Fedratinib (TG101348)

For research use only. Not for use in humans.

Catalog No.S2736 Synonyms: SAR302503

29 publications

Fedratinib (TG101348) Chemical Structure

Molecular Weight(MW): 524.68

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. Phase 2.

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Selleck's Fedratinib (TG101348) has been cited by 29 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. 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 NHnQdWJCeG:ydH;zbZMhSXO|YYm= NYThNHByOC53LUKg{txO NVLKcVBtOTJvNEigbC=> MmDrSG1UVw>? MVHpcoR2[2W|IHHwc5B1d3OrczDpckBjd3SqIHTvd4UuKGGwZDD0bY1mNSCmZYDlcoRmdnRibXHucoVz M4juPVI2QDZ7MkGw
H1650 NUnxXZRzSXCxcITvd4l{KEG|c3H5 MXmwMlUuOiEQvF2= M{XHb|EzNTR6IHi= MnzLSG1UVw>? NV;PT5RFcW6mdXPld{BieG:ydH;zbZMhcW5iYn;0bEBld3OnLTDhcoQhfGmvZT2g[IVx\W6mZX70JI1idm6nch?= MVOyOVg3QTJzMB?=
H1975 NGD4PFZHfW6ldHnvckBCe3OjeR?= NY\tb2NZOC5{NT2xJO69VQ>? MUKyOEBp NG\4d5JFVVOR MnXrbY5pcWKrdIOg[ZhxemW|c3nvckBw\iCjcH;weI9{cXNvcnXsZZRm\CCycn;0[YlvKEKlbD3YUEwhSmOuLUKsJJN2en[rdnnuMEBZUUGS M1zhcVI2QDZ7MkGw
H1650 M2HZTWZ2dmO2aX;uJGF{e2G7 NVf2S5dqOC5{NT2xJO69VQ>? MnvmNlQhcA>? M3W0V2ROW09? NEPyU4JqdmirYnn0d{BmgHC{ZYPzbY9vKG:oIHHwc5B1d3Orcz3y[YxifGWmIIDyc5RmcW5iQnPsMXhNNCCEY3ytNkwhe3W{dnn2bY4tKFiLQWC= M4fBUlI2QDZ7MkGw
H1975 M3znZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPDTJVEOSEQvF2= MXO0PEBp NHLteZZFVVOR NEPQOWp{\W6|aYTpfoV{KGOnbHzzJJRwKHSqZTDjfZRwfG:6aXPpeJkhd2ZiZYLsc5Rqdmmk MUiyOVg3QTJzMB?=
H1650 M3O2cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkWzNUDPxE1? NV7yUIw5PDhiaB?= NWLUV3dUTE2VTx?= NF7QNZh{\W6|aYTpfoV{KGOnbHzzJJRwKHSqZTDjfZRwfG:6aXPpeJkhd2ZiZYLsc5Rqdmmk MmTHNlU5Pjl{MUC=
CD4+ T MkXUSpVv[3Srb36gRZN{[Xl? NVHDV4F1OC5yMT2xJO69VQ>? NYjzbJZOPDhiaB?= NYXKVXh2TE2VTx?= Mn\odoVlfWOnczD0bIUheGixc4Doc5J6dGG2aX;uJIxmfmWuczDv[kBLSUt{IHHu[EBUXEGWM9Mg MnzNNlU2PzJ3M{W=
Caco-2  MUPGeY5kfGmxbjDBd5NigQ>? NFjpfZMxNTF{MDFOwG0> MVy3JI1qdg>? NWTtO3VKcW6qaXLpeJMhfGirYX3pcoUhfXC2YXvlJJdqfGhiYX6gTWM2OMLib3[gNk4yyqEEtV2= M3\IflI2ODZ|Nkey
Caco-2  NF7SXGNHfW6ldHnvckBCe3OjeR?= MnOwNVAwPTBxMUCwJO69VQ>? MnjuNkBp MVXk[YNz\WG|ZYOgeIhmKG[udYigc4YhYzOKXYTobYFucW6nIHHjdo9{eyC2aHWgcY9vd2yjeXXyJJdqfGhiSVO1NEBw\iB4LkZCpO69VQ>? NITrWJozPTB4M{[3Ni=>
HEK293 MSR  MWXGeY5kfGmxbjDBd5NigQ>? NFfUXlIxNTFyIN88US=> M1TOXFchdWmw MkDCbY5pcWKrdIOgbHRJXFJ{IIfpeIgh[W5iSVO1NOKhd2ZiMT6yxsDDvU1? MV2yOVA3OzZ5Mh?=
MedB-1 NH;KcpJHfW6ldHnvckBCe3OjeR?= MYqxM|Ih|ryP NH[5WmIzPCCq NVy4foQz\GWlcnXhd4V{KFOWQWS2JJBpd3OyaH;yfYxifGmxbjDjc45k\W62cnH0bY9vKGSncHXu[IVvfGy7 NHj1V5kzPDl5N{[2PC=>
U2940 MnLhSpVv[3Srb36gRZN{[Xl? M{PEW|EwOiEQvF2= Ml20NlQhcA>? M3W0foRm[3KnYYPld{BUXEGWNjDwbI9{eGixconsZZRqd25iY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? NX:ycIFDOjR7N{e2Olg>
