Ruxolitinib-phosphate-INCB018424-phosphate-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemERuxolitinib phosphateCat. No.: HY-50858CAS No.: 1092939-17-7Synonyms: INCB018424 phosphate分式: CHNOP分量: 404.36作靶点: JAK; Autophagy; Mitophagy作通路: Epigenetics; JAK/STAT Signaling; Stem Cell/Wnt; Autophagy储存式: Powder -20C 3 years4C

2、2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 31 mg/mL (76.66 mM)H2O : 5.4 mg/mL (13.35 mM; Need ultrasonic and warming)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.4730 mL 12.3652 mL 24.7304 mL5 mM 0.4946 mL 2.4730 mL 4.9461 mL10 mM 0.24

3、73 mL 1.2365 mL 2.4730 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 Ruxolitinib phosphate is dissolved in 5% dimethyl acetamide, 0.5% methylcellulose2.BIOLOGICAL ACTIVITY物活性 Ruxolitinib phosphate种有效的 JAK1/2 抑制剂， IC50 分别为3.3 nM/2.8 nM，JAK3选择性130倍。1/3 Master of Small Molecules 您边的抑制剂师www.MedChem

4、EIC50 & Target JAK2 JAK1 Tyk2 JAK32.8 nM (IC50) 3.3 nM (IC50) 19 nM (IC50) 428 nM (IC50)体外研究 Ruxolitinib (INCB018424) potently and selectively inhibits JAK2V617F-mediated signaling and proliferation.Ruxolitinib inhibits the growth of HEL cells with EC50 of 186 nM. Ruxolitinib markedly increases apop

5、tosis inBa/F3-EpoR-JAK2V617F cell system, and inhibits hematopoietic progenitor cell proliferation in primary MPNpatient samples 1.体内研究 Ruxolitinib (180 mg/kg, p.o.) reduces the tumor burden of mice inoculated with JAK2V617F-expressing cellswithout causing anemia or lymphopenia 1.PROTOCOLCell Assay

6、1 Cells are seeded at 2000/well of white bottom 96-well plates, treated with compounds from DMSO stocks(0.2% final DMSO concentration), and incubated for 48 hours at 37C with 5% CO2. Viability is measured bycellular ATP determination using the Cell-Titer Glo luciferase reagent or viable cell countin

7、g. Values aretransformed to percent inhibition relative to vehicle control, and IC50 curves are fitted according to nonlinearregression analysis of the data using PRISM GraphPad.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice are fed standar

8、d rodent chow and provided with water ad libitum. Ba/F3-JAK2V617F cells (105 perAdministration 1 mouse) are inoculated intravenously into 6- to 8-week-old female BALB/c mice. Survival is monitored daily,and moribund mice are humanely killed and considered deceased at time of death. Treatment with ve

9、hicle(5% dimethyl acetamide, 0.5% methocellulose) or Ruxolitinib (INCB018424) begins within 24 hours of cellinoculation, twice daily by oral gavage. Hematologic parameters are measured using a Bayer Advia120analyzed, and statistical significance is determined using Dunnett testing.MCE has not indepe

10、ndently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Nat Med. 2018 Aug;24(8):1143-1150. Cancer Discov. 2018 May;8(5):616-631. Gut. 2019 May 10. pii: gutjnl-2018-317424. Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. Blood. 2014 Dec 18;124(26):3924-31.See more

11、 customer validations on HYPERLINK / www.MedChemEREFERENCES1. Quintas-Cardama A, et al. Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for thetreatment of myeloproliferative neoplasms. Blood, 2010, 115(15), 3109-3117.2. Fleischman AG, et al. The C

12、SF3R T618I mutation causes a lethal neutrophilic neoplasia in mice that is responsive to therapeutic JAK2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEinhibition. Blood. 2013 Nov 21;122(22):3628-31.3. de Bock CE, et al. HOXA9 Cooperates with Activated JAK/STAT Signaling to Drive Leukemia Development. Cancer Discov. 2018May;8(5):616-631.McePdfHeightCaution: