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JAK2和JAK2V617F激酶的IC50值均为3 nM。菲达替尼相对于JAK1和JAK3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。
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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。 |
靶点 |
|
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 |
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. |
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 << |
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 |
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 |