生物活性 | |||
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描述 | Tyrosine Kinase nonreceptor 2 (TNK2) is a cytoplasmic kinase also known as ACK1 (activated CDC42-associated kinase) which is part of a family of cytoplasmic tyrosine kinases. TNK2 mutations have been found in renal cancer cells and also in lung, ovarian, and gastric cancers[2]. XMD8-87 is a potent TNK2 inhibitor with IC50 values of 38 and 113 nM for the D163E and R806Q mutations, respectively. XMD8-87 potently inhibits phosphorylation of TNK2 truncation mutations found in solid tumor types. But, it’s very highly cleared in vivo in rodent PK studies[3]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.24mL 0.45mL 0.22mL |
11.22mL 2.24mL 1.12mL |
22.45mL 4.49mL 2.24mL |
参考文献 |
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