Fedratinib (TG101348)

For research use only.

Catalog No.S2736 Synonyms: SAR302503

57 publications

Fedratinib (TG101348) Chemical Structure

CAS No. 936091-26-8

Fedratinib (SAR302503, TG101348) is a selective inhibitor of JAK2 with IC50 of 3 nM in cell-free assays, 35- and 334-fold more selective for JAK2 versus JAK1 and JAK3. Fedratinib also inhibits FMS-like tyrosine kinase 3 (FLT3) and RET (c-RET) with IC50 of 15 nM and 48 nM, respectively. Fedratinib has potential antineoplastic activity. Fedratinib inhibits proliferation and induces apoptosis. Phase 2.

Selleck's Fedratinib (TG101348) has been cited by 57 publications

Purity & Quality Control

Choose Selective JAK Inhibitors

Biological Activity

Description Fedratinib (SAR302503, TG101348) is a selective inhibitor of JAK2 with IC50 of 3 nM in cell-free assays, 35- and 334-fold more selective for JAK2 versus JAK1 and JAK3. Fedratinib also inhibits FMS-like tyrosine kinase 3 (FLT3) and RET (c-RET) with IC50 of 15 nM and 48 nM, respectively. Fedratinib has potential antineoplastic activity. Fedratinib inhibits proliferation and induces apoptosis. Phase 2.
Targets
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
In vitro

TG-101348 also significantly inhibits JAK2 V617F, Flt3, and Ret with IC50 of 3 nM, 15 nM, and 48 nM, respectively. TG101348 has an IC50 ~300-fold higher for the closely related JAK3 and is a less potent inhibitor of the JAK1 and TYK2 family members. TG101348 inhibits 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 IC50 of 305 nM and 270 nM, respectively. TG-101348 also inhibits proliferation of parental Ba/F3 cells to a comparable level, with IC50 of ~420 nM. TG101348 treatment reduces STAT5 phosphorylation at concentrations that parallel the concentrations required to inhibit cell proliferation. TG101348 induces apoptosis in both HEL and Ba/F3 JAK2V617F cells in a dose-dependent manner. TG101348 does not show proapoptotic activity in control normal human dermal fibroblasts at concentrations up to 10 μM, and the antiproliferative IC50 against fibroblasts is >5 μM. [1] TG101348 treatment decreases GATA-1 expression, which is associated with erythroid-skewing of JAK2V617F+ progenitor differentiation, and inhibits STAT5 as well as GATA S310 phosphorylation. [2] TG101348 inhibits the proliferation of HMC-1.1 (KITV560G) cells, with somewhat lower potency than HMC-1.2 (KITD816V, KITV560G) cells, with IC50 of 740 nM and 407 nM, respectively. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
H1975 NWfqdYNOSXCxcITvd4l{KEG|c3H5 NF;NVG0xNjVvMjFOwG0> MYqxNk01QCCq MoLhSG1UVw>? M3XmWIlv\HWlZYOgZZBweHSxc3nzJIlvKGKxdHig[I9{\S1iYX7kJJRqdWVvIHTldIVv\GWwdDDtZY5v\XJ? MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh4OUKxNEc,OjV6NkmyNVA9N2F-
H1650 MXTBdI9xfG:|aYOgRZN{[Xl? M4XF[lAvPS1{IN88US=> NVK1SXBiOTJvNEigbC=> MXTEUXNQ NXjx[Jk2cW6mdXPld{BieG:ydH;zbZMhcW5iYn;0bEBld3OnLTDhcoQhfGmvZT2g[IVx\W6mZX70JI1idm6nch?= NF31R2c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUi2PVIyOCd-MkW4OlkzOTB:L3G+
H1975 M1qweWZ2dmO2aX;uJGF{e2G7 MUiwMlI2NTFizszN MYiyOEBp NFHxbm1FVVOR M3rEN4lvcGmkaYTzJIV5eHKnc4Ppc44hd2ZiYYDvdJRwe2m|LYLlcIF1\WRicILveIVqdiCEY3ytXGwtKEKlbD2yMEB{fXK4aY\pckwhYEmDUB?= NGPmO2M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUi2PVIyOCd-MkW4OlkzOTB:L3G+
H1650 M2nVeWZ2dmO2aX;uJGF{e2G7 MUGwMlI2NTFizszN NXHDXm5EOjRiaB?= MkKzSG1UVw>? MmXMbY5pcWKrdIOg[ZhxemW|c3nvckBw\iCjcH;weI9{cXNvcnXsZZRm\CCycn;0[YlvKEKlbD3YUEwhSmOuLUKsJJN2en[rdnnuMEBZUUGS NUmyO3A2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4OlkzOTBpPkK1PFY6OjFyPD;hQi=>
H1975 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFm2d20yKM7:TR?= NFHobGI1QCCq MVjEUXNQ Ml7xd4Vve2m2aYrld{Bk\WyuczD0c{B1cGViY4n0c5RwgGmlaYT5JI9nKGW{bH;0bY5q[g>? MnzuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6NkmyNVAoRjJ3OE[5NlExRC:jPh?=
H1650 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnX5NUDPxE1? M17PfVQ5KGh? NUHIOHZ6TE2VTx?= NFHZfpd{\W6|aYTpfoV{KGOnbHzzJJRwKHSqZTDjfZRwfG:6aXPpeJkhd2ZiZYLsc5Rqdmmk M1XzWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OE[5NlExLz5{NUi2PVIyODxxYU6=
CD4+ T NEfabJBHfW6ldHnvckBCe3OjeR?= NH7rPW0xNjBzLUGg{txO NIfjS4Y1QCCq NYfVcVl{TE2VTx?= MYLy[YR2[2W|IITo[UBxcG:|cHjvdplt[XSrb36gcIV3\Wy|IH;mJGpCUzJiYX7kJHNVSVR|wrC= NFTLRpo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUW3NlU{PSd-MkW1O|I2OzV:L3G+
Caco-2  NYjoVlJCTnWwY4Tpc44hSXO|YYm= MmS3NE0yOjBizszN MorCO{BucW5? M3\OUIlvcGmkaYTzJJRpcWGvaX7lJJVxfGGtZTD3bZRpKGGwIFnDOVDDqG:oIEKuNeKhyrWP Mnz0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyNkO2O|IoRjJ3ME[zOlczRC:jPh?=
Caco-2  NWPaTHh6TnWwY4Tpc44hSXO|YYm= NUjNZ4o3OTBxNUCvNVAxKM7:TR?= MYmyJIg> NHvMUIpl\WO{ZXHz[ZMhfGinIH\seZghd2ZiW{PIYZRpcWGvaX7lJIFkem:|czD0bIUhdW:wb3zhfYVzKHerdHigTWM2OCCxZjC2MlXDqM7:TR?= NWjGZY9QRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwOlM3PzJpPkK1NFY{Pjd{PD;hQi=>
HEK293 MSR  Mn;tSpVv[3Srb36gRZN{[Xl? NUDFZlh5OC1zMDFOwG0> NWD1dJROPyCvaX6= NITEZ5JqdmirYnn0d{BpXEiWUkKge4l1cCCjbjDJR|UxyqCxZjCxMlLDqML3TR?= NGjudYY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC2N|Y4Oid-MkWwOlM3PzJ:L3G+
MedB-1 M1TzTGZ2dmO2aX;uJGF{e2G7 NF\DOI8yNzJizszN M3ntbFI1KGh? NWe5NGNQ\GWlcnXhd4V{KFOWQWS2JJBpd3OyaH;yfYxifGmxbjDjc45k\W62cnH0bY9vKGSncHXu[IVvfGy7 NEnEXYU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm3O|Y3QCd-MkS5O|c3Pjh:L3G+
U2940 M{LhNGZ2dmO2aX;uJGF{e2G7 M{D4OFEwOiEQvF2= M3nl[|I1KGh? NEXmVmxl\WO{ZXHz[ZMhW1SDVE[gdIhwe3Cqb4L5cIF1cW:wIHPvcoNmdnS{YYTpc44h\GWyZX7k[Y51dHl? MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl5N{[2PEc,OjR7N{e2Olg9N2F-
K1106 Ml\PSpVv[3Srb36gRZN{[Xl? M2K0dlEwOiEQvF2= NY\3fphUOjRiaB?= NWLJTXhx\GWlcnXhd4V{KFOWQWS2JJBpd3OyaH;yfYxifGmxbjDjc45k\W62cnH0bY9vKGSncHXu[IVvfGy7 MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl5N{[2PEc,OjR7N{e2Olg9N2F-
K562 M{W5[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHTS3QxNTFizszN NIOw[o44OiCq MUHpcohq[mm2czDLOVYzKGOnbHygdJJwdGmoZYLheIlwdiCjdDDobYdpKGOxbnPlcpRz[XSrb36= M{\VbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2N{e1N|A5Lz5{NEe3OVMxQDxxYU6=
MDA-MB-468  MkP0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjoemMxOyEEtV2= M3LX[lQ5KGh? NH3GOGVmdmijbnPl[EB{cWKlbE[gbY5lfWOnZDDsc5N{KG:oIHPlcIwhfmmjYnnsbZR6yqB? Ml3KQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NkK4NVgoRjJ2Nk[yPFE5RC:jPh?=
