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鲁索利替尼 (Synonyms: 芦可替尼; INCB18424)

目录号: PC78824 纯度: ≥98%

Ruxolitinib (INCB018424) is a JAK1/2 inhibitor (IC50=3.3/2.8 nM) that is potent and selective. Rixolitinib exhibits antitumor activity and induces autophagy and apoptosis.

CAS No. :941678-49-5

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中文名称	鲁索利替尼
中文别名	苹果酸卡博替尼;卡博替尼苹果酸盐;苹果酸盐;N-[4-[(6,7-二甲氧基-4-喹啉基)氧基]苯基]-N'-(4-氟苯基)-1,1-环丙烷二甲酰胺 (S)-苹果酸盐;卡博替尼;卡博替尼杂质;苹果酸卡博替尼（CABOZANTINIB S-MALATE）;苹果酸卡博替尼（XL184）;卡博替尼苹果酸盐 ;Cabozantinib (S)-苹果酸盐
英文名称	Ruxolitinib (INCB018424)
英文别名	quinolinyl)oxy]phenyl]-N'-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide;Cabozantinib;Cabozantinib malate (XL184);(2S)-2-Hydroxybutanedioic acid compd. with N-[4-[(6,7-dimethoxy-4-quinolinyl)oxy]phenyl]-N'-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide (1:1);1-N-[4-(6,7-dimethoxyquinolin-4-yl)oxyphenyl]-1-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide,(2S)-2-hydroxybutanedioic acid;Cabozantinib L-Malate Salt;Cabozantinib S-malate;XL-184 L(-)-Malic acid salt;Cabozantinib malate;Cabozantinib malate salt;cyclopropane-1,1-dicarboxylic acid [4-(6,7-dimethoxyquinoline-4-yloxy)phenyl]amide (4-fluoro-phenyl)amide (L)-malate salt;cyclopropane-1,1-dicarboxylic acid [4-(6,7-dimethoxy-quinoline-4-yloxy)-phenyl]-amide (4-fluoro-phenyl)-amide L-malate;N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-d;Smalate;UNII-DR7ST46X58;XL184;XL-184
Cas No.	941678-49-5
分子式	C₁₇H₁₈N₆
分子量	306.37
包装储存	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.

产品详情	Ruxolitinib (INCB018424) is a JAK1/2 inhibitor (IC50=3.3/2.8 nM) that is potent and selective. Rixolitinib exhibits antitumor activity and induces autophagy and apoptosis.
生物活性	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]
储存方式	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.
参考文献	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.

溶解度数据	H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 60 mg/mL (195.85 mM) Ethanol: < 1 mg/mL (insoluble or slightly soluble) 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5.7 mg/mL (18.61 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.

溶解度数据

H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 60 mg/mL (195.85 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5.7 mg/mL (18.61 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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