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 67 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 MkDyRZBweHSxc3nzJGF{e2G7 NYPOeJNmOC53LUKg{txO NIP2eW8yOi12ODDo MkfCSG1UVw>? NVTBcZpocW6mdXPld{BieG:ydH;zbZMhcW5iYn;0bEBld3OnLTDhcoQhfGmvZT2g[IVx\W6mZX70JI1idm6nch?= NU[3Z3Z7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4OlkzOTBpPkK1PFY6OjFyPD;hQi=>
H1650 NUfNUW1vSXCxcITvd4l{KEG|c3H5 NWnSZ|N6OC53LUKg{txO MUWxNk01QCCq NWrnTZZ6TE2VTx?= MV;pcoR2[2W|IHHwc5B1d3OrczDpckBjd3SqIHTvd4UuKGGwZDD0bY1mNSCmZYDlcoRmdnRibXHucoVz NEjmU|Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUi2PVIyOCd-MkW4OlkzOTB:L3G+
H1975 MWPGeY5kfGmxbjDBd5NigQ>? M4jP[VAvOjVvMTFOwG0> MU[yOEBp NHPzXoJFVVOR NWH1RpFDcW6qaXLpeJMh\XiycnXzd4lwdiCxZjDhdI9xfG:|aYOtdoVt[XSnZDDwdo91\WmwIFLjcE1ZVCxiQnPsMVItKHO3co\peolvNCC[SVHQ MnrMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6NkmyNVAoRjJ3OE[5NlExRC:jPh?=
H1650 MXnGeY5kfGmxbjDBd5NigQ>? M4TDWVAvOjVvMTFOwG0> MljINlQhcA>? NYHZbmwxTE2VTx?= M1rzTIlvcGmkaYTzJIV5eHKnc4Ppc44hd2ZiYYDvdJRwe2m|LYLlcIF1\WRicILveIVqdiCEY3ytXGwtKEKlbD2yMEB{fXK4aY\pckwhYEmDUB?= MlfZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6NkmyNVAoRjJ3OE[5NlExRC:jPh?=
H1975 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PVfFEh|ryP Ml;XOFghcA>? NEfrclZFVVOR M2juXZNmdnOrdHn6[ZMh[2WubIOgeI8hfGinIHP5eI91d3irY3n0fUBw\iCncnzveIlvcWJ? M{Owb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OE[5NlExLz5{NUi2PVIyODxxYU6=
H1650 NEPXcXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXLSJoyKM7:TR?= MWe0PEBp NGrJOphFVVOR NFvR[nR{\W6|aYTpfoV{KGOnbHzzJJRwKHSqZTDjfZRwfG:6aXPpeJkhd2ZiZYLsc5Rqdmmk MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh4OUKxNEc,OjV6NkmyNVA9N2F-
CD4+ T MV3GeY5kfGmxbjDBd5NigQ>? M2\sNlAvODFvMTFOwG0> Mmq4OFghcA>? M1PQPGROW09? NVXVTXdOemWmdXPld{B1cGVicHjvd5Bpd3K7bHH0bY9vKGyndnXsd{Bw\iCMQVuyJIFv\CCVVFHUN:Kh NIr5[Wg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUW3NlU{PSd-MkW1O|I2OzV:L3G+
Caco-2  MlHvSpVv[3Srb36gRZN{[Xl? NUPNOYpSOC1zMkCg{txO NXLr[ZlrPyCvaX6= MWLpcohq[mm2czD0bIlidWmwZTD1dJRic2Vid3n0bEBidiCLQ{WwxsBw\iB{LkJCpOK2VQ>? NHXqU4Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC2N|Y4Oid-MkWwOlM3PzJ:L3G+
Caco-2  NFfYV4hHfW6ldHnvckBCe3OjeR?= NHW1SWIyOC93MD:xNFAh|ryP M4K2RVIhcA>? NVnzOmFy\GWlcnXhd4V{KHSqZTDmcJV5KG:oIGuzTH11cGmjbXnu[UBi[3Kxc4OgeIhmKG2xbn;sZZlmeiC5aYToJGlEPTBib3[gOk42yqEQvF2= MlK5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyNkO2O|IoRjJ3ME[zOlczRC:jPh?=
HEK293 MSR  NHLZUmpHfW6ldHnvckBCe3OjeR?= Mnm0NE0yOCEQvF2= NWXjUnVrPyCvaX6= MnjjbY5pcWKrdIOgbHRJXFJ{IIfpeIgh[W5iSVO1NOKhd2ZiMT6yxsDDvU1? NGP1cYI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC2N|Y4Oid-MkWwOlM3PzJ:L3G+
MedB-1 NEnJ[IhHfW6ldHnvckBCe3OjeR?= NGnWS2IyNzJizszN NGjNem0zPCCq MYrk[YNz\WG|ZYOgV3RCXDZicHjvd5Bpd3K7bHH0bY9vKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> Mo\1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7N{e2OlgoRjJ2OUe3OlY5RC:jPh?=
U2940 M4XkemZ2dmO2aX;uJGF{e2G7 MWexM|Ih|ryP MYqyOEBp MnnW[IVkemWjc3XzJHNVSVR4IIDoc5NxcG:{eXzheIlwdiClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl5N{[2PEc,OjR7N{e2Olg9N2F-
K1106 NVOzeWpyTnWwY4Tpc44hSXO|YYm= MoPUNU8zKM7:TR?= M2K5[|I1KGh? MX\k[YNz\WG|ZYOgV3RCXDZicHjvd5Bpd3K7bHH0bY9vKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> NV;RZmpFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5O|c3PjhpPkK0PVc4PjZ6PD;hQi=>
K562 M12yNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHsNE0yKM7:TR?= M{TCN|czKGh? Mnn3bY5pcWKrdIOgT|U3OiClZXzsJJBzd2yrZnXyZZRqd25iYYSgbIlocCClb37j[Y51emG2aX;u M1zDeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2N{e1N|A5Lz5{NEe3OVMxQDxxYU6=
MDA-MB-468  MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnZ[FRFOyEEtV2= NX\WRVdFPDhiaB?= M2rhWYVvcGGwY3XkJJNq[mOuNjDpcoR2[2WmIHzvd5Mhd2ZiY3XscEB3cWGkaXzpeJnDqA>? M3LIZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2Nk[yPFE5Lz5{NE[2NlgyQDxxYU6=
MDA-MB-468 MlzLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX[4OmN7OC12IN88US=> MlH6OFghcA>? NWrZWVljemW|dXz0d{B{cWewaX\pZ4FvfCCub4PzJI9nKH[rYXLpcIl1gSClb33wZZJm\CC2bzDSTU1DWEliYXzvcoU> M3mwTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2Nk[yPFE5Lz5{NE[2NlgyQDxxYU6=
L428 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmqxNE02KM7:TR?= MnTZOFghcA>? NX30T5NscW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZzMEiyO{c,OjR4MUC4Nlc9N2F-
KMH2 MojiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWCwMVUh|ryP MnuzOFghcA>? NUC5XolXcW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> M1\ufFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkGwPFI4Lz5{NE[xNFgzPzxxYU6=
L1236 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWCwMVUh|ryP M2nZWVQ5KGh? M2\NVIlvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZzMEiyO{c,OjR4MUC4Nlc9N2F-
SUPHD1 NVy0RWF7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PocVAuPSEQvF2= MYK0PEBp NYqwdohNcW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> M2C4dVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkGwPFI4Lz5{NE[xNFgzPzxxYU6=
HDLM2 NHvsXpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY[wMVUh|ryP M3HYTlQ5KGh? M2fSSolvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= MoTxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4MUC4NlcoRjJ2NkGwPFI4RC:jPh?=
K1106P NUTiXXhuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofzNE02KM7:TR?= MorzOFghcA>? MYTpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 NUHrU|FyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2NVA5OjdpPkK0OlExQDJ5PD;hQi=>
L428 M1m0[GFxd3C2b4Ppd{BCe3OjeR?= NGjBR5UxNzBwNkK1M|EvOjVizszN MlLqOFghcA>? NUPjR2l7cW6mdXPld{B1cGViYYDvdJRwe2m|wrC= NWrMVIVZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2NVA5OjdpPkK0OlExQDJ5PD;hQi=>
KMH2 M4DhSmFxd3C2b4Ppd{BCe3OjeR?= M4TrNVAwOC54MkWvNU4zPSEQvF2= M1PLUVQ5KGh? M4DDUIlv\HWlZYOgeIhmKGGyb4D0c5Nqe8Li MnntQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4MUC4NlcoRjJ2NkGwPFI4RC:jPh?=
L1236 M4X3fWFxd3C2b4Ppd{BCe3OjeR?= NGPJb|gxNzBwNkK1M|EvOjVizszN M4HZflQ5KGh? NFLxUHFqdmS3Y3XzJJRp\SCjcH;weI9{cXQEoB?= Mny2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4MUC4NlcoRjJ2NkGwPFI4RC:jPh?=
SUPHD1 M{L2cWFxd3C2b4Ppd{BCe3OjeR?= MlfQNE8xNjZ{NT:xMlI2KM7:TR?= MW[0PEBp M33NRYlv\HWlZYOgeIhmKGGyb4D0c5Nqe8Li Mk\0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4MUC4NlcoRjJ2NkGwPFI4RC:jPh?=
HDLM2 NF7Lb3pCeG:ydH;zbZMhSXO|YYm= NEDTOpUxNzBwNkK1M|EvOjVizszN NUfqZZBYPDhiaB?= NWDmd291cW6mdXPld{B1cGViYYDvdJRwe2m|wrC= MlflQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4MUC4NlcoRjJ2NkGwPFI4RC:jPh?=
K1106P M4fMcmFxd3C2b4Ppd{BCe3OjeR?= MYiwM|AvPjJ3L{GuNlUh|ryP MkPQOFghcA>? NGjYc5RqdmS3Y3XzJJRp\SCjcH;weI9{cXQEoB?= MonCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4MUC4NlcoRjJ2NkGwPFI4RC:jPh?=
L428 Mn3jSpVv[3Srb36gRZN{[Xl? MmjQNE02KM7:TR?= M1f6eFI1KGh? M4PoZYlvcGmkaYTzJGpCUzJxU2TBWEB{cWewYXzpcoc> NY\LSlNZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2NVA5OjdpPkK0OlExQDJ5PD;hQi=>
KMH2 MkDUSpVv[3Srb36gRZN{[Xl? MV6wMVUh|ryP MXeyOEBp MoC5bY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZzMEiyO{c,OjR4MUC4Nlc9N2F-
L1236 M4XLNWZ2dmO2aX;uJGF{e2G7 NVzOeZNFOC13IN88US=> MVuyOEBp MlWwbY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> MoPrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4MUC4NlcoRjJ2NkGwPFI4RC:jPh?=
