Tosedostat is a aminopeptidase inhibitor with IC50 of 220, > 1000 nM for aminopeptidase N and aminopeptidase B respectively.
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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]. |
计算器 | ||||
存储液制备 | 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 |
CAS号 | 238750-77-1 |
分子式 | C21H30N2O6 |
分子量 | 406.473 |
别名 | CHR-2797 |
运输 | 蓝冰 |
存储条件 |
粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 25 mg/mL(61.5 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |