Ruxolitinib (INCB18424) 是有效，选择性的 JAK1/2 抑制剂， IC50 值分别为 3.3 nM 和 2.8 nM，选择性是 JAK3 的 130 多倍。Ruxolitinib 诱导自噬 (autophagy)，通过毒性线粒体自噬 (mitophagy) 杀死肿瘤细胞。

方法：Ba/F3-EpoR-JAK2V617F 细胞用 Ruxolitinib (0-10 μM) 处理 48 h，使用 Cell-Titer Glo 检测的细胞活力。
结果：Ruxolitinib 剂量依赖性降低细胞活力，IC50 为 126 nM。[1]
方法：霍奇金淋巴瘤细胞 HDLM-2 用 Ruxolitinib (10-100 nM) 处理 24 h，使用 Western Blot 方法检测靶点蛋白表达水平。
结果：Ruxolitinib 显著抑制下游活性 p-STAT3 和 p-STAT5，且呈剂量依赖性，而总 STAT3 和 STAT5 水平保持不变。[2]
方法：为检测体内抗肿瘤活性，将 Ruxolitinib (3-30 mg/kg，5% dimethyl acetamide, 0.5% methocellulose) 灌胃给药给携带肿瘤 Ba/F3-JAK2V617F 的 BALB/c 小鼠，每天两次，持续三周。
结果：Ruxolitinib 显著降低了脾肿大和炎症细胞因子的循环水平，并优先消除了肿瘤细胞，从而显著延长了生存期，而没有骨髓抑制或免疫抑制作用。[1]
方法：为检测体内抗肿瘤活性，将 Ruxolitinib (150 mg/kg) 口服给药给携带人结直肠肿瘤 LS411N 的 BALB/c nude 小鼠，每两天一次，持续两周。
结果：口服 Ruxolitinib 可显著抑制人结直肠肿瘤的体内生长，而不会引起肝毒性。[3]

store at low temperature,keep away from direct sunlight,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

1.Quintás-Cardama A, et al. Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms. Blood. 2010 Apr 15;115(15):3109-17.
2.Lee S, et al. Ruxolitinib significantly enhances in vitro apoptosis in Hodgkin lymphoma and primary mediastinal B-cell lymphoma and survival in a lymphoma xenograft murine model. Oncotarget. 2018 Jan 18;9(11):9776-9788.
3.Li X, et al. Ruxolitinib induces apoptosis of human colorectal cancer cells by downregulating the JAK1/2-STAT1-Mcl-1 axis. Oncol Lett. 2021 May;21(5):352.
4.Datta J, Lamichhane P, Dai X, et al. Combined MEK and STAT3 inhibition reprograms the tumor microenvironment to overcome immunotherapy resistance in pancreatic cancer[J]. bioRxiv. 2021
5.Ryan M M, Patel M, Hogan K, et al. Ruxolitinib inhibits IFNγ licensing of human bone marrow derived Mesenchymal Stromal Cells[J]. Transplantation and Cellular Therapy. 2021, 27(5): 389. e1-389. e10.
6.Chen X, Gao C, Cheng Z, et al. Ruxolitinib exerts neuroprotection via repressing ferroptosis in a mouse model of traumatic brain injury[J]. Experimental Neurology. 2021: 113762.
7.Zhang C, Yan Y, He H, et al. IFN-stimulated P2Y13 protects mice from viral infection by suppressing the cAMP/EPAC1 signaling pathway[J]. Journal of molecular cell biology. 2018 Aug 22.
8.Espinet E, Gu Z, Imbusch C D, et al. Cancer Discovery. 2021, 11(3): 638-659.

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