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Fedratinib {[allProObj[0].p_purity_real_show]}

货号:A345883 同义名: SAR 302503;TG 101348

Fedratinib(TG-101348)是一种强效、选择性、ATP竞争性和口服活性的JAK2抑制剂,对JAK2JAK2V617F激酶的IC50值均为3 nM。菲达替尼相对于JAK1JAK3显示出35倍和334倍的选择性。它诱导癌细胞凋亡,并具有潜在的骨髓增殖性疾病研究价值。

Fedratinib 化学结构 CAS号:936091-26-8
Fedratinib 化学结构
CAS号:936091-26-8
Fedratinib 3D分子结构
CAS号:936091-26-8
Fedratinib 化学结构 CAS号:936091-26-8
Fedratinib 3D分子结构 CAS号:936091-26-8
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Fedratinib 纯度/质量文件 产品仅供科研

货号:A345883 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 c-RET 其他靶点 纯度
Regorafenib +++

RET, IC50: 1.5 nM

98%
TG101209 ++

RET, IC50: 17 nM

FLT3 99%+
Danusertib +

RET, IC50: 31 nM

99%+
AD80 ++++

RET V804M, IC50: 0.6 nM

RET wt, IC50: 1.3 nM

Src,Raf 99+%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。
产品名称 JAK1 JAK2 JAK3 Tyk2 其他靶点 纯度
Decernotinib +++

JAK1, Ki: 11 nM

JAK1, IC50: 11 nM

+++

JAK2, Ki: 13 nM

++++

JAK3, Ki: 2.5 nM

+++

TYK2, Ki: 13 nM

99%+
ZM39923 HCl +

JAK1, pIC50: 4.4

+

JAK3, pIC50: 7.1

EGFR 97%
Cerdulatinib +++

JAK1, IC50: 12 nM

+++

JAK2, IC50: 6 nM

+++

JAK3, IC50: 8 nM

++++

TYK2, IC50: 0.5 nM

99%+
Momelotinib +++

JAK1, IC50: 11 nM

++

JAK2, IC50: 18 nM

+

JAK3, IC50: 155 nM

99%+
XL019 +

JAK1, IC50: 134.3 nM

++++

JAK2, IC50: 2.2 nM

+

JAK3, IC50: 214.2 nM

FLT3 99%+
Ruxolitinib +++

JAK1, IC50: 3.3 nM

++++

JAK2, IC50: 2.8 nM

98%
Tofacitinib +

JAK1, IC50: 112 nM

++

JAK2, IC50: 20 nM

++++

JAK3, IC50: 1 nM

98%
Ruxolitinib (S enantiomer) +++

JAK1, IC50: 3.3 nM

++++

JAK2, IC50: 2.8 nM

++

TYK2, IC50: 19 nM

98%
Filgotinib +++

JAK1, IC50: 10 nM

++

JAK2, IC50: 28 nM

+

JAK3, IC50: 810 nM

+

TYK2, IC50: 116 nM

99%
Baricitinib +++

JAK1, IC50: 5.9 nM

+++

JAK2, IC50: 5.7 nM

++

TYK2, IC50: 53 nM

99%
Gandotinib ++

JAK1, IC50: 19.8 nM

++++

JAK2, IC50: 0.288 nM

JAK2 (V617F), Ki: 0.245 nM

++

JAK3, IC50: 48.0 nM

++

TYK2, IC50: 44 nM

FLT3 99%+
Oclacitinib maleate +++

JAK1, IC50: 10nM

++

JAK2, IC50: 18nM

+

JAK3, IC50: 99nM

+

TYK2, IC50: 84nM

98+%
NVP-BSK805 2HCl ++

JAK1, IC50: 31.63 nM

++++

JAK2, IC50: ~0.5 nM

++

JAK3, IC50: 18.68 nM

+++

TYK2, IC50: 10.76 nM

99+%
Peficitinib 98%
Go6976 FLT3 99%+
AZD-1480 ++++

JAK2, IC50: 0.26 nM

99%+
Fedratinib +++

JAK2 (V617F), IC50: 3 nM

JAK2, IC50: 3 nM

FLT3,RET 99%+
WP1066 +

JAK2, IC50: 2.3 μM

98%
Curcumol 98%
AZ960 ++++

JAK2, Ki: 0.45 nM

JAK2, IC50: <3 nM

97%
GLPG0634 analog 99%+
CEP-33779 ++++

JAK2, IC50: 1.8 nM

99%+
FLLL32 +

JAK2, IC50: <5 μM

99%+
WHI-P154 +

JAK3, IC50: 1.8 μM

EGFR,Src,VEGFR 98%
BMS-911543 ++++

JAK2, IC50: 1.1 nM

+

JAK3, IC50: 75 nM

++

TYK2, IC50: 66 nM

98%
TG101209 +++

JAK2, IC50: 6 nM

+

JAK3, IC50: 169 nM

FLT3,RET 99%+
AT9283 ++++

JAK2, IC50: 1.2 nM

++++

JAK3, IC50: 1.1 nM

99%+
Pacritinib ++

JAK2 (V617F), IC50: 19 nM

JAK2, IC50: 23 nM

+

JAK3, IC50: 520 nM

++

TYK2, IC50: 50 nM

FLT3 97%
Tofacitinib citrate ++

JAK2, IC50: 20 nM

++++

JAK3, IC50: 1 nM

99%
FM-381 ++++

JAK3, IC50: 127 pM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。
产品名称 FLT3 其他靶点 纯度
R406 Syk 98%
Go6976 99%+
Quizartinib +++

FLT3 (ITD), IC50: 1.1 nM

FLT3 (WT), IC50: 4.2 nM

98%
Gilteritinib ++++

FLT3, IC50: 0.29 nM

99%+
Amuvatinib +

FLT3 (D835Y), IC50: 81 nM

99%+
Pacritinib ++

FLT3 (D835Y), IC50: 6 nM

FLT3, IC50: 22 nM

97%
Dovitinib ++++

FLT3, IC50: 1 nM

c-Kit 99%+
Denfivontinib ++++

FLT3 (D835Y), IC50: 0.4 nM

FLT3, IC50: 0.4 nM

RET 99%+
TAK-659 HCl ++

FLT3, IC50: 4.6 nM

Syk 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Fedratinib 生物活性

靶点
  • JAK2

    JAK2 (V617F), IC50:3 nM

    JAK2, 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].

Fedratinib 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
Caco-2 10/50/100 μM Function Assay 2 h decreases the flux of [3H]thiamine across the monolayer with IC50 of 6.5 μM 25063672

Fedratinib 动物研究

Dose Mice: 1 g/kg[2] (p.o.), 30 mg/kg - 200 mg/kg[1] (p.o.) Rat: 2 mg/kg[3] (i.v.)
Administration p.o., i.v.

Fedratinib 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 <<

Fedratinib 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.

Fedratinib 实验方案

计算器
存储液制备 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

Fedratinib 技术信息

CAS号936091-26-8
分子式C27H36N6O3S
分子量 524.678
别名 SAR 302503;TG 101348
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

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

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
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