产品说明书

Tosedostat

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Chemical Structure| 238750-77-1 同义名 : CHR-2797
CAS号 : 238750-77-1
货号 : A212860
分子式 : C21H30N2O6
纯度 : 99%+
分子量 : 406.473
MDL号 : MFCD13185162
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：
生物活性
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
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

[1]DiNardo CD, Cortes JE. Tosedostat for the treatment of relapsed and refractory acute myeloid leukemia. Expert Opin Investig Drugs. 2014;23(2):265-272

[2]Jenkins C, Hewamana S, Krige D, Pepper C, Burnett A. Aminopeptidase inhibition by the novel agent CHR-2797 (tosedostat) for the therapy of acute myeloid leukemia. Leuk Res. 2011;35(5):677-681

[3]Singh R, Xie W, Williams J, Vince R, More SS. Discovery of Anticancer Clinical Candidate, Tosedostat, As an Analgesic Agent. ACS Chem Neurosci. 2019;10(9):4007-4017

[4]Grierson P, Teague A, Suresh R, et al. Phase Ib/II study combining tosedostat with capecitabine in patients with advanced pancreatic adenocarcinoma. J Gastrointest Oncol. 2020;11(1):61-67