Fedratinib (TG101348)

For research use only. Not for use in humans.

目录号：S2736 别名： SAR302503 中文名称：费德拉替尼

Fedratinib (TG101348) Chemical Structure

CAS No. 936091-26-8

Fedratinib (SAR302503, TG101348)是一种选择性JAK2抑制剂，在无细胞试验中IC50为3 nM，作用于JAK2比作用于JAK1和JAK3选择性高35和334倍。Fedratinib也可抑制 FMS-like tyrosine kinase 3 (FLT3) 和 Ret (c-RET)，对应的IC50值分别为15 nM和48 nM。Fedratinib有潜在的抗肿瘤活性。Fedratinib可抑制细胞增殖并促进凋亡。Phase 2。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1812.56 现货
RMB 897.44 现货
RMB 1414.65 现货
RMB 3030.91 现货
RMB 4651.14 现货
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客户使用Selleck生产的Fedratinib (TG101348)发表文献58篇：

产品安全说明书

JAK抑制剂选择性比较

生物活性

产品描述 Fedratinib (SAR302503, TG101348)是一种选择性JAK2抑制剂，在无细胞试验中IC50为3 nM，作用于JAK2比作用于JAK1和JAK3选择性高35和334倍。Fedratinib也可抑制 FMS-like tyrosine kinase 3 (FLT3) 和 Ret (c-RET)，对应的IC50值分别为15 nM和48 nM。Fedratinib有潜在的抗肿瘤活性。Fedratinib可抑制细胞增殖并促进凋亡。Phase 2。
靶点
JAK2 [1]
(Cell-free assay)		 JAK2 (V617F) [1]
(Cell-free assay)		 FLT3 [1]
(Cell-free assay)		 RET [1]
(Cell-free assay)
3 nM 3 nM 15 nM 48 nM
体外研究

