Fedratinib (TG101348)

目录号:S2736 别名: SAR302503 中文名称:费德拉替尼

仅限科研使用

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)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。

Fedratinib (TG101348) Chemical Structure

CAS: 936091-26-8

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 4651.14 现货
大包装 有超大折扣

今日订购,明日送达 全国免运费 分装免费 分装成小规格产品(单支最小为1mg)
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全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck生产的Fedratinib (TG101348)发表文献68篇:

产品安全说明书

JAK抑制剂选择性比较

相关JAK产品

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)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 MV3BdI9xfG:|aYOgRZN{[Xl? MlLiNE42NTJizszN M4q1ZlEzNTR6IHi= M2XjNmROW09? NHf5N2NqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCkb4ToJIRwe2VvIHHu[EB1cW2nLTDk[ZBmdmSnboSgcYFvdmW{ NEThOZM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUi2PVIyOCd-MkW4OlkzOTB:L3G+
H1650 Ml\qRZBweHSxc3nzJGF{e2G7 M3m5OVAvPS1{IN88US=> MVWxNk01QCCq MlzySG1UVw>? NVzHd5JvcW6mdXPld{BieG:ydH;zbZMhcW5iYn;0bEBld3OnLTDhcoQhfGmvZT2g[IVx\W6mZX70JI1idm6nch?= NIroO3c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUi2PVIyOCd-MkW4OlkzOTB:L3G+
H1975 NGXjW3VHfW6ldHnvckBCe3OjeR?= NXvqfmZHOC5{NT2xJO69VQ>? NXj4OVloOjRiaB?= MmfHSG1UVw>? NFn4NG5qdmirYnn0d{BmgHC{ZYPzbY9vKG:oIHHwc5B1d3Orcz3y[YxifGWmIIDyc5RmcW5iQnPsMXhNNCCEY3ytNkwhe3W{dnn2bY4tKFiLQWC= MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh4OUKxNEc,OjV6NkmyNVA9N2F-
H1650 MmXESpVv[3Srb36gRZN{[Xl? M{T1S|AvOjVvMTFOwG0> MnfvNlQhcA>? MV7EUXNQ MYrpcohq[mm2czDlfJBz\XO|aX;uJI9nKGGyb4D0c5Nqey2{ZXzheIVlKHC{b4TlbY4hSmOuLWjMMEBD[2xvMjygd5Vzfmm4aX6sJHhKSVB? MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh4OUKxNEc,OjV6NkmyNVA9N2F-
H1975 NIjGdmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrxNUDPxE1? NYriUms4PDhiaB?= M3;TOWROW09? MkDjd4Vve2m2aYrld{Bk\WyuczD0c{B1cGViY4n0c5RwgGmlaYT5JI9nKGW{bH;0bY5q[g>? NHrObHo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUi2PVIyOCd-MkW4OlkzOTB:L3G+
H1650 M{jreWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX:xJO69VQ>? M17tWFQ5KGh? MkLMSG1UVw>? MV7z[Y5{cXSrenXzJINmdGy|IITvJJRp\SCleYTveI95cWOrdImgc4Yh\XKub4Tpcolj MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh4OUKxNEc,OjV6NkmyNVA9N2F-
CD4+ T M4Ho[2Z2dmO2aX;uJGF{e2G7 M3TFR|AvODFvMTFOwG0> M3TL[FQ5KGh? NGq2ZldFVVOR MYLy[YR2[2W|IITo[UBxcG:|cHjvdplt[XSrb36gcIV3\Wy|IH;mJGpCUzJiYX7kJHNVSVR|wrC= Ml\iQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV3N{K1N|UoRjJ3NUeyOVM2RC:jPh?=
Caco-2  NFjsT4FHfW6ldHnvckBCe3OjeR?= MofWNE0yOjBizszN NXLsWGtMPyCvaX6= MWrpcohq[mm2czD0bIlidWmwZTD1dJRic2Vid3n0bEBidiCLQ{WwxsBw\iB{LkJCpOK2VQ>? NH7xeJM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC2N|Y4Oid-MkWwOlM3PzJ:L3G+
Caco-2  NYjuZoZCTnWwY4Tpc44hSXO|YYm= NFG5SJMyOC93MD:xNFAh|ryP MmHMNkBp NYnWNWxy\GWlcnXhd4V{KHSqZTDmcJV5KG:oIGuzTH11cGmjbXnu[UBi[3Kxc4OgeIhmKG2xbn;sZZlmeiC5aYToJGlEPTBib3[gOk42yqEQvF2= Mnu1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyNkO2O|IoRjJ3ME[zOlczRC:jPh?=
HEK293 MSR  NIHpTYtHfW6ldHnvckBCe3OjeR?= MnLkNE0yOCEQvF2= NHXieIQ4KG2rbh?= NXnJRWV5cW6qaXLpeJMhcFSKVGKyJJdqfGhiYX6gTWM2OMLib3[gNU4zyqEEtV2= MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB4M{[3Nkc,OjVyNkO2O|I9N2F-