MDA-MB-468 NYS0dVMxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzRTG0xNTRizszN M3nt[lQ5KGh? NES4NYNz\XO3bITzJJNq\26rZnnjZY51KGyxc4Ogc4YhfmmjYnnsbZR6KGOxbYDhdoVlKHSxIGLJMWJRUSCjbH;u[S=> NETkS|E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[2NlgyQCd-MkS2OlI5OTh:L3G+
L428 M4XYSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIG4SFUxNTVizszN NHfvV|k1QCCq MX;pcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZzMEiyO{c,OjR4MUC4Nlc9N2F-
KMH2 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1e0W|AuPSEQvF2= NHjWUGo1QCCq NF\2cnJqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 NIDHc2Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[xNFgzPyd-MkS2NVA5Ojd:L3G+
L1236 M3Pmc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXuwMVUh|ryP NXPXXlVOPDhiaB?= M2C0dIlvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZzMEiyO{c,OjR4MUC4Nlc9N2F-
SUPHD1 MlHYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLENE02KM7:TR?= NV;BOZZ3PDhiaB?= NIrEeoVqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZzMEiyO{c,OjR4MUC4Nlc9N2F-
HDLM2 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVewMVUh|ryP NETGVFI1QCCq MkLGbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= Mkf1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4MUC4NlcoRjJ2NkGwPFI4RC:jPh?=
K1106P NX65NIlVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXKwMVUh|ryP NWTCN|V7PDhiaB?= NWTXNXB1cW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> MknHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4MUC4NlcoRjJ2NkGwPFI4RC:jPh?=
L428 NX;scWF[SXCxcITvd4l{KEG|c3H5 NYPtVZpnOC9yLk[yOU8yNjJ3IN88US=> Mk\YOFghcA>? M4XKeYlv\HWlZYOgeIhmKGGyb4D0c5Nqe8Li MkLzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4MUC4NlcoRjJ2NkGwPFI4RC:jPh?=
KMH2 NVLiVXExSXCxcITvd4l{KEG|c3H5 NF;tdVExNzBwNkK1M|EvOjVizszN MYC0PEBp MnXXbY5lfWOnczD0bIUh[XCxcITvd4l{yqB? NYPVXFlWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2NVA5OjdpPkK0OlExQDJ5PD;hQi=>
L1236 M2XtOmFxd3C2b4Ppd{BCe3OjeR?= MoLUNE8xNjZ{NT:xMlI2KM7:TR?= NFTURoE1QCCq NWHlPWRvcW6mdXPld{B1cGViYYDvdJRwe2m|wrC= NVzybolvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2NVA5OjdpPkK0OlExQDJ5PD;hQi=>
SUPHD1 M1rlVGFxd3C2b4Ppd{BCe3OjeR?= MYewM|AvPjJ3L{GuNlUh|ryP NVzqbVViPDhiaB?= M1ixdolv\HWlZYOgeIhmKGGyb4D0c5Nqe8Li MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZzMEiyO{c,OjR4MUC4Nlc9N2F-
HDLM2 NUHNd4xnSXCxcITvd4l{KEG|c3H5 MoDQNE8xNjZ{NT:xMlI2KM7:TR?= MXO0PEBp Mm\0bY5lfWOnczD0bIUh[XCxcITvd4l{yqB? M1m0TVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkGwPFI4Lz5{NE[xNFgzPzxxYU6=
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L428 M1PNWmZ2dmO2aX;uJGF{e2G7 M{fTb|AuPSEQvF2= NVT6Vm11OjRiaB?= MXLpcohq[mm2czDKRWszN1OWQWSgd4lodmGuaX7n MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZzMEiyO{c,OjR4MUC4Nlc9N2F-
KMH2 NVPqVINFTnWwY4Tpc44hSXO|YYm= MoGxNE02KM7:TR?= MViyOEBp MkH4bY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> M1vYXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkGwPFI4Lz5{NE[xNFgzPzxxYU6=
L1236 MWjGeY5kfGmxbjDBd5NigQ>? MViwMVUh|ryP NGHKZYszPCCq NYXVRodOcW6qaXLpeJMhUkGNMj;TWGFVKHOrZ37hcIlv\w>? MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZzMEiyO{c,OjR4MUC4Nlc9N2F-
SUPHD1 M3jDbGZ2dmO2aX;uJGF{e2G7 MUGwMVUh|ryP NH;iV|IzPCCq M2HXVolvcGmkaYTzJGpCUzJxU2TBWEB{cWewYXzpcoc> NWfueolHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2NVA5OjdpPkK0OlExQDJ5PD;hQi=>
HDLM2 NGjxOmZHfW6ldHnvckBCe3OjeR?= M3TzR|AuPSEQvF2= MnzxNlQhcA>? MlPobY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> NH3RUXM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[xNFgzPyd-MkS2NVA5Ojd:L3G+
K1106P M1PP[GZ2dmO2aX;uJGF{e2G7 NWDD[3NyOC13IN88US=> M4\oRlI1KGh? NGe0[oJqdmirYnn0d{BLSUt{L2PURXQhe2mpbnHsbY5o NF70VGs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[xNFgzPyd-MkS2NVA5Ojd:L3G+
MM.1S  NGHuOWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;WdWlEPTB;MT2zJO69VQ>? Ml\HQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3OESxNFEoRjJ2NUi0NVAyRC:jPh?=
TpoR JAK2 WT NFe0XnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFGx[FNKSzVyPUGuOEApOS5|4pETNU42MSEQvF2= M3TrUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MkWxO|kxLz5{NEK1NVc6ODxxYU6=
TpoR JAK2 V617F M3joWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjrSYpKSzVyPUCuPEApOC554pETNE46MSEQvF2= M2PsVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MkWxO|kxLz5{NEK1NVc6ODxxYU6=
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Bcr-abl MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnJeYpKSzVyPUKuO{ApOi5{4pETN{4{MSEQvF2= M2\2PVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MkWxO|kxLz5{NEK1NVc6ODxxYU6=
JAK2 TW M333dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTFwODCoNU426oDVMj6zLUDPxE1? Mn3ZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR{NUG3PVAoRjJ2MkWxO|kxRC:jPh?=