TG-101348也显著抑制JAK2 V617F, Flt3和Ret，IC50分别为3 nM, 15 nM和48 nM。TG101348对密切相关的JAK3的IC50高300倍以上，对JAK1和TYK2家族抑制效果不强。TG101348抑制有JAK2V617F突变的人红细胞白血病细胞系，以及一种表达人JAK2V617F（的Ba/F3 JAK2V617F）鼠前B细胞系的增殖，IC50分别是305 nM 和270 nM。G-101348也抑制亲本Ba/F3细胞的增殖至一般水平，IC50约为420 nM。TG101348降低STAT5磷酸化的浓度和抑制细胞增殖所需的浓度一致。TG101348以剂量依赖的方式诱导HEL和JAK2V617F Ba/F3细胞的凋亡。TG101348在浓度高达10 μM时对正常人真皮成纤维细胞没有促凋亡活性。[1] TG101348降低GATA-1的表达，这和erythroid-skewing JAK2V617F+祖细胞分化有关，并且抑制STAT5和GATA S310的磷酸化。[2] TG101348抑制HMC-1.1（KITV560G）细胞的增殖，活性低于HMC-1.2 (KITD816V, KITV560G)细胞，IC50分别为740 nM和407 nM。[3]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
H1975 NXrXc4h4SXCxcITvd4l{KEG|c3H5 NYrZVHZzOC53LUKg{txO MXqxNk01QCCq NFjWXFBFVVOR MlezbY5lfWOnczDhdI9xfG:|aYOgbY4h[m:2aDDkc5NmNSCjbnSgeIlu\S1iZHXw[Y5l\W62IH3hco5meg>? NXn5Z5RsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4OlkzOTBpPkK1PFY6OjFyPD;hQi=>
H1650 MoXORZBweHSxc3nzJGF{e2G7 NGK4PJQxNjVvMjFOwG0> MkDPNVIuPDhiaB?= M2C5SWROW09? NVO5T5F4cW6mdXPld{BieG:ydH;zbZMhcW5iYn;0bEBld3OnLTDhcoQhfGmvZT2g[IVx\W6mZX70JI1idm6nch?= MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh4OUKxNEc,OjV6NkmyNVA9N2F-
H1975 M{DzTWZ2dmO2aX;uJGF{e2G7 MWiwMlI2NTFizszN NETDOoEzPCCq MlfnSG1UVw>? MkfkbY5pcWKrdIOg[ZhxemW|c3nvckBw\iCjcH;weI9{cXNvcnXsZZRm\CCycn;0[YlvKEKlbD3YUEwhSmOuLUKsJJN2en[rdnnuMEBZUUGS NFfkbVA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUi2PVIyOCd-MkW4OlkzOTB:L3G+
H1650 Mmj5SpVv[3Srb36gRZN{[Xl? NXPme5RxOC5{NT2xJO69VQ>? MmLmNlQhcA>? NY[5PGR5TE2VTx?= NE\2b2JqdmirYnn0d{BmgHC{ZYPzbY9vKG:oIHHwc5B1d3Orcz3y[YxifGWmIIDyc5RmcW5iQnPsMXhNNCCEY3ytNkwhe3W{dnn2bY4tKFiLQWC= MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh4OUKxNEc,OjV6NkmyNVA9N2F-
H1975 NVm4bJNET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYGxJO69VQ>? NVTtb|h3PDhiaB?= NELxc4JFVVOR MXHz[Y5{cXSrenXzJINmdGy|IITvJJRp\SCleYTveI95cWOrdImgc4Yh\XKub4Tpcolj NGHH[IM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUi2PVIyOCd-MkW4OlkzOTB:L3G+
H1650 Mn\TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWWxJO69VQ>? MVe0PEBp MUPEUXNQ MnL3d4Vve2m2aYrld{Bk\WyuczD0c{B1cGViY4n0c5RwgGmlaYT5JI9nKGW{bH;0bY5q[g>? NVTQOXh5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4OlkzOTBpPkK1PFY6OjFyPD;hQi=>
CD4+ T M4DDXmZ2dmO2aX;uJGF{e2G7 NYPNNZVJOC5yMT2xJO69VQ>? NWfNNVZyPDhiaB?= MVnEUXNQ NFT1fJpz\WS3Y3XzJJRp\SCyaH;zdIhwenmuYYTpc44hdGW4ZXzzJI9nKEqDS{KgZY5lKFOWQWSzxsA> NFTsemE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUW3NlU{PSd-MkW1O|I2OzV:L3G+
Caco-2  M1rOVmZ2dmO2aX;uJGF{e2G7 MWWwMVEzOCEQvF2= M3XrNFchdWmw M1TEXolvcGmkaYTzJJRpcWGvaX7lJJVxfGGtZTD3bZRpKGGwIFnDOVDDqG:oIEKuNeKhyrWP NELHfYU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC2N|Y4Oid-MkWwOlM3PzJ:L3G+
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MedB-1 NYnjcJdyTnWwY4Tpc44hSXO|YYm= MmL3NU8zKM7:TR?= NHftNJczPCCq NUG4W2Zt\GWlcnXhd4V{KFOWQWS2JJBpd3OyaH;yfYxifGmxbjDjc45k\W62cnH0bY9vKGSncHXu[IVvfGy7 NX7LeoEzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5O|c3PjhpPkK0PVc4PjZ6PD;hQi=>
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K1106 M1L4dGZ2dmO2aX;uJGF{e2G7 NEH3e|UyNzJizszN M4T0dFI1KGh? NIDQS4Zl\WO{ZXHz[ZMhW1SDVE[gdIhwe3Cqb4L5cIF1cW:wIHPvcoNmdnS{YYTpc44h\GWyZX7k[Y51dHl? NX3QO|ZORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5O|c3PjhpPkK0PVc4PjZ6PD;hQi=>
K562 NXHq[49kT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHGNZEyOC1zIN88US=> MlKwO|IhcA>? NY[yNWxxcW6qaXLpeJMhUzV4MjDj[YxtKHC{b3zp[oVz[XSrb36gZZQhcGmpaDDjc45k\W62cnH0bY9v MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd5NUOwPEc,OjR5N{WzNFg9N2F-
MDA-MB-468  MlPhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTIN{DDvU1? MkXsOFghcA>? MYjlcohidmOnZDDzbYJkdDZiaX7keYNm\CCub4PzJI9nKGOnbHygeoli[mmuaYT5xsA> MluzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NkK4NVgoRjJ2Nk[yPFE5RC:jPh?=
MDA-MB-468 Mn;zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXSwMVQh|ryP NEjldYI1QCCq M1LldJJme3WudIOgd4lodmmoaXPhcpQhdG:|czDv[kB3cWGkaXzpeJkh[2:vcHHy[YQhfG9iUlmtRnBKKGGub37l M1XGPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2Nk[yPFE5Lz5{NE[2NlgyQDxxYU6=
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KMH2 NGWzcpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYr1PI16OC13IN88US=> MVy0PEBp NYWyUZFIcW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> NHmy[Y89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[xNFgzPyd-MkS2NVA5Ojd:L3G+
L1236 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXewMVUh|ryP NHXOO3Q1QCCq NFnzVpBqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 M2PCfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkGwPFI4Lz5{NE[xNFgzPzxxYU6=
SUPHD1 NHTDUGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4ntXlAuPSEQvF2= MXq0PEBp NHz1ZmlqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 NEDCVno9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[xNFgzPyd-MkS2NVA5Ojd:L3G+
HDLM2 NX6zbXFzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWPBSo1WOC13IN88US=> NUTJTplWPDhiaB?= M2OxdolvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= NF;kOpk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[xNFgzPyd-MkS2NVA5Ojd:L3G+
K1106P M3HtV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHLZWExNTVizszN NUO5bXdzPDhiaB?= Mlm1bY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= MoLkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4MUC4NlcoRjJ2NkGwPFI4RC:jPh?=
L428 NUPUNHd[SXCxcITvd4l{KEG|c3H5 MlTnNE8xNjZ{NT:xMlI2KM7:TR?= MUS0PEBp NUTMe3JpcW6mdXPld{B1cGViYYDvdJRwe2m|wrC= NEHVVpA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[xNFgzPyd-MkS2NVA5Ojd:L3G+
KMH2 M364W2Fxd3C2b4Ppd{BCe3OjeR?= NHPl[lgxNzBwNkK1M|EvOjVizszN M1jFZ|Q5KGh? NGHaTXNqdmS3Y3XzJJRp\SCjcH;weI9{cXQEoB?= MlzHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4MUC4NlcoRjJ2NkGwPFI4RC:jPh?=
L1236 M3vD[WFxd3C2b4Ppd{BCe3OjeR?= NYLMdG9UOC9yLk[yOU8yNjJ3IN88US=> M3vQWFQ5KGh? M4LUfIlv\HWlZYOgeIhmKGGyb4D0c5Nqe8Li Mn7sQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4MUC4NlcoRjJ2NkGwPFI4RC:jPh?=
SUPHD1 MkPNRZBweHSxc3nzJGF{e2G7 NUDvTGEyOC9yLk[yOU8yNjJ3IN88US=> NUD0O3RPPDhiaB?= NWG4WlE6cW6mdXPld{B1cGViYYDvdJRwe2m|wrC= M2nXc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkGwPFI4Lz5{NE[xNFgzPzxxYU6=
HDLM2 Mlu5RZBweHSxc3nzJGF{e2G7 NVXxdY5TOC9yLk[yOU8yNjJ3IN88US=> MoezOFghcA>? MoL5bY5lfWOnczD0bIUh[XCxcITvd4l{yqB? M13iSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkGwPFI4Lz5{NE[xNFgzPzxxYU6=
K1106P NWPSXpZJSXCxcITvd4l{KEG|c3H5 NGDQXnExNzBwNkK1M|EvOjVizszN MnG0OFghcA>? NH;0UYdqdmS3Y3XzJJRp\SCjcH;weI9{cXQEoB?= MnnpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4MUC4NlcoRjJ2NkGwPFI4RC:jPh?=
L428 NXqzRnlbTnWwY4Tpc44hSXO|YYm= MVywMVUh|ryP NW[1RlA3OjRiaB?= MVLpcohq[mm2czDKRWszN1OWQWSgd4lodmGuaX7n NG\Ce2E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[xNFgzPyd-MkS2NVA5Ojd:L3G+
KMH2 NFLCRnVHfW6ldHnvckBCe3OjeR?= NIT3NHYxNTVizszN MYeyOEBp MWXpcohq[mm2czDKRWszN1OWQWSgd4lodmGuaX7n MofJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4MUC4NlcoRjJ2NkGwPFI4RC:jPh?=
L1236 NHfSVXlHfW6ldHnvckBCe3OjeR?= NWOyfYRSOC13IN88US=> MXOyOEBp NW\HXFVocW6qaXLpeJMhUkGNMj;TWGFVKHOrZ37hcIlv\w>? NFnoPZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[xNFgzPyd-MkS2NVA5Ojd:L3G+
SUPHD1 NYjrN2NPTnWwY4Tpc44hSXO|YYm= NFLIZY0xNTVizszN MmLyNlQhcA>? MlXTbY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> NHS0fVc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[xNFgzPyd-MkS2NVA5Ojd:L3G+
HDLM2 MVLGeY5kfGmxbjDBd5NigQ>? NXTUZ4pTOC13IN88US=> NXjk[JVjOjRiaB?= MnjnbY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> MmnVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4MUC4NlcoRjJ2NkGwPFI4RC:jPh?=
K1106P NFfEeIVHfW6ldHnvckBCe3OjeR?= MmPzNE02KM7:TR?= M2TZd|I1KGh? NGjJZ3BqdmirYnn0d{BLSUt{L2PURXQhe2mpbnHsbY5o MmPQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4MUC4NlcoRjJ2NkGwPFI4RC:jPh?=
MM.1S  NYToPJVMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDsTWM2OD1zLUOg{txO MnrjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3OESxNFEoRjJ2NUi0NVAyRC:jPh?=
TpoR JAK2 WT NFLQeWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1P2UmlEPTB;MT60JEgyNjQkgKOxMlUqKM7:TR?= NX;1d4FrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyOVE4QTBpPkK0NlUyPzlyPD;hQi=>
TpoR JAK2 V617F NWLOenh{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzSZ4xKSzVyPUCuPEApOC554pETNE46MSEQvF2= NUPy[VcxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyOVE4QTBpPkK0NlUyPzlyPD;hQi=>
TpoR W515L NFiyTZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDyXWRKSzVyPUCuPEApOC554pETNU4xMSEQvF2= MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJ3MUe5NEc,OjR{NUG3PVA9N2F-
Bcr-abl NXPrRpZVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTJwNzCoNk4z6oDVMz6zLUDPxE1? NIjZUng9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEK1NVc6OCd-MkSyOVE4QTB:L3G+
JAK2 TW NGjwS5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXWPG9KSzVyPUGuPEApOS534pETNk4{MSEQvF2= NF3GWVc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEK1NVc6OCd-MkSyOVE4QTB:L3G+
JAK2 V617F MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTBwNjCoNE436oDVMD63LUDPxE1? MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJ3MUe5NEc,OjR{NUG3PVA9N2F-
MedB-1 MnPMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGLoVGU1KM7:TR?= M1rPTlI1NzR6L{eyJIg> NHzzUYxFVVOR NX3DU2U3cW6qaXLpeJMh[2WubDDndo94fGhidHnt[UBl\XCnbnTlcpRtgQ>? M3HXVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OEWyN|Y3Lz5{M{i1NlM3PjxxYU6=
K1106 MoXFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3XOEDPxE1? M3z6XVI1NzR6L{eyJIg> MofzSG1UVw>? NHrUZZBqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 M3\xd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OEWyN|Y3Lz5{M{i1NlM3PjxxYU6=
U2940 NX7i[IpjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWK0JO69VQ>? MmnENlQwPDhxN{KgbC=> M2LBTGROW09? MVjpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 MlHKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6NUKzOlYoRjJ|OEWyN|Y3RC:jPh?=
FE-PD M1PzUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYWwMlA3Oy12IN88US=> NV6zeGR4UUN3ME25MlUh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 M{T0S|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{eyOlY6Lz5{M{O3NlY3QTxxYU6=
HEL MmjmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HtOFAvODZ|LUSg{txO NF3IeoZKSzVyPUGuOUDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= NH:zOoE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O3NlY3QSd-MkOzO|I3Pjl:L3G+
K-562 MkOyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3ONE4xPjNvNDFOwG0> MorNTWM2OD1{LkWg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 MkW0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|N{K2OlkoRjJ|M{eyOlY6RC:jPh?=
L-82 NVfo[Gx{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVewMlA3Oy12IN88US=> MmDuTWM2OD1yLkm4JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= NGDrc3I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O3NlY3QSd-MkOzO|I3Pjl:L3G+
MAC-1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\0NE4xPjNvNDFOwG0> M4\GV2lEPTB;MD61NkDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= M1[zRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{eyOlY6Lz5{M{O3NlY3QTxxYU6=
MAC-2A M4HYUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYmwMlA3Oy12IN88US=> MoK4TWM2OD1yLk[5JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= M2DI[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{eyOlY6Lz5{M{O3NlY3QTxxYU6=
MAC-2B NWnCbVJIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXKwMlA3Oy12IN88US=> Ml7BTWM2OD1yLkW0JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= M1nnWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{eyOlY6Lz5{M{O3NlY3QTxxYU6=
MY-LA NFfkbWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfNOI9rOC5yNkOtOEDPxE1? MnLkTWM2OD1{LkGg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 M{XaSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{eyOlY6Lz5{M{O3NlY3QTxxYU6=
NC-NC NX2xd4NLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVWwMlA3Oy12IN88US=> M2O5UGlEPTB;MT6wJO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= NW\TRVZzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzO|I3PjlpPkKzN|czPjZ7PD;hQi=>
SE-AX MnvnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnriNE4xPjNvNDFOwG0> NHW1UJFKSzVyPUGuOUDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= M2rTVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{eyOlY6Lz5{M{O3NlY3QTxxYU6=
SR-786 NEfPcJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvseVRXOC5yNkOtOEDPxE1? MYPJR|UxRTRwNjFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? M4HVZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{eyOlY6Lz5{M{O3NlY3QTxxYU6=
M-MOK  M{LC[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4K5[|I2KML3TdMg NX;SbHJZOjRxNEivO|IhcA>? NYG4V2JITE2VTx?= MXrpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 MmfBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF6NUOxOVcoRjJzOEWzNVU4RC:jPh?=
HEL Ml3QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTNyNTDuUS=> MkjOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh|OUS1OVQoRjF6M{m0OVU1RC:jPh?=
Ba/F3 JAK2V617F MkjDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\aUmlEPTB;MkewJI5O M{XHZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6M{m0OVU1Lz5zOEO5OFU2PDxxYU6=
MV4-11 NUG0fpRRSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NWroW5Y3PzJiaILz NVm0bopISW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNWlQuOTFiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JINmdGy2aYTldk1jdHWnIHHzd4F6NCCHQ{WwJF0hOC5yN{mg{txONg>? MkTuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OECyOlEoRjJ6MkiwNlYyRC:jPh?=
MM1S MX\BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MlvkO|IhcHK| MV3BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2PMWOgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KHS{eYDhckBjdHWnIHX4Z4x2e2mxbjDhd5NigSxiSVO1NEA:KDFizszNMi=> M2jVVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MkiwNlYyLz5{OEK4NFI3OTxxYU6=
NB1643 MWPxTHRUKGG|c3H5 MX7xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJzNkSzJINmdGy| MkjIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC NEXOdFRyUFSVIHHzd4F6 M1LFcpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMW1EKGOnbHzz M{\QR|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
p-JAK2 / p-STAT1 / p-STAT3 / p-STAT6 / p-STAT5 / JAK2 ; 

