生物活性 | |||
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描述 | Src is among the first oncogenes to be discovered and encodes a non-receptor protein tyrosine kinase that regulates many cancer-related cellular processes including mitogenesis, angiogenesis, adhesion, invasion, migration, and survival. DGY-06-116 is an irreversible and selective covalent inhibitor of Src with an IC50 value of 2.6 nM. DGY-06-116 covalently binds to Src in a manner similar to SM1-71, where the p-loop must kink to establish the covalent bond[1]. | ||
作用机制 | DGY-06-116 forms a covalent bond with Cys-280, and hydrophobic interactions with the back pocket significantly contribute to affinity[1]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.67mL 0.33mL 0.17mL |
8.37mL 1.67mL 0.84mL |
16.75mL 3.35mL 1.67mL |
参考文献 |
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