K1106 M3\Zb2Z2dmO2aX;uJGF{e2G7 MV[xM|Ih|ryP NGXrVJAzPCCq MkK1[IVkemWjc3XzJHNVSVR4IIDoc5NxcG:{eXzheIlwdiClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 MYeyOFk4PzZ4OB?=
K562 NGKyUmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfGNo5zOC1zIN88US=> NGW1XZc4OiCq NY\1N5l5cW6qaXLpeJMhUzV4MjDj[YxtKHC{b3zp[oVz[XSrb36gZZQhcGmpaDDjc45k\W62cnH0bY9v NFLXSZQzPDd5NUOwPC=>
MDA-MB-468  NWPDcVhiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVizJOK2VQ>? M2LZdVQ5KGh? NVG2RoJR\W6qYX7j[YQhe2mkY3y2JIlv\HWlZXSgcI9{eyCxZjDj[YxtKH[rYXLpcIl1gcLi NGPMNHkzPDZ4MkixPC=>
MDA-MB-468 NIXLeIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGexSHQxNTRizszN M2PWeVQ5KGh? M3zKcJJme3WudIOgd4lodmmoaXPhcpQhdG:|czDv[kB3cWGkaXzpeJkh[2:vcHHy[YQhfG9iUlmtRnBKKGGub37l NHW2dlkzPDZ4MkixPC=>
L428 NX;HUnZOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYmwMVUh|ryP Ml3LOFghcA>? NUPsOWZxcW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> M1m3dFI1PjFyOEK3
KMH2 NXTYdop7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLC[YNPOC13IN88US=> MnH1OFghcA>? NEjXNmhqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 NXfvT4tDOjR4MUC4Nlc>
L1236 MljDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYKwMVUh|ryP M3PNb|Q5KGh? M1fPeolvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= MnX4NlQ3OTB6Mke=
SUPHD1 NFiz[IhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLmNE02KM7:TR?= MkO2OFghcA>? MV3pcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 MkHRNlQ3OTB6Mke=
HDLM2 MnezS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoX3NE02KM7:TR?= M2LpO|Q5KGh? MVLpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 NXLFUoU2OjR4MUC4Nlc>
K1106P NFe3c5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV6wMVUh|ryP NF\2e4U1QCCq MV;pcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 NH3ReXAzPDZzMEiyOy=>
L428 MkDBRZBweHSxc3nzJGF{e2G7 NYnuTJJ[OC9yLk[yOU8yNjJ3IN88US=> NUXDWJhbPDhiaB?= NUPU[m82cW6mdXPld{B1cGViYYDvdJRwe2m|wrC= MW[yOFYyODh{Nx?=
KMH2 M1;1NGFxd3C2b4Ppd{BCe3OjeR?= MnTyNE8xNjZ{NT:xMlI2KM7:TR?= M3qxPFQ5KGh? M4jxd4lv\HWlZYOgeIhmKGGyb4D0c5Nqe8Li NVLBUpJ3OjR4MUC4Nlc>
L1236 MV7BdI9xfG:|aYOgRZN{[Xl? NIHFRXAxNzBwNkK1M|EvOjVizszN MY[0PEBp NGqwfJhqdmS3Y3XzJJRp\SCjcH;weI9{cXQEoB?= MWKyOFYyODh{Nx?=
SUPHD1 NXjEcZYxSXCxcITvd4l{KEG|c3H5 MX6wM|AvPjJ3L{GuNlUh|ryP MXi0PEBp MlHEbY5lfWOnczD0bIUh[XCxcITvd4l{yqB? M4jyO|I1PjFyOEK3
HDLM2 NITSWJJCeG:ydH;zbZMhSXO|YYm= M1\XPFAwOC54MkWvNU4zPSEQvF2= NEX3Zm81QCCq MYrpcoR2[2W|IITo[UBieG:ydH;zbZPDqA>? M1LDUlI1PjFyOEK3
K1106P M1q5[WFxd3C2b4Ppd{BCe3OjeR?= MUiwM|AvPjJ3L{GuNlUh|ryP NHXzZ|k1QCCq NXjWXJdrcW6mdXPld{B1cGViYYDvdJRwe2m|wrC= NE\rV2gzPDZzMEiyOy=>
L428 MljuSpVv[3Srb36gRZN{[Xl? MYOwMVUh|ryP NGDoXpEzPCCq MWTpcohq[mm2czDKRWszN1OWQWSgd4lodmGuaX7n MoLSNlQ3OTB6Mke=
KMH2 MmfZSpVv[3Srb36gRZN{[Xl? NF3NW2wxNTVizszN MoXWNlQhcA>? MUPpcohq[mm2czDKRWszN1OWQWSgd4lodmGuaX7n MniwNlQ3OTB6Mke=
L1236 NGXZdlNHfW6ldHnvckBCe3OjeR?= M4\CTVAuPSEQvF2= M4[1ZlI1KGh? M3S1UIlvcGmkaYTzJGpCUzJxU2TBWEB{cWewYXzpcoc> Mn3TNlQ3OTB6Mke=
SUPHD1 NXjBdmRHTnWwY4Tpc44hSXO|YYm= NH7lWFMxNTVizszN NXqzVmo5OjRiaB?= Mn7ybY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> M{HJe|I1PjFyOEK3
HDLM2 M1LxXmZ2dmO2aX;uJGF{e2G7 MnzoNE02KM7:TR?= M1;LfFI1KGh? NHHzVoZqdmirYnn0d{BLSUt{L2PURXQhe2mpbnHsbY5o MV:yOFYyODh{Nx?=
K1106P NHy0N3BHfW6ldHnvckBCe3OjeR?= MoKwNE02KM7:TR?= MVyyOEBp NY\zRpYzcW6qaXLpeJMhUkGNMj;TWGFVKHOrZ37hcIlv\w>? NYjqcolxOjR4MUC4Nlc>
MM.1S  MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXy0VWtvUUN3ME2xMVMh|ryP Mnf3NlQ2QDRzMEG=
TpoR JAK2 WT MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXmNFVKSzVyPUGuOEApOS5|4pETNU42MSEQvF2= Mkf6NlQzPTF5OUC=
TpoR JAK2 V617F MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3z6b2lEPTB;MD64JEgxNjgkgKOwMlkqKM7:TR?= M3HpXFI1OjVzN{mw
TpoR W515L MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7URVZKSzVyPUCuPEApOC554pETNU4xMSEQvF2= NHm1ZoszPDJ3MUe5NC=>
Bcr-abl NIPudHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrNZ3lxUUN3ME2yMlchMDJwMvMAl|MvOylizszN NXfJWm1bOjR{NUG3PVA>
JAK2 TW NEXNd5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjaeXplUUN3ME2xMlghMDFwNfMAl|IvOylizszN NGjp[XMzPDJ3MUe5NC=>
JAK2 V617F M2XXNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjkb21KSzVyPUCuOkApOC544pETNE44MSEQvF2= MV[yOFI2OTd7MB?=
MedB-1 MkDJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXpVpdoPCEQvF2= MY[yOE81QC95MjDo NX[3bYx{TE2VTx?= MWDpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 MVuyN|g2OjN4Nh?=
K1106 Mmr0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\OXnM1KM7:TR?= MofjNlQwPDhxN{KgbC=> NVXwW4diTE2VTx?= NUXjdVBvcW6qaXLpeJMh[2WubDDndo94fGhidHnt[UBl\XCnbnTlcpRtgQ>? MXiyN|g2OjN4Nh?=
U2940 NFvaN5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYm0JO69VQ>? NXrSNmdVOjRxNEivO|IhcA>? NIn1R3BFVVOR NWqwb2E2cW6qaXLpeJMh[2WubDDndo94fGhidHnt[UBl\XCnbnTlcpRtgQ>? M1LMNVI{QDV{M{[2
FE-PD M13pUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVGwMlA3Oy12IN88US=> MX\JR|UxRTlwNTFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? NXHPcW41OjN|N{K2Olk>
HEL MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rCdlAvODZ|LUSg{txO MmTFTWM2OD1zLkWg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 MX[yN|M4OjZ4OR?=
K-562 NInIVmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV[wMlA3Oy12IN88US=> NXjCR3F[UUN3ME2yMlUh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 M3i0WlI{Ozd{Nk[5
L-82 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPaNE4xPjNvNDFOwG0> M4jjeGlEPTB;MD65PEDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= MXmyN|M4OjZ4OR?=
MAC-1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HYUlAvODZ|LUSg{txO M33iN2lEPTB;MD61NkDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= MXyyN|M4OjZ4OR?=
MAC-2A NHfTTFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1G3TFAvODZ|LUSg{txO NWX0d482UUN3ME2wMlY6KM7:TTygbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MV6yN|M4OjZ4OR?=
MAC-2B NIXFem9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzwNE4xPjNvNDFOwG0> M3;oc2lEPTB;MD61OEDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= M2XoU|I{Ozd{Nk[5
MY-LA M4flNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEH2bYkxNjB4Mz20JO69VQ>? MWHJR|UxRTJwMTFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? NF;TboczOzN5Mk[2PS=>
NC-NC MoW2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1i5WFAvODZ|LUSg{txO MVnJR|UxRTFwMDFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? MVyyN|M4OjZ4OR?=
SE-AX MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHNOFlrOC5yNkOtOEDPxE1? M3LUR2lEPTB;MT61JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= M2TC[lI{Ozd{Nk[5
SR-786 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHFU40xNjB4Mz20JO69VQ>? M4C3bWlEPTB;ND62JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= NWnZbJBlOjN|N{K2Olk>
M-MOK  NEWzfWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXWyOUDDvU4EoB?= MYOyOE81QC95MjDo M2i2OGROW09? MX;pcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 MnHGNlE5PTNzNUe=
HEL NVv0VphrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4juU2lEPTB;M{C1JI5O NIfYTZIyQDN7NEW1OC=>
Ba/F3 JAK2V617F M33Y[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nVWmlEPTB;MkewJI5O MU[xPFM6PDV3NB?=

... 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
  • Formulation: Dissolved in DMSO, and diluted in saline
  • 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
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% DMSO+30% polyethylene glycol+1% Tween 80
For best results, use promptly after mixing.
30 mg/mL

* 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=C(NC2=CC=CC(=C2)[S](=O)(=O)NC(C)(C)C)N=C(NC3=CC=C(OCCN4CCCC4)C=C3)N=C1

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 Not yet recruiting Drug: Fedratinib Healthy Volunteers|Hepatic Impairment Celgene|Impact Biomedicines Inc. a wholly owned subsidiary of Celgene Corporation December 15 2019 Phase 1
NCT03983239 Not yet recruiting Drug: Fedratinib|Drug: Rifampin|Drug: Rifabutin Healthy Volunteers Celgene|Impact Biomedicines Inc. a wholly owned subsidiary of Celgene Corporation December 15 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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