PubMed: 24610827     


Western analysis of pJAK2 and the downstream pSTATs following treatment with vehicle or the indicated concentrations of fedratinib for 24 hours. Total JAK2 and GAPDH are similarly analyzed.

c-Myc / PIM1 ; 

PubMed: 24610827     


Western analysis of c-MYC and PIM1 protein levels in cHL and MLBCL cell lines treated with vehicle or fedratinib at the indicated concentration for 24 hours. Data are representative of three independent experiments.

24610827
Growth inhibition assay
Cell proliferation ; 

PubMed: 24610827     


Cellular proliferation of cHL cell lines (L428, KMH2, L1236, SUPHD1 and HDLM2) and the MLBCL cell line (K1106P), following treatment with vehicle or fedratinib at indicated concentration for 48 hours. For each cell line, the previously reported 9p24.1/JAK2 copy numbers (7) are indicated in parenthesis. At a given dose of the JAK2 inhibitor (1.25 μM), a Kruskal-Wallis test was performed to assess the association between the ranked values of inhibition and copy number gain (p = .009, cHL and MLBCL cell lines; p = .019, cHL cell lines).

24610827
体内研究

TG101348有治疗JAK2V617F相关的骨髓增生性疾病(MPD)的潜力。在TG101348处理的动物中血细胞比容和白细胞计数有统计学显著减少，以剂量依赖性减少/消除髓外造血，至少在某些情况下，表现为衰减性骨髓纤维化，具有替代终点，包括减少/消除的JAK2V617F疾病负担，抑制内源性红细胞集落的形成相关，在体内抑制JAK-STAT信号转导。有没有明显的毒性并对T细胞数量无影响。[1] TG101348（120 mg/kg）口服显著抑制体内光伏红系祖细胞分化。[2]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验：

[1]
- 合并

无细胞激酶活性测定:

TG101348 的IC 50值使用Invitrogen公司的223激酶试剂盒测定，其中包括JAK2和JAK2V617F，或者Carna Biosciences的所有Janus激酶家族成员试剂盒，包括JAK1和TYK2。ATP浓度设定为激酶的Km值。
细胞实验：

[1]
- 合并
  • Cell lines: EpoBa/F3 JAK2V617F, Ba/F3p210, HEL和K562细胞
  • Concentrations: 溶解在DMSO中至终浓度约10 μM
  • Incubation Time: 72小时
  • Method:

    约2×103细胞接种到微量滴定板的孔中，加入含指定浓度抑制剂的100μLRPMI-1640培养基。TG101348温育72小时，50 μL XTT染料加入到每个孔中并孵育4小时，在CO2培养箱中培养。有色甲臜产物用分光光度法在450nm处测定在650nm处校正。50％的抑制作用（IC50）的浓度用GraphPad Prism 4.0软件确定。所有的实验都重复3次，并且结果和未处理的细胞的生长做比较。EpoBa/F3 JAK2V617F，Ba/F3p210，HEL和K562细胞凋亡是用DMSO和TG101348浓度的增加诱导来确定。


    (Only for Reference)
动物实验：

[1]
- 合并
  • Animal Models: C57BL / 6小鼠静脉注射表达JAK2V617F的全骨髓
  • Dosages: 约120 mg/kg
  • Administration: 口服，每天两次
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 100 mg/mL (190.59 mM)
Water Insoluble
Ethanol Insoluble

* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 524.68
化学式

C27H36N6O3S
CAS号 936091-26-8
储存条件 粉状
溶于溶剂
别名 SAR302503

动物体内配方计算器 (澄清溶液)

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量 只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时，请务必参考Selleck产品标签上、SDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液，使用的计算公式为：

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时，请务必参考Selleck产品标签上、SDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量：

总分子量：g/mol

注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04955938 Not yet recruiting Drug: Ivosidenib|Drug: Enasidenib|Drug: Fedratinib IDH Mutation|IDH1 Mutation|IDH2 Gene Mutation|Blood Cancer|Myeloproliferative Neoplasm University of Chicago October 1 2021 Phase 1
NCT04702464 Not yet recruiting Drug: Fedratinib|Drug: Fluconazole Healthy Volunteers Celgene|Impact Biomedicines Inc. a wholly owned subsidiary of Celgene Corporation January 8 2021 Phase 1
NCT03983161 Recruiting Drug: Fedratinib Healthy Volunteers|Hepatic Impairment Celgene|Impact Biomedicines Inc. a wholly owned subsidiary of Celgene Corporation July 15 2019 Phase 1
NCT03983239 Completed Drug: Fedratinib|Drug: Rifampin|Drug: Efavirenz Healthy Volunteers Celgene|Impact Biomedicines Inc. a wholly owned subsidiary of Celgene Corporation June 21 2019 Phase 1
NCT02596347 Completed Procedure: Blood draw|Procedure: bronchoscopy Chronic Beryllium Disease (CBD)|Beryllium Sensitization (BeS) National Jewish Health April 2015 --
NCT01692366 Completed Drug: SAR302503 Myelofibrosis Sanofi November 2012 Phase 2

