aurora C and 100-fold more selective for Aurora A than 55 other kinases A potent and selective pan-ARK inhibitor;Aurora Kinase抑制剂
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Tozasertib
CAS number:639089-54-6 molecular formula:C23H28N8OS
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| Chinese alias | 陶扎色替 | ||
| English alias | VX-680 | MK-0457 | Cyclopropane carboxylic acid{4-[4-(4-methyl-piperazin-1-yl)-6-(5-methyl-2H-pyrazol-3-ylamino)-pyrimidin-2-ylsulphanyl]-phenyl}-amide | Cyclopropanecarboxamide, N-[4-[[4-(4-methyl-1-piperazinyl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]-2-pyri | ||
| CAS number | 639089-54-6 | molecular formula | C23H28N8OS |
| molecular weight | 464.6 g/mol | Exact mass | - |
| PSA | 127.000 Ų | logp | 3.4 |
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