MedB-1 M3XROGZ2dmO2aX;uJGF{e2G7 MmTnNU8zKM7:TR?= MVeyOEBp M{HBZYRm[3KnYYPld{BUXEGWNjDwbI9{eGixconsZZRqd25iY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? MmTDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7N{e2OlgoRjJ2OUe3OlY5RC:jPh?=
U2940 MmHuSpVv[3Srb36gRZN{[Xl? M37zSFEwOiEQvF2= MXOyOEBp MX;k[YNz\WG|ZYOgV3RCXDZicHjvd5Bpd3K7bHH0bY9vKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> M1;mZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUe3OlY5Lz5{NEm3O|Y3QDxxYU6=
K1106 MVnGeY5kfGmxbjDBd5NigQ>? MYCxM|Ih|ryP Mlj4NlQhcA>? M{\4dYRm[3KnYYPld{BUXEGWNjDwbI9{eGixconsZZRqd25iY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? MonoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7N{e2OlgoRjJ2OUe3OlY5RC:jPh?=
K562 NH:1O|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELHVmQxNTFizszN MXi3NkBp M3rLRolvcGmkaYTzJGs2PjJiY3XscEBxem:uaX\ldoF1cW:wIHH0JIhq\2hiY3;uZ4VvfHKjdHnvci=> NYq2R5d7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3O|U{ODhpPkK0O|c2OzB6PD;hQi=>
MDA-MB-468  NXLKTVd1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUKzJOK2VQ>? MYC0PEBp MlTs[Y5p[W6lZXSgd4lj[2x4IHnu[JVk\WRibH;zd{Bw\iClZXzsJJZq[WKrbHn0feKh NHWydpc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[2NlgyQCd-MkS2OlI5OTh:L3G+
MDA-MB-468 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnvWNE01KM7:TR?= NVPBWGJpPDhiaB?= NViydWtpemW|dXz0d{B{cWewaX\pZ4FvfCCub4PzJI9nKH[rYXLpcIl1gSClb33wZZJm\CC2bzDSTU1DWEliYXzvcoU> MnPUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NkK4NVgoRjJ2Nk[yPFE5RC:jPh?=
L428 NXvMeHYyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17ldFAuPSEQvF2= NYTze4xwPDhiaB?= M{PufIlvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= NITPNHI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[xNFgzPyd-MkS2NVA5Ojd:L3G+
KMH2 M2q3U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX6wMVUh|ryP M4PyU|Q5KGh? MYfpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 MnThQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4MUC4NlcoRjJ2NkGwPFI4RC:jPh?=
L1236 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzOZ3MxNTVizszN M{fFOFQ5KGh? NUHrRphmcW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> MnfDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4MUC4NlcoRjJ2NkGwPFI4RC:jPh?=
SUPHD1 M1TyOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1P2SFAuPSEQvF2= NHnYfHY1QCCq M4\pdolvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= NF7vdVU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[xNFgzPyd-MkS2NVA5Ojd:L3G+
HDLM2 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nsWFAuPSEQvF2= M2j3PVQ5KGh? M4riSYlvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= MljtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4MUC4NlcoRjJ2NkGwPFI4RC:jPh?=
K1106P MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\Me|AuPSEQvF2= NV\afXRwPDhiaB?= NF70emZqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZzMEiyO{c,OjR4MUC4Nlc9N2F-
L428 M{nseGFxd3C2b4Ppd{BCe3OjeR?= MVewM|AvPjJ3L{GuNlUh|ryP Ml3vOFghcA>? M4TMWYlv\HWlZYOgeIhmKGGyb4D0c5Nqe8Li Mom1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4MUC4NlcoRjJ2NkGwPFI4RC:jPh?=
KMH2 NEfTZpRCeG:ydH;zbZMhSXO|YYm= NIX3[5kxNzBwNkK1M|EvOjVizszN NYHMWmNNPDhiaB?= Ml;0bY5lfWOnczD0bIUh[XCxcITvd4l{yqB? NUHwR4NyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2NVA5OjdpPkK0OlExQDJ5PD;hQi=>