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

  • * 必填项
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JAK Signaling Pathway Map

JAK Inhibitors with Unique Features

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    FLLL32 是一种有效的 JAK2/STAT3 抑制剂，IC50 <5 μM。FLLL32 在乳腺癌细胞中通过 IFNα 和 IL-6 来抑制STAT3磷酸化的诱导。

  • Cerdulatinib (PRT062070) hydrochloride New

    Cerdulatinib (PRT-062070, PRT2070) hydrochloride 是一种具有口服活性的多靶点酪氨酸激酶抑制剂，对JAK1/JAK2/JAK3/TYK2和Syk的IC50分别为12 nM/6 nM/8 nM/0.5 nM和32 nM。也能够抑制测试的其他19种激酶，IC50均低于200 nM。

  • Ruxolitinib (INCB018424)

    Ruxolitinib (INCB018424)是第一个应用于临床的，有效的，选择性JAK1/2抑制剂，在无细胞试验中IC50为3.3 nM/2.8 nM。作用于JAK1， JAK2与作用于JAK3相比，选择性高130多倍。Ruxolitinib 通过毒性线粒体自噬杀死肿瘤细胞。Ruxolitinib 可诱导自噬并增强细胞凋亡。

  • Tofacitinib (CP-690550) Citrate

    Tofacitinib citrate (CP-690550, Tasocitinib)是一种新型JAK抑制剂，对JAK3，JAK2，JAK1的IC50分别为1 nM, 20 nM 和112 nM。Tofacitinib citrate 还具有抗感染的活性。

  • Tofacitinib (CP-690550)

    Tofacitinib (CP-690550,Tasocitinib)是一种新型JAK3抑制剂，在无细胞试验中IC50为1 nM，作用于JAK2和JAK1选择性低20到100倍。Tofacitinib 可在人类浆细胞样树突状细胞PDC中抑制抗凋亡的BCL-A1和BCL-XL并诱导PDC凋亡。

  • AZD1480

    AZD1480是一种新型，ATP竞争性的JAK2抑制剂，无细胞试验中IC50为0.26 nM，选择性作用于JAK3和Tyk2，对JAK1的作用较弱。Phase 1。

    Features:AZD1480为治疗多发性骨髓瘤的潜在新型治疗剂。

  • Momelotinib (CYT387)

    Momelotinib (CYT387, LM-1149 , CYT11387) 是一种ATP竞争性JAK1/JAK2抑制剂，IC50为11 nM/18 nM，比作用于JAK3选择性约高10倍左右。Momelotinib (CYT387) 可诱导凋亡和自噬。Phase 3。

    Features:CYT387是ATP竞争性小分子JAK1 和JAK2抑制剂。

  • WP1066

    WP1066 是一种新型JAK2和STAT3抑制剂，在HEL细胞中IC50分别为2.30 μM和2.43 μM；对JAK2，STAT3，STAT5和ERK1/2具有抑制活性，而对JAK1和JAK3没有作用。WP1066 可诱导凋亡。Phase 1。

    Features:WP1066像它的母体化合物一样能抑制JAK2的磷酸化作用，但与AG490不同WP1066还能减少JAK2的蛋白量。

  • Baricitinib (INCB028050)

    Baricitinib (LY3009104, INCB028050)是一种选择性JAK1和JAK2抑制剂，无细胞试验中IC50分别为5.9 nM和5.7 nM，比作用于JAK3和Tyk2选择性高70和10倍左右，对c-Met和Chk2没有抑制作用。Baricitinib被发现可以减少或干扰病毒进入目标细胞，并用于COVID-19的治疗研究中。Phase 3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID