Fedratinib (SAR302503, TG101348)

Catalog No.S2736

Fedratinib (SAR302503, 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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Cited by 17 Publications

4 Customer Reviews

  • Colony-forming assay results showing that the Jak2 inhibitor TG101348 reduces CFU-GM colonies generated from mutant fetal liver R2 cells. Results from 4 independent control or mutant fetal livers treated with TG101348 or dimethylsulfoxide (DMSO) are shown (mean ?SD). ***P < .001.

    Blood 2014 123(20), 3175-84. Fedratinib (SAR302503, TG101348) purchased from Selleck.

  • Janus kinase (JAK) 1/2 inhibitors increase vesicular stomatitis virus-green fluorescent protein (VSV-GFP) susceptibility in SCC25 cells. Representative photographs of VSV infection in treated cells with and without JAK1/2 inhibitors.

    Cancer Gene Ther 2013 20, 582-9. Fedratinib (SAR302503, TG101348) purchased from Selleck.

  • Claude HAAN Université du Luxembour. Fedratinib (SAR302503, TG101348) purchased from Selleck.

  • Effects of JAK2, STAT3, and STAT1 inhibitor on surface and total expression of PD-L1 in the lung adenocarcinoma cell line HCC4006. JAK2 inhibition suppresses surface and whole expression of PD-L1 in HCC4006 cells. HCC4006 cells were treated for 48 hours with the JAK2 pharmacological inhibitor TG101348 (200 nM or 500 nM) or DMSO. Surface (A) and total (B) expression of PD-L1 were evaluated by flow cytometry. Results are representative of five independent experiments. STAT3 inhibition suppresses total expression of PD-L1 in HCC4006 cells but has no effect on surface expression of PD-L1. HCC4006 cells were treated for 48 hours with the STAT3 pharmacological inhibitor BP-1-102 (0.5 μM or 5 μM) or DMSO. Surface (C) and total (D) expression of PD-L1 were evaluated by flow cytometry. Results are representative of four independent experiments. Asterisks indicate statistically significant differences between the experimental and DMSO-treated cells (*p < 0.05, **p < 0.01, ***p < 0.001).

    J Thorac Oncol, 2016, 11(1):62-71. Fedratinib (SAR302503, TG101348) purchased from Selleck.

