芬戈莫德(FTY720)是一种免疫抑制剂,通常用于治疗多发性硬化症,也有抗癌作用,可以作为HDACi(组蛋白脱乙酰酶抑制剂)[1]。

在体外,在7.5或10µM时,芬戈莫德诱导D283和DAOY培养物中的细胞活力明显下降,还导致乙酰化H3的水平明显增加[1]。在体外,Fingolimod对雄性激素依赖性和非依赖性前列腺癌细胞显示出细胞毒性抗增殖作用,IC50范围为3.0±0.3至6.8±1.7 µM[2]。Jurkat T淋巴细胞接触Fingolimod后,以时间和浓度依赖的方式抑制延迟整流K+ 电流(IK(DR))的振幅,IC50值为1.51 µM[3]。Fingolimod降低了Ph(+)和Ph(-)ALL细胞系和患者样本的增殖和生存能力,其生存能力的IC50值在5.3至7.9 µM之间[4] 。Fingolimod对OSCC细胞系SCC4、SCC25和SCC2095的生存能力有不同程度的抑制,IC50值分别为6.1、6.3和4.5 µM[5]。

体内试验表明,E13 C57BL/6野生型小鼠在照射4周后,用1 mg/kg的剂量处理,可明显提高DG(齿状回)和SVZ(室下区)中DCX+神经元的存活率,同时增殖细胞也有轻微增加[6]。在体内,5xFAD小鼠接受1 mg/kg/day的芬戈莫德治疗后,外周血淋巴细胞计数和大脑Aβ 水平均下降,但接受0.03 mg/kg/day的治疗后,记忆力得到改善,大脑小胶质细胞和星形胶质细胞的激活减少,海马的GABA和甘油磷酸胆碱水平恢复,对循环淋巴细胞计数没有影响[7]。在体内,C57BL/6JOlaHsd小鼠接受0.5 mg/kg芬戈莫德治疗后,病变大小(中风)增加,但同侧脑萎缩减少,对行为结果没有影响[8]。

产品性质：

Cas No.：162359-56-0

别名：盐酸芬戈莫德; FTY720

化学名：2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol;hydrochloride

Canonical SMILES：CCCCCCCCC1=CC=C(C=C1)CCC(CO)(CO)N.Cl

分子式：C19H34ClNO2

分子量：343.94

溶解度：DMSO : ≥ 100 mg/mL; Water : 50 mg/mL

储存条件：Store at -20°C

注意事项：

为了您的安全和健康，请穿实验服并戴一次性手套操作。

References:

[1] Perla AS, et al. Fingolimod (Fingolimod) reduces viability and survival and increases histone H3 acetylation in medulloblastoma cells. Pediatr Hematol Oncol. 2020 Mar;37(2):170-175.

[2] Allam RM, et al. Fingolimod interrupts the cross talk between estrogen metabolism and sphingolipid metabolism within prostate cancer cells. Toxicol Lett. 2018 Jul;291:77-85.

[3] Chang WT, et al. Actions of Fingolimod (Fingolimod), a Sphingosine-1-Phosphate Receptor Modulator, on Delayed-Rectifier K+ Current and Intermediate-Conductance Ca2+-Activated K+ Channel in Jurkat T-Lymphocytes. Molecules. 2020 Oct 2;25(19):4525.

[4] Wallington-Beddoe CT, et al. Fingolimod produces caspase-independent cell death of acute lymphoblastic leukemia cells. Autophagy. 2011 Jul;7(7):707-15.

[5] Bai LY, et al. Fingolimod Induces Autophagy-Associated Apoptosis in Human Oral Squamous Carcinoma Cells, in Part, through a Reactive Oxygen Species/Mcl-1-Dependent Mechanism. Sci Rep. 2017 Jul 17;7(1):5600.

[6] Metzdorf J, et al. Fingolimod for Irradiation-Induced Neurodegeneration. Front Neurosci. 2019 Jul 9;13:699.

[7] Carreras I, et al. Dual dose-dependent effects of fingolimod in a mouse model of Alzheimer's disease. Sci Rep. 2019 Jul 29;9(1):10972.

[8] Diaz Diaz AC, et al. Preclinical Evaluation of Fingolimod in Rodent Models of Stroke With Age or Atherosclerosis as Comorbidities. Front Pharmacol. 2022 Jul 13;13:920449.