产品说明书

Fedratinib

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Chemical Structure| 936091-26-8 同义名 : SAR 302503;TG 101348
CAS号 : 936091-26-8
货号 : A345883
分子式 : C27H36N6O3S
纯度 : 99%+
分子量 : 524.678
MDL号 : MFCD12922515
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(228.71 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • JAK2

    JAK2, IC50:3 nM

    JAK2 (V617F), IC50:3 nM
描述 Fedratinib is a selective JAK2 inhibitor with IC50 values of 3nM, 3nM, 15nM and 48nM for JAK2, JAK2 V617F, Flt3 and Ret, respectively. Fedratinib inhibited proliferation of a human erythroblast leukemia (HEL) cell line that harbors the JAK2V617F mutation, as well as a murine pro-B cell line expressing human JAK2V617F (Ba/F3 JAK2V617F), with an IC50 value of approximately 300nM for either line. Exposure of these cells to Fedratinib reduced STAT5 phosphorylation at concentrations that parallel the concentrations required to inhibit cell proliferation. Also it induced apoptosis in both HEL and Ba/F3 JAK2V617F cells in a dose-dependent manner. It showed therapeutic efficacy in a murine model of myeloproliferative disease induced by the JAK2V617F mutation. It triggered a statistically significant reduction in hematocrit and leukocyte count, a dose-dependent reduction/elimination of extramedullary hematopoiesis, and, at least in some instances, evidence for attenuation of myelofibrosis[2].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
Ba/F3 JAK2V617F Growth Inhibition Assay IC50=270 nM 18394554
Bcr-abl Growth Inhibition Assay IC50=2.7 (2.2–3.3) μM 24251790
Caco-2 0-120 μM Function Assay 7 min inhibits thiamine uptake with an IC50 of 2.1 µM 25063672
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01437787 Hematopoietic Neoplasm Phase 3 Completed - -
NCT01585623 Solid Tumor Phase 1 Completed - United States, Georgia ... 展开 >> Investigational Site Number 840004 Augusta, Georgia, United States, 30912 United States, Michigan Investigational Site Number 840001 Detroit, Michigan, United States, 48201 United States, Pennsylvania Investigational Site Number 840002 Philadelphia, Pennsylvania, United States, 19111 收起 <<
NCT01836705 Neoplasm Malignant Phase 1 Completed - United States, California ... 展开 >> Investigational Site Number 840003 Los Angeles, California, United States, 90048 United States, Georgia Investigational Site Number 840007 Augusta, Georgia, United States, 30912 United States, Michigan Investigational Site Number 840002 Detroit, Michigan, United States, 48201 United States, Missouri Investigational Site Number 840001 St Louis, Missouri, United States, 63110 United States, Ohio Investigational Site Number 840004 Cincinnati, Ohio, United States, 45267-0542 United States, Pennsylvania Investigational Site Number 840005 Philadelphia, Pennsylvania, United States, 19111 United States, Texas Investigational Site Number 840006 San Antonio, Texas, United States, 78229 Investigational Site Number 840008 San Antonio, Texas, United States, 78229 Belgium Investigational Site Number 056001 Bruxelles, Belgium, 1200 Investigational Site Number 056002 Gent, Belgium, 9000 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.91mL

0.38mL

0.19mL

9.53mL

1.91mL

0.95mL

19.06mL

3.81mL

1.91mL
参考文献

[1]Wernig G, Kharas MG, et al. Efficacy of TG101348, a selective JAK2 inhibitor, in treatment of a murine model of JAK2V617F-induced polycythemia vera. Cancer Cell. 2008 Apr;13(4):311-20.

[2]Wernig G, Kharas MG, Okabe R, Moore SA, Leeman DS, Cullen DE, Gozo M, McDowell EP, Levine RL, Doukas J, Mak CC, Noronha G, Martin M, Ko YD, Lee BH, Soll RM, Tefferi A, Hood JD, Gilliland DG. Efficacy of TG101348, a selective JAK2 inhibitor, in treatment of a murine model of JAK2V617F-induced polycythemia vera. Cancer Cell. 2008 Apr;13(4):311-20. doi: 10.1016/j.ccr.2008.02.009. PMID: 18394554.