SUPHD1 MmDHSpVv[3Srb36gRZN{[Xl? MWqwMVUh|ryP MVKyOEBp NVHkeY1XcW6qaXLpeJMhUkGNMj;TWGFVKHOrZ37hcIlv\w>? M1L5cFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkGwPFI4Lz5{NE[xNFgzPzxxYU6=
HDLM2 MX3GeY5kfGmxbjDBd5NigQ>? M1;ocVAuPSEQvF2= MYOyOEBp MVLpcohq[mm2czDKRWszN1OWQWSgd4lodmGuaX7n NX;aOVB2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2NVA5OjdpPkK0OlExQDJ5PD;hQi=>
K1106P NHnVRYpHfW6ldHnvckBCe3OjeR?= NEjaPZAxNTVizszN MmjYNlQhcA>? M4LrdIlvcGmkaYTzJGpCUzJxU2TBWEB{cWewYXzpcoc> MnvQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4MUC4NlcoRjJ2NkGwPFI4RC:jPh?=
MM.1S  M1HMWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHxXIZZUUN3ME2xMVMh|ryP NHT0eXg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW4OFExOSd-MkS1PFQyODF:L3G+
TpoR JAK2 WT NVrZRXVxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;nWmlEPTB;MT60JEgyNjQkgKOxMlUqKM7:TR?= NH34TJI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEK1NVc6OCd-MkSyOVE4QTB:L3G+
TpoR JAK2 V617F MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTBwODCoNE446oDVMD65LUDPxE1? M3HVUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MkWxO|kxLz5{NEK1NVc6ODxxYU6=
TpoR W515L M4j5b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{TEW2lEPTB;MD64JEgxNjgkgKOxMlAqKM7:TR?= MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJ3MUe5NEc,OjR{NUG3PVA9N2F-
Bcr-abl M3HiRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHtTWM2OD1{LkegLFIvOuLCk{OuN{kh|ryP Mn7PQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR{NUG3PVAoRjJ2MkWxO|kxRC:jPh?=
JAK2 TW NVzDZ|FOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MluwTWM2OD1zLkigLFEvPeLCk{KuN{kh|ryP Mn7SQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR{NUG3PVAoRjJ2MkWxO|kxRC:jPh?=
JAK2 V617F NHLpdnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHYeXhKSzVyPUCuOkApOC544pETNE44MSEQvF2= MmGyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR{NUG3PVAoRjJ2MkWxO|kxRC:jPh?=
MedB-1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXK0cHY1PCEQvF2= M4TOSFI1NzR6L{eyJIg> MVLEUXNQ M3vsUIlvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> Mnn1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6NUKzOlYoRjJ|OEWyN|Y3RC:jPh?=
K1106 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYXaWHhjPCEQvF2= NWryVHVGOjRxNEivO|IhcA>? Mn\ZSG1UVw>? NFiwbFJqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 NI\C[5g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i1NlM3Pid-MkO4OVI{PjZ:L3G+
U2940 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfp[Y81KM7:TR?= M{\oZVI1NzR6L{eyJIg> MXTEUXNQ M1:ySYlvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh3MkO2Okc,OjN6NUKzOlY9N2F-
FE-PD NX\yS41ST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4TxTVAvODZ|LUSg{txO NHHJSm9KSzVyPUmuOUDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= NITaWnE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O3NlY3QSd-MkOzO|I3Pjl:L3G+
HEL NXfKN2F6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTSNE4xPjNvNDFOwG0> M3XKfWlEPTB;MT61JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= MlfXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|N{K2OlkoRjJ|M{eyOlY6RC:jPh?=
K-562 MkH6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrQNE4xPjNvNDFOwG0> MXPJR|UxRTJwNTFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? MmjnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|N{K2OlkoRjJ|M{eyOlY6RC:jPh?=
L-82 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jBN|AvODZ|LUSg{txO NFHaeI5KSzVyPUCuPVgh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MlPOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|N{K2OlkoRjJ|M{eyOlY6RC:jPh?=
MAC-1 M1LFRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXDNE4xPjNvNDFOwG0> MVLJR|UxRTBwNUKg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN5Mk[2PUc,OjN|N{K2Olk9N2F-
MAC-2A MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnyUIsxNjB4Mz20JO69VQ>? MU\JR|UxRTBwNkmg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN5Mk[2PUc,OjN|N{K2Olk9N2F-
MAC-2B NGXVfnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LH[FAvODZ|LUSg{txO NFjVTHlKSzVyPUCuOVQh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MmPlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|N{K2OlkoRjJ|M{eyOlY6RC:jPh?=
MY-LA M2DjT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vnc|AvODZ|LUSg{txO Ml;lTWM2OD1{LkGg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 NEf6fmo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O3NlY3QSd-MkOzO|I3Pjl:L3G+
NC-NC M2fHO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVqwMlA3Oy12IN88US=> MUjJR|UxRTFwMDFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? NFLSTGE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O3NlY3QSd-MkOzO|I3Pjl:L3G+
SE-AX MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnoO45HOC5yNkOtOEDPxE1? MnvQTWM2OD1zLkWg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 M2nTOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{eyOlY6Lz5{M{O3NlY3QTxxYU6=
SR-786 M376OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\PUpoxNjB4Mz20JO69VQ>? M1rJWGlEPTB;ND62JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= M1WydVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{eyOlY6Lz5{M{O3NlY3QTxxYU6=
M-MOK  NVvGUGtUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnDSGVtOjViwsXNxsA> MVmyOE81QC95MjDo MnraSG1UVw>? MoC1bY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> NW\1UXdyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG4OVMyPTdpPkKxPFU{OTV5PD;hQi=>
HEL NUjhN2hGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPGWnk1UUN3ME2zNFUhdk1? NU\qbIk4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUizPVQ2PTRpPkG4N|k1PTV2PD;hQi=>
Ba/F3 JAK2V617F NULQPXFsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XHVGlEPTB;MkewJI5O MoTzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh|OUS1OVQoRjF6M{m0OVU1RC:jPh?=
MV4-11 M1;RPGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MVe3NkBpenN? MXHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2YND2xNUBk\WyuczDh[pRmeiB5MjDodpMh[nliY3XscJRqfGW{LXLseYUh[XO|YYmsJGVEPTBiPTCwMlA4QSEQvF2u NXP3bmxtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyPFAzPjFpPkK4NlgxOjZzPD;hQi=>
MM1S Ml7uRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NIe3O444OiCqcoO= NUfQRWVXSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNUVFUKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTD0dplx[W5iYnz1[UBmgGOudYPpc44h[XO|YYmsJGlEPTBiPTCxJO69VS5? M4TL[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MkiwNlYyLz5{OEK4NFI3OTxxYU6=
NB1643 NWjCfWZLeUiWUzDhd5NigQ>? NX\KbGdMeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CNVY1OyClZXzsdy=> NGf2PJM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SK-N-MC NVfkeIVqeUiWUzDhd5NigQ>? NVq3W5BReUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uVUNiY3XscJM> NHOwVlc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
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

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

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 Not yet recruiting 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 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 --

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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