MK-5108也叫VX-689,是一种新型有效选择性Aurora A激酶(AAK)抑制剂,通过竞争性结合AAK的ATP结合位点,有效抑制AAK活性,IC50值为0.064 nM。MK-5108对Aurora家族的其他激酶也有抑制作用,作用于Aurora B激酶的IC50值为14 nM,Aurora C激酶的IC50值为12 nM。MK-5108已被广泛研究,发现其对各种癌症包括乳腺癌、宫颈癌、结直肠癌、卵巢癌和胰腺癌均具有抗肿瘤活性。
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MK-5108 (VX-689)
CAS number:1010085-13-8 molecular formula:C22H21ClFN3O3S
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| Chinese alias | - | ||
| English alias | HMS3656D06 | NCGC00024591-03 | BRD-K53665955-001-01-4 | GTPL8061 | MK 5108 | NSC800796 | NSC-800796 | MFCD22124479 | trans-4-(3-chloro-2-fluorophenoxy)-1-[[6-(1,3-thiazol-2-ylamino)pyridin-2-yl]methyl]cyclohexane-1-carboxylic acid | SW220174-1 | trans-4-( | ||
| CAS number | 1010085-13-8 | molecular formula | C22H21ClFN3O3S |
| molecular weight | 461.94 g/mol | Exact mass | - |
| PSA | 113.000 Ų | logp | 5.4 |
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