L1236 NVL3co11SXCxcITvd4l{KEG|c3H5 MUCwM|AvPjJ3L{GuNlUh|ryP NVm5WJNuPDhiaB?= MWDpcoR2[2W|IITo[UBieG:ydH;zbZPDqA>? MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZzMEiyO{c,OjR4MUC4Nlc9N2F-
SUPHD1 NWLveFQ{SXCxcITvd4l{KEG|c3H5 M1zxd|AwOC54MkWvNU4zPSEQvF2= MmHwOFghcA>? MmnMbY5lfWOnczD0bIUh[XCxcITvd4l{yqB? NUnWSoJqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2NVA5OjdpPkK0OlExQDJ5PD;hQi=>
HDLM2 MU\BdI9xfG:|aYOgRZN{[Xl? MY[wM|AvPjJ3L{GuNlUh|ryP MXe0PEBp NWHoblF4cW6mdXPld{B1cGViYYDvdJRwe2m|wrC= M3vMRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkGwPFI4Lz5{NE[xNFgzPzxxYU6=
K1106P NEDwXGRCeG:ydH;zbZMhSXO|YYm= NX3Bbol3OC9yLk[yOU8yNjJ3IN88US=> MVS0PEBp MWfpcoR2[2W|IITo[UBieG:ydH;zbZPDqA>? M2P5W|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkGwPFI4Lz5{NE[xNFgzPzxxYU6=
L428 M1[0XWZ2dmO2aX;uJGF{e2G7 NEjEfFcxNTVizszN MVeyOEBp Mm\ubY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> M2rZTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkGwPFI4Lz5{NE[xNFgzPzxxYU6=
KMH2 NYPMUnVsTnWwY4Tpc44hSXO|YYm= NULlSFF1OC13IN88US=> MoexNlQhcA>? NETuU|FqdmirYnn0d{BLSUt{L2PURXQhe2mpbnHsbY5o MlPmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4MUC4NlcoRjJ2NkGwPFI4RC:jPh?=
L1236 M3L5TmZ2dmO2aX;uJGF{e2G7 M1zmV|AuPSEQvF2= NWXsSldzOjRiaB?= M{fZXolvcGmkaYTzJGpCUzJxU2TBWEB{cWewYXzpcoc> MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZzMEiyO{c,OjR4MUC4Nlc9N2F-
SUPHD1 NV;PWIV1TnWwY4Tpc44hSXO|YYm= NGnrO|MxNTVizszN M2qybVI1KGh? NIj5UplqdmirYnn0d{BLSUt{L2PURXQhe2mpbnHsbY5o MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZzMEiyO{c,OjR4MUC4Nlc9N2F-
HDLM2 MmDJSpVv[3Srb36gRZN{[Xl? MnPhNE02KM7:TR?= NF3Te44zPCCq NEPrcFFqdmirYnn0d{BLSUt{L2PURXQhe2mpbnHsbY5o NX3UXHpGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2NVA5OjdpPkK0OlExQDJ5PD;hQi=>
K1106P M2PFdmZ2dmO2aX;uJGF{e2G7 M3u5UVAuPSEQvF2= M2jTSVI1KGh? MYrpcohq[mm2czDKRWszN1OWQWSgd4lodmGuaX7n NYDTcohyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2NVA5OjdpPkK0OlExQDJ5PD;hQi=>
MM.1S  NV7aXVBsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfES2ZKSzVyPUGtN{DPxE1? NGXUd3M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW4OFExOSd-MkS1PFQyODF:L3G+
TpoR JAK2 WT MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFPo[XhKSzVyPUGuOEApOS5|4pETNU42MSEQvF2= NVS4eVNjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyOVE4QTBpPkK0NlUyPzlyPD;hQi=>
TpoR JAK2 V617F MkLBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TvbWlEPTB;MD64JEgxNjgkgKOwMlkqKM7:TR?= NFfFSpI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEK1NVc6OCd-MkSyOVE4QTB:L3G+
TpoR W515L NVvE[G1CT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jrdWlEPTB;MD64JEgxNjgkgKOxMlAqKM7:TR?= NUTqfFdJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyOVE4QTBpPkK0NlUyPzlyPD;hQi=>
Bcr-abl NVXw[oM4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfpb4NKSzVyPUKuO{ApOi5{4pETN{4{MSEQvF2= NVridXg4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyOVE4QTBpPkK0NlUyPzlyPD;hQi=>
JAK2 TW MlO5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDvPFFKSzVyPUGuPEApOS534pETNk4{MSEQvF2= MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJ3MUe5NEc,OjR{NUG3PVA9N2F-
JAK2 V617F NVi0e2pTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mme1TWM2OD1yLk[gLFAvPuLCk{CuO{kh|ryP NYXoc297RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyOVE4QTBpPkK0NlUyPzlyPD;hQi=>
