Fedratinib (TG101348)

For research use only.

Catalog No.S2736 Synonyms: SAR302503

40 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 with IC50 of 15 nM and 48 nM, respectively. Fedratinib has potential antineoplastic activity. Fedratinib inhibits proliferation and induces apoptosis. Phase 2.

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Selleck's Fedratinib (TG101348) has been cited by 40 publications

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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 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 NWW3eFFFSXCxcITvd4l{KEG|c3H5 MkDPNE42NTJizszN NF3MdZIyOi12ODDo NIW0dJhFVVOR MVnpcoR2[2W|IHHwc5B1d3OrczDpckBjd3SqIHTvd4UuKGGwZDD0bY1mNSCmZYDlcoRmdnRibXHucoVz NWnJUmt6OjV6NkmyNVA>
H1650 NHLTbFJCeG:ydH;zbZMhSXO|YYm= M2LRR|AvPS1{IN88US=> MXexNk01QCCq M1nq[GROW09? NUe3dlRncW6mdXPld{BieG:ydH;zbZMhcW5iYn;0bEBld3OnLTDhcoQhfGmvZT2g[IVx\W6mZX70JI1idm6nch?= M3fLOFI2QDZ7MkGw
H1975 NYO4c4p{TnWwY4Tpc44hSXO|YYm= M3viVFAvOjVvMTFOwG0> M2Hs[VI1KGh? MoS4SG1UVw>? MXvpcohq[mm2czDlfJBz\XO|aX;uJI9nKGGyb4D0c5Nqey2{ZXzheIVlKHC{b4TlbY4hSmOuLWjMMEBD[2xvMjygd5Vzfmm4aX6sJHhKSVB? NGLrWoQzPTh4OUKxNC=>
H1650 NVnDU3RHTnWwY4Tpc44hSXO|YYm= NHfqZVUxNjJ3LUGg{txO MmLPNlQhcA>? MVLEUXNQ Mle5bY5pcWKrdIOg[ZhxemW|c3nvckBw\iCjcH;weI9{cXNvcnXsZZRm\CCycn;0[YlvKEKlbD3YUEwhSmOuLUKsJJN2en[rdnnuMEBZUUGS MkXNNlU5Pjl{MUC=
H1975 NHS0[3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnzfIYyKM7:TR?= MXG0PEBp MYrEUXNQ Mn7ud4Vve2m2aYrld{Bk\WyuczD0c{B1cGViY4n0c5RwgGmlaYT5JI9nKGW{bH;0bY5q[g>? MWmyOVg3QTJzMB?=
H1650 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYr1doVOOSEQvF2= MmfJOFghcA>? M1\DVGROW09? MnPsd4Vve2m2aYrld{Bk\WyuczD0c{B1cGViY4n0c5RwgGmlaYT5JI9nKGW{bH;0bY5q[g>? NETPcpIzPTh4OUKxNC=>
CD4+ T M1rWd2Z2dmO2aX;uJGF{e2G7 NF;3UHoxNjBzLUGg{txO NXHUNm5bPDhiaB?= NU\qSWRiTE2VTx?= Mlr2doVlfWOnczD0bIUheGixc4Doc5J6dGG2aX;uJIxmfmWuczDv[kBLSUt{IHHu[EBUXEGWM9Mg Ml[4NlU2PzJ3M{W=
Caco-2  M4DFdWZ2dmO2aX;uJGF{e2G7 M{HtVFAuOTJyIN88US=> NV;IZY5QPyCvaX6= M4T5UIlvcGmkaYTzJJRpcWGvaX7lJJVxfGGtZTD3bZRpKGGwIFnDOVDDqG:oIEKuNeKhyrWP NWqySWRtOjVyNkO2O|I>
Caco-2  NUjTW29[TnWwY4Tpc44hSXO|YYm= NXjmc3hwOTBxNUCvNVAxKM7:TR?= MWiyJIg> NGPLSGZl\WO{ZXHz[ZMhfGinIH\seZghd2ZiW{PIYZRpcWGvaX7lJIFkem:|czD0bIUhdW:wb3zhfYVzKHerdHigTWM2OCCxZjC2MlXDqM7:TR?= NEXGN5ozPTB4M{[3Ni=>
HEK293 MSR  MVHGeY5kfGmxbjDBd5NigQ>? M33ScFAuOTBizszN MnzGO{BucW5? Ml;ObY5pcWKrdIOgbHRJXFJ{IIfpeIgh[W5iSVO1NOKhd2ZiMT6yxsDDvU1? M4PWbVI2ODZ|Nkey
MedB-1 MYLGeY5kfGmxbjDBd5NigQ>? MnzWNU8zKM7:TR?= MljaNlQhcA>? MVnk[YNz\WG|ZYOgV3RCXDZicHjvd5Bpd3K7bHH0bY9vKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> M2XRNFI1QTd5Nk[4
U2940 NHrtUIpHfW6ldHnvckBCe3OjeR?= NWHrNIZGOS9{IN88US=> NWDSd44yOjRiaB?= MkDp[IVkemWjc3XzJHNVSVR4IIDoc5NxcG:{eXzheIlwdiClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 MUOyOFk4PzZ4OB?=
K1106 M{DOSmZ2dmO2aX;uJGF{e2G7 MWqxM|Ih|ryP M1ra[lI1KGh? MonC[IVkemWjc3XzJHNVSVR4IIDoc5NxcG:{eXzheIlwdiClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 MlO2NlQ6Pzd4Nki=
K562 NWfwXoxrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUiwMVEh|ryP MlHjO|IhcA>? M1i0eolvcGmkaYTzJGs2PjJiY3XscEBxem:uaX\ldoF1cW:wIHH0JIhq\2hiY3;uZ4VvfHKjdHnvci=> M2Wz[|I1Pzd3M{C4
MDA-MB-468  NYrXRXloT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTzS5JmOyEEtV2= M2jWOVQ5KGh? M{DhRYVvcGGwY3XkJJNq[mOuNjDpcoR2[2WmIHzvd5Mhd2ZiY3XscEB3cWGkaXzpeJnDqA>? NXKwV|UzOjR4NkK4NVg>
MDA-MB-468 MmC5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTPOFgxNTRizszN NW\YdJhkPDhiaB?= NV3nWGVKemW|dXz0d{B{cWewaX\pZ4FvfCCub4PzJI9nKH[rYXLpcIl1gSClb33wZZJm\CC2bzDSTU1DWEliYXzvcoU> MmnlNlQ3PjJ6MUi=
L428 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlrXNE02KM7:TR?= NWK4UplVPDhiaB?= MVrpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 Mk\rNlQ3OTB6Mke=
KMH2 M1vvZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTpc4cxNTVizszN MlLhOFghcA>? NIG3VlNqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 NHPod5EzPDZzMEiyOy=>
L1236 NWDrOXJ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1L0TVAuPSEQvF2= Mkj4OFghcA>? MYXpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 NGS2T4ozPDZzMEiyOy=>
SUPHD1 NIezSIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17pTFAuPSEQvF2= M3nrbVQ5KGh? NUS5ZWh4cW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> NFz1WFczPDZzMEiyOy=>
HDLM2 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXqOHlPOC13IN88US=> M1HoeVQ5KGh? NVzJbI0ycW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> NGfCVZMzPDZzMEiyOy=>
K1106P MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\vcIFROC13IN88US=> NVHYPZJbPDhiaB?= NI[5SIdqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 MojhNlQ3OTB6Mke=
L428 MVnBdI9xfG:|aYOgRZN{[Xl? MlPZNE8xNjZ{NT:xMlI2KM7:TR?= MV[0PEBp NYfu[VR7cW6mdXPld{B1cGViYYDvdJRwe2m|wrC= M2HzOFI1PjFyOEK3
KMH2 MlnvRZBweHSxc3nzJGF{e2G7 M3PKdFAwOC54MkWvNU4zPSEQvF2= M2rLVlQ5KGh? NFnKcohqdmS3Y3XzJJRp\SCjcH;weI9{cXQEoB?= MUGyOFYyODh{Nx?=
L1236 MY\BdI9xfG:|aYOgRZN{[Xl? MkTUNE8xNjZ{NT:xMlI2KM7:TR?= M4HJVVQ5KGh? MlL2bY5lfWOnczD0bIUh[XCxcITvd4l{yqB? NESyRnYzPDZzMEiyOy=>
SUPHD1 NWnQSmpCSXCxcITvd4l{KEG|c3H5 MUSwM|AvPjJ3L{GuNlUh|ryP NYfjeFdQPDhiaB?= NGLuZ|dqdmS3Y3XzJJRp\SCjcH;weI9{cXQEoB?= NEnRU3czPDZzMEiyOy=>
HDLM2 M{LYbmFxd3C2b4Ppd{BCe3OjeR?= MmDHNE8xNjZ{NT:xMlI2KM7:TR?= NXzPNmhjPDhiaB?= MWTpcoR2[2W|IITo[UBieG:ydH;zbZPDqA>? M{DMWlI1PjFyOEK3
K1106P NYDJVJVwSXCxcITvd4l{KEG|c3H5 M{nTelAwOC54MkWvNU4zPSEQvF2= M13HOFQ5KGh? MkC2bY5lfWOnczD0bIUh[XCxcITvd4l{yqB? MUOyOFYyODh{Nx?=
L428 NVr3bJlnTnWwY4Tpc44hSXO|YYm= M1;CSlAuPSEQvF2= M3X0eFI1KGh? MnS2bY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> M{DER|I1PjFyOEK3
KMH2 MlXvSpVv[3Srb36gRZN{[Xl? MVuwMVUh|ryP MWWyOEBp M2CxfIlvcGmkaYTzJGpCUzJxU2TBWEB{cWewYXzpcoc> MmDCNlQ3OTB6Mke=
L1236 MnjESpVv[3Srb36gRZN{[Xl? M3rKTVAuPSEQvF2= M1jSTVI1KGh? NV;tNmpHcW6qaXLpeJMhUkGNMj;TWGFVKHOrZ37hcIlv\w>? M4LtRlI1PjFyOEK3
SUPHD1 M3jPbWZ2dmO2aX;uJGF{e2G7 MXywMVUh|ryP MoHWNlQhcA>? Mo\MbY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> M3LGUFI1PjFyOEK3
HDLM2 MmPESpVv[3Srb36gRZN{[Xl? MofXNE02KM7:TR?= MWOyOEBp NH;TbHNqdmirYnn0d{BLSUt{L2PURXQhe2mpbnHsbY5o NWPBO2xFOjR4MUC4Nlc>
K1106P MnPmSpVv[3Srb36gRZN{[Xl? MmPkNE02KM7:TR?= MkPrNlQhcA>? MUDpcohq[mm2czDKRWszN1OWQWSgd4lodmGuaX7n MlrsNlQ3OTB6Mke=
MM.1S  NH\zfmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTFvMzFOwG0> MnjONlQ2QDRzMEG=
TpoR JAK2 WT MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrXZnRnUUN3ME2xMlQhMDFwM,MAl|EvPSlizszN NFTse2IzPDJ3MUe5NC=>
TpoR JAK2 V617F M{HlXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7mOWFKSzVyPUCuPEApOC554pETNE46MSEQvF2= NHz1PWczPDJ3MUe5NC=>
TpoR W515L M3PRbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnNR5RFUUN3ME2wMlghMDBwN,MAl|EvOClizszN MWeyOFI2OTd7MB?=
Bcr-abl M2r1UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTJwNzCoNk4z6oDVMz6zLUDPxE1? MoXZNlQzPTF5OUC=
JAK2 TW MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFfQXlJKSzVyPUGuPEApOS534pETNk4{MSEQvF2= NFvH[3QzPDJ3MUe5NC=>
JAK2 V617F MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\TTY5SUUN3ME2wMlYhMDBwNvMAl|AvPylizszN MV2yOFI2OTd7MB?=
MedB-1 M1PpOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUm0JO69VQ>? MYOyOE81QC95MjDo NIr6e5VFVVOR M4\KSYlvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> NXrRNJplOjN6NUKzOlY>
K1106 M{CxfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rFS|Qh|ryP NFnFcmQzPC92OD:3NkBp MVzEUXNQ M1XnT4lvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> M1LaeFI{QDV{M{[2
U2940 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnTGOEDPxE1? NUDkVJlYOjRxNEivO|IhcA>? M2rxU2ROW09? M2LGZYlvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> NIr0VHQzOzh3MkO2Oi=>
FE-PD MoWwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXZNWRuOC5yNkOtOEDPxE1? NVPZWII2UUN3ME25MlUh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NUjqPFNDOjN|N{K2Olk>
HEL NYrJflVtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\pOFAvODZ|LUSg{txO MVvJR|UxRTFwNTFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? NWHZTYFHOjN|N{K2Olk>
K-562 M{jp[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XBXFAvODZ|LUSg{txO NGXiT|RKSzVyPUKuOUDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= MnTCNlM{PzJ4Nkm=
L-82 M3jL[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TI[FAvODZ|LUSg{txO NULRbZB5UUN3ME2wMlk5KM7:TTygbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NGnXelUzOzN5Mk[2PS=>
MAC-1 NXO3bpVsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nsZ|AvODZ|LUSg{txO M{fvd2lEPTB;MD61NkDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= MkO3NlM{PzJ4Nkm=
MAC-2A M4roRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3xcmcxNjB4Mz20JO69VQ>? NV\XblVOUUN3ME2wMlY6KM7:TTygbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MXuyN|M4OjZ4OR?=
MAC-2B MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\mNE4xPjNvNDFOwG0> M4PmPWlEPTB;MD61OEDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= MV:yN|M4OjZ4OR?=
MY-LA MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrV[pExNjB4Mz20JO69VQ>? NX31TY9oUUN3ME2yMlEh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 M33HWlI{Ozd{Nk[5
NC-NC NVLifZlPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\lN|AvODZ|LUSg{txO NX;LfVM2UUN3ME2xMlAh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 M{LKT|I{Ozd{Nk[5
SE-AX NUXPSm9RT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVKwMlA3Oy12IN88US=> NIqyVJVKSzVyPUGuOUDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= M4W2PVI{Ozd{Nk[5
SR-786 MljNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvBXIMxNjB4Mz20JO69VQ>? NIXOZmpKSzVyPUSuOkDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= M3PvblI{Ozd{Nk[5
M-MOK  MlzlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmnENlUhyrWPwrC= MXWyOE81QC95MjDo MX;EUXNQ M2TmNIlvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> M{XZOVIyQDV|MUW3
HEL NFK1TmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPhbXdsUUN3ME2zNFUhdk1? M{TJc|E5Ozl2NUW0
Ba/F3 JAK2V617F NV7Cc3ZGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjqNWpKSzVyPUK3NEBvVQ>? M2jOZ|E5Ozl2NUW0

... 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:

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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 ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

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 MSDS / 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 MSDS / 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
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 Unknown status 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
NCT01523171 Completed Drug: SAR302503 Hematopoietic Neoplasm Sanofi April 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