JAK2 V617F MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFO3V3JKSzVyPUCuOkApOC544pETNE44MSEQvF2= NWfJN4djRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyOVE4QTBpPkK0NlUyPzlyPD;hQi=>
MedB-1 MnXMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHHOnhFPCEQvF2= M2jGS|I1NzR6L{eyJIg> M4rISGROW09? MUXpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 NFuwOYg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i1NlM3Pid-MkO4OVI{PjZ:L3G+
K1106 NUf6[HV[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPuPI1xPCEQvF2= MoLRNlQwPDhxN{KgbC=> MY\EUXNQ MnTNbY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh3MkO2Okc,OjN6NUKzOlY9N2F-
U2940 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUC0JO69VQ>? NXzRUY1XOjRxNEivO|IhcA>? MUXEUXNQ MnHPbY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> NUHHS|doRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OVI{PjZpPkKzPFUzOzZ4PD;hQi=>
FE-PD MkjOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWLkXXBJOC5yNkOtOEDPxE1? NG\ieYxKSzVyPUmuOUDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= NXPmSoRxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzO|I3PjlpPkKzN|czPjZ7PD;hQi=>
HEL NGq4SYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlW2NE4xPjNvNDFOwG0> M1ToTGlEPTB;MT61JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= NF:4d2o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O3NlY3QSd-MkOzO|I3Pjl:L3G+
K-562 M3n6b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1v1OlAvODZ|LUSg{txO NGnZNmFKSzVyPUKuOUDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= M2fHWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{eyOlY6Lz5{M{O3NlY3QTxxYU6=
L-82 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\lNE4xPjNvNDFOwG0> MWfJR|UxRTBwOUig{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN5Mk[2PUc,OjN|N{K2Olk9N2F-
MAC-1 MkHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTxbGExNjB4Mz20JO69VQ>? NUG1ZZoyUUN3ME2wMlUzKM7:TTygbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MnHWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|N{K2OlkoRjJ|M{eyOlY6RC:jPh?=
MAC-2A M4H0bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUiwMlA3Oy12IN88US=> NX;nNFFZUUN3ME2wMlY6KM7:TTygbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NIjNPZQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O3NlY3QSd-MkOzO|I3Pjl:L3G+
MAC-2B MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPvNE4xPjNvNDFOwG0> NFzNOXFKSzVyPUCuOVQh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 Ml\jQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|N{K2OlkoRjJ|M{eyOlY6RC:jPh?=
MY-LA M4O3NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXztc2o5OC5yNkOtOEDPxE1? M2jQ[mlEPTB;Mj6xJO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= NGX6WJU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O3NlY3QSd-MkOzO|I3Pjl:L3G+
NC-NC NUmzR|BvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnwNE4xPjNvNDFOwG0> Mmf4TWM2OD1zLkCg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 NVrZ[m9wRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzO|I3PjlpPkKzN|czPjZ7PD;hQi=>
SE-AX MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY[zblFHOC5yNkOtOEDPxE1? M4jWSGlEPTB;MT61JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN5Mk[2PUc,OjN|N{K2Olk9N2F-
SR-786 Mke0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLE[GNtOC5yNkOtOEDPxE1? M3nyOmlEPTB;ND62JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN5Mk[2PUc,OjN|N{K2Olk9N2F-
M-MOK  NInqXppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1PscVI2KML3TdMg MoTrNlQwPDhxN{KgbC=> MVfEUXNQ M{HsSYlvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> NGW2eFU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUi1N|E2Pyd-MkG4OVMyPTd:L3G+
HEL M4X4WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\QTWM2OD1|MEWgcm0> MmK5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh|OUS1OVQoRjF6M{m0OVU1RC:jPh?=
Ba/F3 JAK2V617F Ml6wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYT6U|htUUN3ME2yO|Ahdk1? MnTPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh|OUS1OVQoRjF6M{m0OVU1RC:jPh?=
MV4-11 M1nES2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 Mn7wO|IhcHK| M4LhXWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTW[0MVEyKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDj[YxtfGm2ZYKtZox2\SCjc4PhfUwhTUN3MDC9JFAvODd7IN88UU4> MnS1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OECyOlEoRjJ6MkiwNlYyRC:jPh?=
MM1S NELxWINCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M1vUTlczKGi{cx?= MXjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2PMWOgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KHS{eYDhckBjdHWnIHX4Z4x2e2mxbjDhd5NigSxiSVO1NEA:KDFizszNMi=> MmHLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OECyOlEoRjJ6MkiwNlYyRC:jPh?=
NB1643 M4X6ZZFJXFNiYYPzZZk> NWnUcHVzeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CNVY1OyClZXzsdy=> NWPpR|VFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-MC MnjzdWhVWyCjc4PhfS=> M1LoWZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMW1EKGOnbHzz M1vxO|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
In vivo

