Fedratinib (TG101348)

Catalog No.S2736 Synonyms: SAR302503

For research use only.

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.

Fedratinib (TG101348) Chemical Structure

CAS No. 936091-26-8

Selleck's Fedratinib (TG101348) has been cited by 68 publications

Purity & Quality Control

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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 NF[0SG5CeG:ydH;zbZMhSXO|YYm= M4TFbFAvPS1{IN88US=> NEfPeFcyOi12ODDo M1e3TmROW09? M2PieYlv\HWlZYOgZZBweHSxc3nzJIlvKGKxdHig[I9{\S1iYX7kJJRqdWVvIHTldIVv\GWwdDDtZY5v\XJ? M3zvUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OE[5NlExLz5{NUi2PVIyODxxYU6=
H1650 NHjBRohCeG:ydH;zbZMhSXO|YYm= MWCwMlUuOiEQvF2= MoPjNVIuPDhiaB?= NVfyfItRTE2VTx?= MVjpcoR2[2W|IHHwc5B1d3OrczDpckBjd3SqIHTvd4UuKGGwZDD0bY1mNSCmZYDlcoRmdnRibXHucoVz NYnkXmVlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4OlkzOTBpPkK1PFY6OjFyPD;hQi=>
H1975 NF;NfFRHfW6ldHnvckBCe3OjeR?= M3nEWFAvOjVvMTFOwG0> M2XSflI1KGh? NGCxc3hFVVOR NGSzVnVqdmirYnn0d{BmgHC{ZYPzbY9vKG:oIHHwc5B1d3Orcz3y[YxifGWmIIDyc5RmcW5iQnPsMXhNNCCEY3ytNkwhe3W{dnn2bY4tKFiLQWC= NWjj[4dqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4OlkzOTBpPkK1PFY6OjFyPD;hQi=>
H1650 MkXRSpVv[3Srb36gRZN{[Xl? NY\kSmFXOC5{NT2xJO69VQ>? MUOyOEBp MVnEUXNQ M2rsSIlvcGmkaYTzJIV5eHKnc4Ppc44hd2ZiYYDvdJRwe2m|LYLlcIF1\WRicILveIVqdiCEY3ytXGwtKEKlbD2yMEB{fXK4aY\pckwhYEmDUB?= NH\STXk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUi2PVIyOCd-MkW4OlkzOTB:L3G+
H1975 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLVNUDPxE1? MXu0PEBp M1:1PWROW09? MVfz[Y5{cXSrenXzJINmdGy|IITvJJRp\SCleYTveI95cWOrdImgc4Yh\XKub4Tpcolj M3O2TFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OE[5NlExLz5{NUi2PVIyODxxYU6=
H1650 MknlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPsNUDPxE1? NGDXVWI1QCCq M4PsfmROW09? MmTzd4Vve2m2aYrld{Bk\WyuczD0c{B1cGViY4n0c5RwgGmlaYT5JI9nKGW{bH;0bY5q[g>? NIj2UpA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUi2PVIyOCd-MkW4OlkzOTB:L3G+
CD4+ T NGfNN2tHfW6ldHnvckBCe3OjeR?= NYjtUIYzOC5yMT2xJO69VQ>? MVW0PEBp MmfnSG1UVw>? MnHkdoVlfWOnczD0bIUheGixc4Doc5J6dGG2aX;uJIxmfmWuczDv[kBLSUt{IHHu[EBUXEGWM9Mg M4rjO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NUeyOVM2Lz5{NUW3NlU{PTxxYU6=
Caco-2  NH7XNWlHfW6ldHnvckBCe3OjeR?= MWiwMVEzOCEQvF2= M1e3VFchdWmw MX\pcohq[mm2czD0bIlidWmwZTD1dJRic2Vid3n0bEBidiCLQ{WwxsBw\iB{LkJCpOK2VQ>? MlPYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyNkO2O|IoRjJ3ME[zOlczRC:jPh?=
Caco-2  NXXy[3o4TnWwY4Tpc44hSXO|YYm= NELQeHoyOC93MD:xNFAh|ryP NEfxVXkzKGh? NVPITmlz\GWlcnXhd4V{KHSqZTDmcJV5KG:oIGuzTH11cGmjbXnu[UBi[3Kxc4OgeIhmKG2xbn;sZZlmeiC5aYToJGlEPTBib3[gOk42yqEQvF2= MnTGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyNkO2O|IoRjJ3ME[zOlczRC:jPh?=
HEK293 MSR  NWPNU2t4TnWwY4Tpc44hSXO|YYm= MYGwMVExKM7:TR?= NHjlVZc4KG2rbh?= MW\pcohq[mm2czDoWGhVWjJid3n0bEBidiCLQ{WwxsBw\iBzLkNCpOK2VQ>? MmPtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyNkO2O|IoRjJ3ME[zOlczRC:jPh?=
MedB-1 MkW3SpVv[3Srb36gRZN{[Xl? NIDvSFAyNzJizszN M1;OeVI1KGh? MlzF[IVkemWjc3XzJHNVSVR4IIDoc5NxcG:{eXzheIlwdiClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NY\xeXZIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5O|c3PjhpPkK0PVc4PjZ6PD;hQi=>
U2940 NFTu[5ZHfW6ldHnvckBCe3OjeR?= M3XLbFEwOiEQvF2= NIrmRogzPCCq MVTk[YNz\WG|ZYOgV3RCXDZicHjvd5Bpd3K7bHH0bY9vKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> MmPUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7N{e2OlgoRjJ2OUe3OlY5RC:jPh?=
K1106 M3ju[2Z2dmO2aX;uJGF{e2G7 MWSxM|Ih|ryP NGrDWYkzPCCq MkHw[IVkemWjc3XzJHNVSVR4IIDoc5NxcG:{eXzheIlwdiClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NGLDcIM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm3O|Y3QCd-MkS5O|c3Pjh:L3G+
K562 NUDoZoFTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjnWJUxNTFizszN M{XadlczKGh? NFHH[nJqdmirYnn0d{BMPTZ{IHPlcIwheHKxbHnm[ZJifGmxbjDheEBpcWeqIHPvcoNmdnS{YYTpc44> M3q5RVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2N{e1N|A5Lz5{NEe3OVMxQDxxYU6=
MDA-MB-468  M{fXV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFGxUHQ{KML3TR?= NHPJSWI1QCCq M4i0VIVvcGGwY3XkJJNq[mOuNjDpcoR2[2WmIHzvd5Mhd2ZiY3XscEB3cWGkaXzpeJnDqA>? Mn\YQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NkK4NVgoRjJ2Nk[yPFE5RC:jPh?=
MDA-MB-468 NYSweWFIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LWTVAuPCEQvF2= NIjDO5M1QCCq M3;PV5Jme3WudIOgd4lodmmoaXPhcpQhdG:|czDv[kB3cWGkaXzpeJkh[2:vcHHy[YQhfG9iUlmtRnBKKGGub37l MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ4MkixPEc,OjR4NkK4NVg9N2F-
L428 Mkf4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXiwMVUh|ryP NXHvW3ZJPDhiaB?= Ml3HbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= NHrjTG89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[xNFgzPyd-MkS2NVA5Ojd:L3G+
KMH2 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlP5NE02KM7:TR?= NFPmOVQ1QCCq Moq5bY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZzMEiyO{c,OjR4MUC4Nlc9N2F-
L1236 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYKwMVUh|ryP M4rUW|Q5KGh? NYPzU|NRcW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> MmqwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4MUC4NlcoRjJ2NkGwPFI4RC:jPh?=
SUPHD1 NFPpbYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nOXFAuPSEQvF2= NX[2N3VsPDhiaB?= NVfaN40ycW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> NEizVFg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[xNFgzPyd-MkS2NVA5Ojd:L3G+
HDLM2 NHexeWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4W1clAuPSEQvF2= M3XIOFQ5KGh? NVXMbWNUcW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> NVXu[JRxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2NVA5OjdpPkK0OlExQDJ5PD;hQi=>
K1106P NEPRPVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2XiZ|AuPSEQvF2= MkfBOFghcA>? M16zOYlvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= NUDWSFY2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2NVA5OjdpPkK0OlExQDJ5PD;hQi=>
L428 MnX2RZBweHSxc3nzJGF{e2G7 M4TROlAwOC54MkWvNU4zPSEQvF2= MmH0OFghcA>? NF;z[5JqdmS3Y3XzJJRp\SCjcH;weI9{cXQEoB?= NV[4OGk2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2NVA5OjdpPkK0OlExQDJ5PD;hQi=>
KMH2 M1W1bmFxd3C2b4Ppd{BCe3OjeR?= MV6wM|AvPjJ3L{GuNlUh|ryP M1W4XVQ5KGh? MoPZbY5lfWOnczD0bIUh[XCxcITvd4l{yqB? NHO1XVU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[xNFgzPyd-MkS2NVA5Ojd:L3G+
L1236 NVvGeGd{SXCxcITvd4l{KEG|c3H5 NFvpO5YxNzBwNkK1M|EvOjVizszN NY\BW3JxPDhiaB?= NEG0blNqdmS3Y3XzJJRp\SCjcH;weI9{cXQEoB?= Mn7YQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4MUC4NlcoRjJ2NkGwPFI4RC:jPh?=
SUPHD1 NIPnZVVCeG:ydH;zbZMhSXO|YYm= NUTzeIdROC9yLk[yOU8yNjJ3IN88US=> M4\lOFQ5KGh? NFHncGJqdmS3Y3XzJJRp\SCjcH;weI9{cXQEoB?= NETn[oE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[xNFgzPyd-MkS2NVA5Ojd:L3G+
HDLM2 NGPaXHFCeG:ydH;zbZMhSXO|YYm= M4P0XFAwOC54MkWvNU4zPSEQvF2= M3mxR|Q5KGh? MVrpcoR2[2W|IITo[UBieG:ydH;zbZPDqA>? NFv3O|M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[xNFgzPyd-MkS2NVA5Ojd:L3G+
K1106P NU\nTZg{SXCxcITvd4l{KEG|c3H5 NVfqSXdUOC9yLk[yOU8yNjJ3IN88US=> M1jLXlQ5KGh? M3LhW4lv\HWlZYOgeIhmKGGyb4D0c5Nqe8Li Ml:zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4MUC4NlcoRjJ2NkGwPFI4RC:jPh?=
L428 MW\GeY5kfGmxbjDBd5NigQ>? NX\MUnBEOC13IN88US=> Ml;rNlQhcA>? NV7Q[ndvcW6qaXLpeJMhUkGNMj;TWGFVKHOrZ37hcIlv\w>? NFLtWGM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[xNFgzPyd-MkS2NVA5Ojd:L3G+
KMH2 M3S2ZWZ2dmO2aX;uJGF{e2G7 MnjPNE02KM7:TR?= NXiybZFNOjRiaB?= MmHRbY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> MkPpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4MUC4NlcoRjJ2NkGwPFI4RC:jPh?=
L1236 MXzGeY5kfGmxbjDBd5NigQ>? Ml;rNE02KM7:TR?= MVuyOEBp MlfabY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> Mmf6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4MUC4NlcoRjJ2NkGwPFI4RC:jPh?=
SUPHD1 MlnsSpVv[3Srb36gRZN{[Xl? M37ZflAuPSEQvF2= MWOyOEBp NH\mOlVqdmirYnn0d{BLSUt{L2PURXQhe2mpbnHsbY5o MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZzMEiyO{c,OjR4MUC4Nlc9N2F-
HDLM2 NXzoUoFCTnWwY4Tpc44hSXO|YYm= M4DIZVAuPSEQvF2= NFrVd2ozPCCq MoDGbY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> NH7WZm09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[xNFgzPyd-MkS2NVA5Ojd:L3G+
K1106P NUS5NpRtTnWwY4Tpc44hSXO|YYm= M{PpO|AuPSEQvF2= NV3sNWhMOjRiaB?= NGLFTmtqdmirYnn0d{BLSUt{L2PURXQhe2mpbnHsbY5o NGHN[lU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[xNFgzPyd-MkS2NVA5Ojd:L3G+
MM.1S  MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\ISZJKSzVyPUGtN{DPxE1? NF36TZc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW4OFExOSd-MkS1PFQyODF:L3G+
TpoR JAK2 WT NEfJW21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnxfJJKSzVyPUGuOEApOS5|4pETNU42MSEQvF2= NHvzVHU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEK1NVc6OCd-MkSyOVE4QTB:L3G+
TpoR JAK2 V617F NUfMRmp3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmSwTWM2OD1yLkigLFAvP+LCk{CuPUkh|ryP M3TlSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MkWxO|kxLz5{NEK1NVc6ODxxYU6=
TpoR W515L NYL4fXVjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDrTWM2OD1yLkigLFAvP+LCk{GuNEkh|ryP NWrISINrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyOVE4QTBpPkK0NlUyPzlyPD;hQi=>
Bcr-abl NYHMXWxRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTJwNzCoNk4z6oDVMz6zLUDPxE1? M3PGe|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MkWxO|kxLz5{NEK1NVc6ODxxYU6=
JAK2 TW NXLqeFRmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTXTWM2OD1zLkigLFEvPeLCk{KuN{kh|ryP Ml\DQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR{NUG3PVAoRjJ2MkWxO|kxRC:jPh?=
JAK2 V617F M2Tkd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1v2ZmlEPTB;MD62JEgxNjckgKOwMlcqKM7:TR?= NGnOfoI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEK1NVc6OCd-MkSyOVE4QTB:L3G+
MedB-1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rtdlQh|ryP M1\pOVI1NzR6L{eyJIg> Mnu5SG1UVw>? MofzbY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> MnjvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6NUKzOlYoRjJ|OEWyN|Y3RC:jPh?=
K1106 M3HlZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzsOEDPxE1? NFe3fWMzPC92OD:3NkBp NIXIZoJFVVOR M2XlNIlvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> NXrFUJhVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OVI{PjZpPkKzPFUzOzZ4PD;hQi=>
U2940 NH2yRpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYW3b5dyPCEQvF2= MVeyOE81QC95MjDo MnLlSG1UVw>? NVfySWF3cW6qaXLpeJMh[2WubDDndo94fGhidHnt[UBl\XCnbnTlcpRtgQ>? NIjjUmE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i1NlM3Pid-MkO4OVI{PjZ:L3G+
FE-PD NEnjb|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLvN5MxNjB4Mz20JO69VQ>? MVfJR|UxRTlwNTFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? NXHXR5htRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzO|I3PjlpPkKzN|czPjZ7PD;hQi=>
HEL NYjJcJhxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWm3TXJmOC5yNkOtOEDPxE1? NIDafYxKSzVyPUGuOUDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= NWLBVXdFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzO|I3PjlpPkKzN|czPjZ7PD;hQi=>
K-562 NXLROnM6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfHPXYxNjB4Mz20JO69VQ>? MofPTWM2OD1{LkWg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 NHfDN|E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O3NlY3QSd-MkOzO|I3Pjl:L3G+
L-82 MmrlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nrNFAvODZ|LUSg{txO NFjMU3pKSzVyPUCuPVgh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MoL3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|N{K2OlkoRjJ|M{eyOlY6RC:jPh?=
MAC-1 NHjGc4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mkj6NE4xPjNvNDFOwG0> NXXo[pY6UUN3ME2wMlUzKM7:TTygbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NVzNcYhiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzO|I3PjlpPkKzN|czPjZ7PD;hQi=>
MAC-2A NHKwc4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXywMlA3Oy12IN88US=> M1XSbmlEPTB;MD62PUDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= NYXTe5g1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzO|I3PjlpPkKzN|czPjZ7PD;hQi=>
MAC-2B NHPDSYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVOwMlA3Oy12IN88US=> NYrQe4kxUUN3ME2wMlU1KM7:TTygbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NYHLVmtCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzO|I3PjlpPkKzN|czPjZ7PD;hQi=>
MY-LA M2Xyc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XEUVAvODZ|LUSg{txO MVPJR|UxRTJwMTFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? M2X3fVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{eyOlY6Lz5{M{O3NlY3QTxxYU6=
NC-NC NEflUm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1qzSFAvODZ|LUSg{txO MVrJR|UxRTFwMDFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? NVLyNHpLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzO|I3PjlpPkKzN|czPjZ7PD;hQi=>
SE-AX MnvCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHnNE4xPjNvNDFOwG0> MVTJR|UxRTFwNTFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? MmDRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|N{K2OlkoRjJ|M{eyOlY6RC:jPh?=
SR-786 NVfVV25wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPtPFRxOC5yNkOtOEDPxE1? MlzlTWM2OD12Lk[g{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN5Mk[2PUc,OjN|N{K2Olk9N2F-
M-MOK  NIfJZldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV2yOUDDvU4EoB?= NV;HNmRjOjRxNEivO|IhcA>? NEDxZodFVVOR M4jYeIlvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> M4nv[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOEWzNVU4Lz5{MUi1N|E2PzxxYU6=
HEL NXrieW5KT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7YWmNKSzVyPUOwOUBvVQ>? MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDN7NEW1OEc,OTh|OUS1OVQ9N2F-
Ba/F3 JAK2V617F MmC4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4D5NWlEPTB;MkewJI5O MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDN7NEW1OEc,OTh|OUS1OVQ9N2F-
MV4-11 M{j1ZWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MVy3NkBpenN? NULOd4o5SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNWlQuOTFiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JINmdGy2aYTldk1jdHWnIHHzd4F6NCCHQ{WwJF0hOC5yN{mg{txONg>? NYPWSJR7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyPFAzPjFpPkK4NlgxOjZzPD;hQi=>
MM1S NV\ISYZQSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NY\Oc2JpPzJiaILz NUTIXnVKSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNUVFUKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTD0dplx[W5iYnz1[UBmgGOudYPpc44h[XO|YYmsJGlEPTBiPTCxJO69VS5? NVrT[GsxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyPFAzPjFpPkK4NlgxOjZzPD;hQi=>
NB1643 M{O2WpFJXFNiYYPzZZk> MlrvdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE6EMU[0N{Bk\Wyucx?= M2TJdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC MVrxTHRUKGG|c3H5 MmjXdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO= MkmyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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
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 (from reference)

Kinase Assay:

[1]

  • 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]

  • 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.

Animal Research:

[1]

  • 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.)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 524.68
Formula

C27H36N6O3S

CAS No. 936091-26-8
Storage 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

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)

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

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