生物活性 | |||
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描述 | Tosedostat (CHR-2797) is an inhibitor of aminopeptidases that blocks a critical step in the protein degradation and re-synthesizes intracellular pathway. This orally bioavailable agent has shown promising activity in vitro and in early clinical trials for patients with relapsed/refractory AML (acute myeloid leukaemia) [1]. CHR-2797 demonstrated marked in vitro cytotoxicity in AML samples and strong synergy with Cytarabine (Ara-C), but significantly less cytotoxicity to normal marrow progenitors[2]. Additionally, when given in combination with morphine, tosedostat exerts a synergistic analgesic effect resulting in a reduction of effective dosages required to achieve the same analgesic effect[3]. Tosedostat with capecitabine displayed tolerable toxicity, and prolonged disease control in a subset of patients[4]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.46mL 0.49mL 0.25mL |
12.30mL 2.46mL 1.23mL |
24.60mL 4.92mL 2.46mL |
参考文献 |
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