Ruxolitinib (INCB018424) (Synonyms: INCB 018424) |
| カタログ番号GC14191 |
強力で選択的なJAK1/JAK2阻害剤
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Cas No.: 941678-49-5
Sample solution is provided at 25 µL, 10mM.
Ruxolitinib (INCB018424), as an inhibitor, inhibits Janus-associated kinases (JAKs)JAK1 and JAK2 with IC50 values of 3.3 nM and 2.8 nM, respectively. Ruxolitinib mediates several cytokine and growth factor signaling important for hematopoietic and immune function[1-3].
Ruxolitinib (INCB018424) (500nM-50μM;30min) significantly inhibited the production of IL-6, TNF-α and MCP-1 as induced by A23817 and substance P in HMC1 cells[4]. Ruxolitinib(0-400nM; 3days) reduced the level of cytokine release in CAR-T cells[5].
Ruxolitinib (INCB018424) (30 mg/kg; p.o.; twice a day 14 days) treatment alleviated renal damage in UUO mice[6]. Ruxolitinib(twice daily by oral gavage; 2 weeks) treatment improves viability and splenomegaly in a JAK2V617F-driven model of malignant disease[3]. Treatment of Fancc-/- mice with ruxolitinib(45 mg/kg; i.p; 5 days/week) decreased anemia, enhanced granulocytosis, delayed clonal progression and prolonged survival during repeated emergency granulopoiesis episodes[7].
References:
[1]. Becker H, Engelhardt M, et,al. Ruxolitinib. Recent Results Cancer Res. 2014;201:249-57. doi: 10.1007/978-3-642-54490-3_16. PMID: 24756798.
[2]. Ajayi S, Becker H, et,al. Ruxolitinib. Recent Results Cancer Res. 2018;212:119-132. doi: 10.1007/978-3-319-91439-8_6. PMID: 30069628.
[3]. Quintás-Cardama A, Vaddi K, 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. doi: 10.1182/blood-2009-04-214957. Epub 2010 Feb 3. PMID: 20130243; PMCID: PMC3953826.
[4]. Hermans MAW, Schrijver B, et,al. The JAK1/JAK2- inhibitor ruxolitinib inhibits mast cell degranulation and cytokine release. Clin Exp Allergy. 2018 Nov;48(11):1412-1420. doi: 10.1111/cea.13217. Epub 2018 Aug 3. PMID: 29939445.
[5]. Xu N, Yang XF, et,al. Ruxolitinib reduces severe CRS response by suspending CAR-T cell function instead of damaging CAR-T cells. Biochem Biophys Res Commun. 2022 Mar 5;595:54-61. doi: 10.1016/j.bbrc.2022.01.070. Epub 2022 Jan 20. PMID: 35101664.
[6]. Bai Y, Wang W, et,al. Ruxolitinib Alleviates Renal Interstitial Fibrosis in UUO Mice. Int J Biol Sci. 2020 Jan 1;16(2):194-203. doi: 10.7150/ijbs.39024. PMID: 31929748; PMCID: PMC6949153.
[7]. Hasan S, Hu L, et,al. Ruxolitinib ameliorates progressive anemia and improves survival during episodes of emergency granulopoiesis in Fanconi C-/- mice. Exp Hematol. 2022 May;109:55-67.e2. doi: 10.1016/j.exphem.2022.03.001. Epub 2022 Mar 9. PMID: 35278531; PMCID: PMC9064927.
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