MedB-1 M3LjPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jUVVQh|ryP MkPiNlQwPDhxN{KgbC=> MkTXSG1UVw>? NYfRcFZZcW6qaXLpeJMh[2WubDDndo94fGhidHnt[UBl\XCnbnTlcpRtgQ>? NUX2boZJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OVI{PjZpPkKzPFUzOzZ4PD;hQi=>
K1106 NUDoOJRnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDWRok1KM7:TR?= MXiyOE81QC95MjDo M2OzbWROW09? MmPRbY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> MkfHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6NUKzOlYoRjJ|OEWyN|Y3RC:jPh?=
U2940 MmTmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVK0JO69VQ>? NH3nU4ozPC92OD:3NkBp NUnS[nJ1TE2VTx?= Ml;CbY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> NFfYWI09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i1NlM3Pid-MkO4OVI{PjZ:L3G+
FE-PD MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mom5NE4xPjNvNDFOwG0> NWrySVdlUUN3ME25MlUh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MmiwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|N{K2OlkoRjJ|M{eyOlY6RC:jPh?=
HEL NX\1PFVGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjuW3B2OC5yNkOtOEDPxE1? NHHTN3hKSzVyPUGuOUDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= NHWxSVU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O3NlY3QSd-MkOzO|I3Pjl:L3G+
K-562 NIjvc5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TsTlAvODZ|LUSg{txO MoC4TWM2OD1{LkWg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 MoHFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|N{K2OlkoRjJ|M{eyOlY6RC:jPh?=
L-82 MoLJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHmZZQxNjB4Mz20JO69VQ>? M2\pWWlEPTB;MD65PEDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN5Mk[2PUc,OjN|N{K2Olk9N2F-
MAC-1 NHm4OY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDQXHAxNjB4Mz20JO69VQ>? MU\JR|UxRTBwNUKg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 M3jTOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{eyOlY6Lz5{M{O3NlY3QTxxYU6=
MAC-2A MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVWwMlA3Oy12IN88US=> NFfYWJVKSzVyPUCuOlkh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NEHOcI89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O3NlY3QSd-MkOzO|I3Pjl:L3G+
MAC-2B NWn4bXprT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnSXG0xNjB4Mz20JO69VQ>? M2\h[GlEPTB;MD61OEDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= Mmj5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|N{K2OlkoRjJ|M{eyOlY6RC:jPh?=
MY-LA NU\sWJU{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTGOW9XOC5yNkOtOEDPxE1? NXL5[IxvUUN3ME2yMlEh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NIDWUGg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O3NlY3QSd-MkOzO|I3Pjl:L3G+
NC-NC MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3u4RVAvODZ|LUSg{txO M4fZUmlEPTB;MT6wJO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN5Mk[2PUc,OjN|N{K2Olk9N2F-
SE-AX MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17ON|AvODZ|LUSg{txO M4\C[2lEPTB;MT61JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= NV;EVWRFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzO|I3PjlpPkKzN|czPjZ7PD;hQi=>
SR-786 MlzzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlv6NE4xPjNvNDFOwG0> NInkfIFKSzVyPUSuOkDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= MlTnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|N{K2OlkoRjJ|M{eyOlY6RC:jPh?=