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 MmXyRZBweHSxc3nzJGF{e2G7 MVSwMlUuOiEQvF2= M{HXeFEzNTR6IHi= MUPEUXNQ NWDvc|FvcW6mdXPld{BieG:ydH;zbZMhcW5iYn;0bEBld3OnLTDhcoQhfGmvZT2g[IVx\W6mZX70JI1idm6nch?= NEDNU3gzPTh4OUKxNC=>
H1650 MYjBdI9xfG:|aYOgRZN{[Xl? MlPjNE42NTJizszN M13MWlEzNTR6IHi= NXnsWpJ4TE2VTx?= MW\pcoR2[2W|IHHwc5B1d3OrczDpckBjd3SqIHTvd4UuKGGwZDD0bY1mNSCmZYDlcoRmdnRibXHucoVz M3mxclI2QDZ7MkGw
H1975 NXW1O2N[TnWwY4Tpc44hSXO|YYm= MoPaNE4zPS1zIN88US=> MlXYNlQhcA>? MoC1SG1UVw>? M2DoZ4lvcGmkaYTzJIV5eHKnc4Ppc44hd2ZiYYDvdJRwe2m|LYLlcIF1\WRicILveIVqdiCEY3ytXGwtKEKlbD2yMEB{fXK4aY\pckwhYEmDUB?= NHrvR|YzPTh4OUKxNC=>
H1650 MlHjSpVv[3Srb36gRZN{[Xl? MmLQNE4zPS1zIN88US=> NIHR[VAzPCCq M3PPNGROW09? NXXsV5ZXcW6qaXLpeJMh\XiycnXzd4lwdiCxZjDhdI9xfG:|aYOtdoVt[XSnZDDwdo91\WmwIFLjcE1ZVCxiQnPsMVItKHO3co\peolvNCC[SVHQ Mn\wNlU5Pjl{MUC=
H1975 NYCwcVNKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUixJO69VQ>? MkfwOFghcA>? NWnsTHBpTE2VTx?= NFjPeoN{\W6|aYTpfoV{KGOnbHzzJJRwKHSqZTDjfZRwfG:6aXPpeJkhd2ZiZYLsc5Rqdmmk M2ezPFI2QDZ7MkGw
H1650 M2TIcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX72OXNqOSEQvF2= Mmn1OFghcA>? M4fkUWROW09? NX7IdndCe2Wwc3n0bZpmeyClZXzsd{B1dyC2aHWgZ5l1d3SxeHnjbZR6KG:oIHXycI91cW6rYh?= MoDsNlU5Pjl{MUC=
CD4+ T NWjGdnhRTnWwY4Tpc44hSXO|YYm= NGn4SIcxNjBzLUGg{txO M4nT[|Q5KGh? MWfEUXNQ NUT1cnMyemWmdXPld{B1cGVicHjvd5Bpd3K7bHH0bY9vKGyndnXsd{Bw\iCMQVuyJIFv\CCVVFHUN:Kh M2XFd|I2PTd{NUO1
Caco-2  NFXOSHlHfW6ldHnvckBCe3OjeR?= NInqOo8xNTF{MDFOwG0> NIHmUHc4KG2rbh?= M1jSRYlvcGmkaYTzJJRpcWGvaX7lJJVxfGGtZTD3bZRpKGGwIFnDOVDDqG:oIEKuNeKhyrWP MmPvNlUxPjN4N{K=
Caco-2  NGi0b2JHfW6ldHnvckBCe3OjeR?= MWSxNE82OC9zMECg{txO NVGxPW9YOiCq M4HoR4Rm[3KnYYPld{B1cGViZnz1fEBw\iCdM1jdeIhq[W2rbnWgZYNzd3O|IITo[UBud26xbHH5[ZIhf2m2aDDJR|UxKG:oIE[uOeKh|ryP M4PPe|I2ODZ|Nkey
HEK293 MSR  NYnZdlBtTnWwY4Tpc44hSXO|YYm= Mn7LNE0yOCEQvF2= NX3SPXh5PyCvaX6= NGCwWZlqdmirYnn0d{BpXEiWUkKge4l1cCCjbjDJR|UxyqCxZjCxMlLDqML3TR?= M3vQNFI2ODZ|Nkey
MedB-1 NY\FZnpjTnWwY4Tpc44hSXO|YYm= MnTRNU8zKM7:TR?= NHjwOlYzPCCq NVf4[IIx\GWlcnXhd4V{KFOWQWS2JJBpd3OyaH;yfYxifGmxbjDjc45k\W62cnH0bY9vKGSncHXu[IVvfGy7 M4LOflI1QTd5Nk[4
U2940 MlLISpVv[3Srb36gRZN{[Xl? Mn;nNU8zKM7:TR?= NXjiXmdlOjRiaB?= MnTS[IVkemWjc3XzJHNVSVR4IIDoc5NxcG:{eXzheIlwdiClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 M1\DVVI1QTd5Nk[4
K1106 MXXGeY5kfGmxbjDBd5NigQ>? MWOxM|Ih|ryP MlvBNlQhcA>? MkTV[IVkemWjc3XzJHNVSVR4IIDoc5NxcG:{eXzheIlwdiClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NWT2NmpGOjR7N{e2Olg>
K562 Ml7JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfWN|UxNTFizszN NGnZUJo4OiCq MY\pcohq[mm2czDLOVYzKGOnbHygdJJwdGmoZYLheIlwdiCjdDDobYdpKGOxbnPlcpRz[XSrb36= NHjidoIzPDd5NUOwPC=>
MDA-MB-468  NGe2cW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DabFMhyrWP NGfTVms1QCCq MUHlcohidmOnZDDzbYJkdDZiaX7keYNm\CCub4PzJI9nKGOnbHygeoli[mmuaYT5xsA> MlXuNlQ3PjJ6MUi=
MDA-MB-468 NYrVbJZrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnvc2IxNTRizszN MmPkOFghcA>? MV3y[ZN2dHS|IIPp[45q\mmlYX70JIxwe3Nib3[geoli[mmuaYT5JINwdXCjcnXkJJRwKFKLLVLQTUBidG:wZR?= NV\0cmxXOjR4NkK4NVg>
L428 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPDNE02KM7:TR?= NFf6WGw1QCCq MWrpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 MVSyOFYyODh{Nx?=
KMH2 NETEPI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nUelAuPSEQvF2= M4OyT|Q5KGh? M2jCRYlvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= NWHwOJJqOjR4MUC4Nlc>
L1236 NXzYZ25zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\ac|AuPSEQvF2= MWO0PEBp NHTWfZBqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 NVzEV2VjOjR4MUC4Nlc>
SUPHD1 NWe5O|JvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIX2OXYxNTVizszN MVG0PEBp MV\pcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 NGfV[nczPDZzMEiyOy=>
HDLM2 NWm5NINFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXuwMVUh|ryP M2jseFQ5KGh? NULtPIZNcW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> NIPoTHQzPDZzMEiyOy=>
K1106P MoOyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37DXlAuPSEQvF2= MV[0PEBp MUHpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 NEXrV4EzPDZzMEiyOy=>
L428 MX;BdI9xfG:|aYOgRZN{[Xl? NVe5TWJYOC9yLk[yOU8yNjJ3IN88US=> MUS0PEBp MXnpcoR2[2W|IITo[UBieG:ydH;zbZPDqA>? MUOyOFYyODh{Nx?=
KMH2 M4LncmFxd3C2b4Ppd{BCe3OjeR?= NVX3RohsOC9yLk[yOU8yNjJ3IN88US=> M{fvTFQ5KGh? MVzpcoR2[2W|IITo[UBieG:ydH;zbZPDqA>? M165Z|I1PjFyOEK3
L1236 MlO0RZBweHSxc3nzJGF{e2G7 MYiwM|AvPjJ3L{GuNlUh|ryP Ml3KOFghcA>? MnLjbY5lfWOnczD0bIUh[XCxcITvd4l{yqB? NVjlTnpFOjR4MUC4Nlc>
SUPHD1 NWTEOY1NSXCxcITvd4l{KEG|c3H5 MVWwM|AvPjJ3L{GuNlUh|ryP MlvZOFghcA>? NGT4dYdqdmS3Y3XzJJRp\SCjcH;weI9{cXQEoB?= MmrZNlQ3OTB6Mke=
HDLM2 M13NZmFxd3C2b4Ppd{BCe3OjeR?= NVrMUWRoOC9yLk[yOU8yNjJ3IN88US=> NWXDWXJrPDhiaB?= MmPQbY5lfWOnczD0bIUh[XCxcITvd4l{yqB? NG\VS5kzPDZzMEiyOy=>
K1106P M1T3RmFxd3C2b4Ppd{BCe3OjeR?= NUSzXFdSOC9yLk[yOU8yNjJ3IN88US=> NFzSbnQ1QCCq NXvuZ25ocW6mdXPld{B1cGViYYDvdJRwe2m|wrC= NIn0b3AzPDZzMEiyOy=>
L428 NF:2ZplHfW6ldHnvckBCe3OjeR?= NXvFW2RwOC13IN88US=> NYXHNYM3OjRiaB?= Mk[1bY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> MoXnNlQ3OTB6Mke=
KMH2 Mnm2SpVv[3Srb36gRZN{[Xl? NX;WU21qOC13IN88US=> NGDZeY0zPCCq MWPpcohq[mm2czDKRWszN1OWQWSgd4lodmGuaX7n NHW2UpczPDZzMEiyOy=>
L1236 M2PRfGZ2dmO2aX;uJGF{e2G7 NVfzPYhkOC13IN88US=> MoPBNlQhcA>? Ml\2bY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> NWLUNHA{OjR4MUC4Nlc>
SUPHD1 NXrJdIl5TnWwY4Tpc44hSXO|YYm= NYPt[WdUOC13IN88US=> NGT1[lIzPCCq MYXpcohq[mm2czDKRWszN1OWQWSgd4lodmGuaX7n NIm4cWMzPDZzMEiyOy=>
HDLM2 NHjsR3BHfW6ldHnvckBCe3OjeR?= NGXycHAxNTVizszN NFLw[WkzPCCq NGTsdYtqdmirYnn0d{BLSUt{L2PURXQhe2mpbnHsbY5o MljUNlQ3OTB6Mke=
