芬戈莫德(FTY720)是一種免疫抑制劑,通常用于治療多發(fā)性硬化癥,也有抗癌作用,可以作為HDACi(組蛋白脫乙酰酶抑制劑)[1]。

在體外,在7.5或10μM時,芬戈莫德誘導(dǎo)D283和DAOY培養(yǎng)物中的細胞活力明顯下降,還導(dǎo)致乙酰化H3的水平明顯增加[1]。在體外,Fingolimod對雄性激素依賴性和非依賴性前列腺癌細胞顯示出細胞毒性抗增殖作用,IC50范圍為3.0±0.3至6.8±1.7 μM[2]。Jurkat T淋巴細胞接觸Fingolimod后,以時間和濃度依賴的方式抑制延遲整流K+ 電流(IK(DR))的振幅,IC50值為1.51 μM[3]。Fingolimod降低了Ph(+)和Ph(-)ALL細胞系和患者樣本的增殖和生存能力,其生存能力的IC50值在5.3至7.9 μM之間[4] 。Fingolimod對OSCC細胞系SCC4、SCC25和SCC2095的生存能力有不同程度的抑制,IC50值分別為6.1、6.3和4.5 μM[5]。

體內(nèi)試驗表明,E13 C57BL/6野生型小鼠在照射4周后,用1 mg/kg的劑量處理,可明顯提高DG(齒狀回)和SVZ(室下區(qū))中DCX+神經(jīng)元的存活率,同時增殖細胞也有輕微增加[6]。在體內(nèi),5xFAD小鼠接受1 mg/kg/day的芬戈莫德治療后,外周血淋巴細胞計數(shù)和大腦Aβ 水平均下降,但接受0.03 mg/kg/day的治療后,記憶力得到改善,大腦小膠質(zhì)細胞和星形膠質(zhì)細胞的激活減少,海馬的GABA和甘油磷酸膽堿水平恢復(fù),對循環(huán)淋巴細胞計數(shù)沒有影響[7]。在體內(nèi),C57BL/6JOlaHsd小鼠接受0.5 mg/kg芬戈莫德治療后,病變大小(中風(fēng))增加,但同側(cè)腦萎縮減少,對行為結(jié)果沒有影響[8]。

產(chǎn)品性質(zhì)：

Cas No.：162359-56-0

別名：鹽酸芬戈莫德; FTY720

化學(xué)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

儲存條件：Store at -20°C

注意事項：

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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.