M-MOK  NWHaSmZsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjCPXkzPSEEtV5CpC=> MV[yOE81QC95MjDo NEXrWVdFVVOR MlHabY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTh3M{G1O{c,OjF6NUOxOVc9N2F-
HEL M3iyXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFn6SIFKSzVyPUOwOUBvVQ>? NH7OSG89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEO5OFU2PCd-MUizPVQ2PTR:L3G+
Ba/F3 JAK2V617F M4r4XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTJ5MDDuUS=> M1fnU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6M{m0OVU1Lz5zOEO5OFU2PDxxYU6=
MV4-11 Ml[wRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MonjO|IhcHK| M1riN2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTW[0MVEyKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDj[YxtfGm2ZYKtZox2\SCjc4PhfUwhTUN3MDC9JFAvODd7IN88UU4> M4\POlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MkiwNlYyLz5{OEK4NFI3OTxxYU6=
MM1S MkSzRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NH\Xc4E4OiCqcoO= NWmxOVJ[SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNUVFUKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTD0dplx[W5iYnz1[UBmgGOudYPpc44h[XO|YYmsJGlEPTBiPTCxJO69VS5? MoDPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OECyOlEoRjJ6MkiwNlYyRC:jPh?=
NB1643 NU\EUWQ6eUiWUzDhd5NigQ>? NVfJWI5EeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CNVY1OyClZXzsdy=> NYe2bXF4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-MC MnjvdWhVWyCjc4PhfS=> NVXRTZlJeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uVUNiY3XscJM> NXHnWooxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Assay
Methods Test Index PMID
Western blot p-JAK2 / p-STAT1 / p-STAT3 / p-STAT6 / p-STAT5 / JAK2 c-Myc / PIM1 24610827
Growth inhibition assay Cell proliferation 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]

  • 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]

  • 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。

动物实验:

[1]

  • 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

溶解度(25°C)

体外

* 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 3年 -20°C 粉状
2年 -80°C 溶于溶剂

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)

mg/kg g μL

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
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

摩尔浓度计算器

质量 浓度 体积 分子量

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04955938 Recruiting Drug: Ivosidenib|Drug: Enasidenib|Drug: Fedratinib IDH Mutation|IDH1 Mutation|IDH2 Gene Mutation|Blood Cancer|Myeloproliferative Neoplasm University of Chicago October 29 2021 Phase 1
NCT05051553 Completed Drug: Fedratinib Healthy Volunteers Bristol-Myers Squibb September 21 2021 Phase 1
NCT04702464 Completed Drug: Fedratinib|Drug: Fluconazole Healthy Volunteers Celgene|Impact Biomedicines Inc. a wholly owned subsidiary of Celgene Corporation January 12 2021 Phase 1
NCT03983161 Recruiting Drug: Fedratinib Healthy Volunteers|Hepatic Impairment Celgene|Impact Biomedicines Inc. a wholly owned subsidiary of Celgene Corporation September 4 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 --

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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