Eflornithine hydrochloride hydrate

CAS号

96020-91-6

分子式

C6H15ClF2N2O3

主要靶点

Decarboxylase

仅限科研使用

Cat No : CM03635

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Synonyms

inhibit|DFMO hydrochloride|DFMO hydrochloride hydrate|DFMO hydrochloride Hydrate|Decarboxylase|Difluoromethylornithine hydrochloride hydrate|Difluoromethylornithine hydrochloride Hydrate|Eflornithine Hydrochloride|Eflornithine hydrochloride Hydrate|Eflornithine hydrochloride hydrate|Eflornithine hydrochloride Monohydrate|Eflornithine hydrochloride|a-difluoromethylornithine hydrochloride Hydrate|MDL-71782 hydrochloride|MDL-71782 hydrochloride hydrate|MDL-71782 hydrochloride Hydrate|Inhibitor|Parasite|RMI-71782 hydrochloride|RMI-71782 hydrochloride Hydrate|RMI-71782 hydrochloride hydrate|α-difluoromethylornithine hydrochloride|α-difluoromethylornithine hydrochloride Hydrate|α-difluoromethylornithine hydrochloride hydrate|依氟鸟氨酸盐酸盐一水合物



产品信息

CAS号 96020-91-6
分子式 C6H15ClF2N2O3
主要靶点 Decarboxylase
主要通路 其他|代谢
分子量 236.64
纯度 99.64%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 inhibit|DFMO hydrochloride|DFMO hydrochloride hydrate|DFMO hydrochloride Hydrate|Decarboxylase|Difluoromethylornithine hydrochloride hydrate|Difluoromethylornithine hydrochloride Hydrate|Eflornithine Hydrochloride|Eflornithine hydrochloride Hydrate|Eflornithine hydrochloride hydrate|Eflornithine hydrochloride Monohydrate|Eflornithine hydrochloride|a-difluoromethylornithine hydrochloride Hydrate|MDL-71782 hydrochloride|MDL-71782 hydrochloride hydrate|MDL-71782 hydrochloride Hydrate|Inhibitor|Parasite|RMI-71782 hydrochloride|RMI-71782 hydrochloride Hydrate|RMI-71782 hydrochloride hydrate|α-difluoromethylornithine hydrochloride|α-difluoromethylornithine hydrochloride Hydrate|α-difluoromethylornithine hydrochloride hydrate|依氟鸟氨酸盐酸盐一水合物

体内活性

方法:为检测体内抗感染活性,将 Eflornithine hydrochloride hydrate (25-50 mg/kg) 和 hydroxyurea (50-100 mg/kg) 口服给药给 B.microti 感染的 BALB/c 小鼠,每天一次,持续 5 天。 结果:口服 hydroxyurea 和 Eflornithine 分别抑制了小鼠体内微小双歧杆菌的增殖 60.1% 和 78.2%。hydroxyurea-DA 和 Eflornithine-DA 联合治疗显示出比单一治疗更高的化疗疗效。[3]

体外活性

方法:卵巢癌细胞 SKOV-3 用 Eflornithine hydrochloride hydrate (1-100 μM) 处理 48 h,通过 PrestoBlue assay 检测细胞活力。 结果:Eflornithine 以剂量依赖的方式显著抑制 SKOV-3 细胞的存活率。[1] 方法:MYCN2 (-) 和 MYCN2 (+) NB 细胞用 Eflornithine hydrochloride hydrate (5 mM) 和 putrescine/spermidine/spermine 处理 72 h,通过 wound healing assay 检测细胞迁移。 结果:未经处理的对照细胞与 Eflornithine 处理的细胞之间的细胞迁移存在显著差异。Eflornithine 分别在MYCN2 (-) 和MYCN2 (+) 细胞中抑制了 73% 和 72% 的细胞迁移。在培养基中补充多胺可以减轻 Eflornithine 对 MYCN2 (-) 和 MYCN2 (+) 的影响。[2]

溶解度

H2O:83.33 mg/mL (352.14 mM);DMSO:2.77 mg/mL (11.71 mM)

细胞实验

BY2 cells are treated with or without cryptogein in the presence or absence of DFMO(Difluoromethylornithine) and monitered the effect of chemicals on cell growth. (Only for Reference)

参考文献

1.Hwang WY, et al. Difluoromethylornithine Induces Apoptosis through Regulation of AP-1 Signaling via JNK Phosphorylation in Epithelial Ovarian Cancer. Int J Mol Sci. 2021 Sep 23;22(19):10255.
2.Koomoa DL, et al. DFMO/eflornithine inhibits migration and invasion downstream of MYCN and involves p27Kip1 activity in neuroblastoma. Int J Oncol. 2013 Apr;42(4):1219-28.
3.El-Saber, et al. Safety and efficacy of hydroxyurea and eflornithine against most blood parasites Babesia and Theileria. PLoS One. 2020 Feb 13;15(2):e0228996.
4.Kumar A, et al. A method to improve the efficacy of topical eflornithine hydrochloride cream. Drug Deliv. 2016 Jun;23(5):1495-501.
5.Lipke DW, et al. Eflornithine alters changes in vascular responsiveness associated with coarctation hypertension. Clin Exp Hypertens. 1997 Apr;19(3):297-312.
6.Dial C N. Modulation of Coxsackievirus Protease Activity by Polyamines[D]. Loyola University Chicago. 2019.
7.Dial C N, Tate P M, Kicmal T M, et al. Coxsackievirus B3 Responds to Polyamine Depletion via Enhancement of 2A and 3C Protease Activity[J]. Viruses. 2019 Apr 30;11(5).
8.Kicmal T M, Tate P M, Dial C N, et al. Polyamine depletion abrogates enterovirus cellular attachment[J]. Journal of virology. 2019, 93(20): e01054-19.
9.Mastrodomenico V, Esin J J, Graham M L, et al. Polyamine depletion inhibits bunyavirus infection via generation of noninfectious interfering virions[J]. Journal of virology. 2019 May 1. pii: JVI.00530-19.

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