TG101348 has potential for efficacious treatment of JAK2V617F-associated myeloproliferative diseases (MPD). In treated animals, there is 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, correlated with surrogate endpoints, including reduction/elimination of JAK2V617F disease burden, suppression of endogenous erythroid colony formation, and in vivo inhibition of JAK-STAT signal transduction. There are no apparent toxicities and no effect on T cell number. [1] Oral administration of TG101348 (120 mg/kg) significantly inhibits PV progenitor erythroid differentiation in vivo. [2]

Protocol

Kinase Assay:

[1]

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Cell-free Kinase Activity Assays:

IC50 values for TG101348 are determined commercially using the InVitrogen kinase profiling service for a 223 kinase screen that included JAK2 and JAK2V617F or Carna Biosciences for the screen of all Janus kinase family members including JAK1 and Tyk2. ATP concentration is set to approximately the Km value for each kinase.
Cell Research:

[1]

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  • Cell lines: EpoBa/F3 JAK2V617F, Ba/F3p210, HEL, and K562
  • Concentrations: Dissolved in DMSO, final concentrations ~10 μM
  • Incubation Time: 72 hours
  • Method:

    Approximately 2 × 103 cells are plated into microtiter-plate wells in 100 μL RPMI-1640 growth media with indicated concentrations of inhibitor. Following 72 hours incubation with TG101348, 50 μL of XTT dye are added to each well and incubated for 4 hours in a CO2 incubator. The colored formazan product is measured by spectrophotometry at 450 nm with correction at 650 nm. The concentration in which 50% of the effect (i.e., inhibition of proliferation) is observed (IC50) is determined using the GraphPad Prism 4.0 software. All experiments are performed in triplicate, and the results are normalized to growth of untreated cells. Induction of apoptosis of EpoBa/F3 JAK2V617F, Ba/F3p210, HEL, and K562 cells is determined by DNA fragmentation with DMSO and increasing concentrations of TG101348.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: C57BL/6 mice injected intravenously with whole bone marrow expressing JAK2V617F
  • Dosages: ~120 mg/kg
  • Administration: Oral gavage twice daily (b.i.d.)
    (Only for Reference)

Solubility (25°C)

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 524.68
Formula

C27H36N6O3S

CAS No. 936091-26-8
Storage powder
in solvent
Synonyms SAR302503
Smiles CC1=CN=C(N=C1NC2=CC(=CC=C2)S(=O)(=O)NC(C)(C)C)NC3=CC=C(C=C3)OCCN4CCCC4

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
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Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • 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):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID