OSI-930是一种新型有效的Flt1、激酶插入结构域受体(KDR)、CSF-1R、Lck、c-Raf和活化受体酪氨酸激酶Kit的抑制剂,IC50值分别为8、9、15、22、41和80 nM。 在其存活高度依赖于Kit 信号的HMC-1细胞系中,OSI-930抑制细胞增殖,诱导细胞凋亡。反之,在正常培养条件下的COLO-205细胞系中,OSI-930不抑制细胞生长。 OSI-930可时间和浓度依赖地使P450 3A4失去活性。此外,OSI-930可减少P450 3A4的CO差光谱。 OSI-930是一种有效的Kit (c-Kit), KDR和CSF-1R抑制剂,IC50分别为80 nM, 9 nM和15 nM,对Flt-1, c-Raf和Lck具有适度的抑制活性,对PDGFRα/β, Flt-3和Abl抑制活性较弱。
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OSI-930
CAS number:728033-96-3 molecular formula:C22H16F3N3O2S
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| Chinese alias | - | ||
| English alias | AKOS026750567 | BDBM50356877 | SMR004701347 | HMS3295O11 | OSI 930 | NSC800811 | NSC-800811 | CELASTROL [MI] | CHEBI:91433 | BRD-K25340465-001-01-2 | 3-(quinolin-4-ylmethylamino)-N-(4-(trifluoromethoxy)phenyl)thiophene-2-carboxamide | OSI930 | OSI-930 | N | ||
| CAS number | 728033-96-3 | molecular formula | C22H16F3N3O2S |
| molecular weight | 443.45 g/mol | Exact mass | - |
| PSA | 91.500 Ų | logp | 6.2 |
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