K1106P MYDGeY5kfGmxbjDBd5NigQ>? MljGNE02KM7:TR?= M1;Ne|I1KGh? M1XiOYlvcGmkaYTzJGpCUzJxU2TBWEB{cWewYXzpcoc> NYPFS3VUOjR4MUC4Nlc>
MM.1S  NGjyNFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWr3SoM{UUN3ME2xMVMh|ryP NWrDUVExOjR3OESxNFE>
TpoR JAK2 WT MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HnXmlEPTB;MT60JEgyNjQkgKOxMlUqKM7:TR?= M4rzOlI1OjVzN{mw
TpoR JAK2 V617F MkLxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmj0TWM2OD1yLkigLFAvP+LCk{CuPUkh|ryP M1HUcFI1OjVzN{mw
TpoR W515L MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTBwODCoNE446oDVMT6wLUDPxE1? Mm\ZNlQzPTF5OUC=
Bcr-abl NHHhSIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTJwNzCoNk4z6oDVMz6zLUDPxE1? MV6yOFI2OTd7MB?=
JAK2 TW MkDMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzufVhKSzVyPUGuPEApOS534pETNk4{MSEQvF2= NEXX[3IzPDJ3MUe5NC=>
JAK2 V617F NFrrbZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;yR4FKSzVyPUCuOkApOC544pETNE44MSEQvF2= NWrjO|hYOjR{NUG3PVA>
MedB-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETP[mU1KM7:TR?= MWSyOE81QC95MjDo MmTXSG1UVw>? Mo\5bY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> NILD[IUzOzh3MkO2Oi=>
K1106 NHLEVIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzaOEDPxE1? M1;sRVI1NzR6L{eyJIg> MXPEUXNQ NVHOclJCcW6qaXLpeJMh[2WubDDndo94fGhidHnt[UBl\XCnbnTlcpRtgQ>? MmWxNlM5PTJ|Nk[=
U2940 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkD4OEDPxE1? MWCyOE81QC95MjDo NFnhZZNFVVOR MX;pcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 M3zWUVI{QDV{M{[2
FE-PD M4\wTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV2wMlA3Oy12IN88US=> NFuxV|hKSzVyPUmuOUDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= NGPDd4IzOzN5Mk[2PS=>
HEL NXfHT5hYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoC0NE4xPjNvNDFOwG0> M2rYTGlEPTB;MT61JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= NFLsPYUzOzN5Mk[2PS=>
K-562 NYTrR2JUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHD[Yg4OC5yNkOtOEDPxE1? MWjJR|UxRTJwNTFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? NIS1UWMzOzN5Mk[2PS=>
L-82 MojjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYCwMlA3Oy12IN88US=> NE\ER|NKSzVyPUCuPVgh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MnLxNlM{PzJ4Nkm=
MAC-1 NH;QRlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1rDfVAvODZ|LUSg{txO M{XP[mlEPTB;MD61NkDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= NHHReG4zOzN5Mk[2PS=>
MAC-2A NXL2Z|NYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWGwMlA3Oy12IN88US=> Mn3yTWM2OD1yLk[5JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= M1;iOFI{Ozd{Nk[5
MAC-2B NV3YXZVjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3O1S|AvODZ|LUSg{txO MX3JR|UxRTBwNUSg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 NH3yeWwzOzN5Mk[2PS=>
MY-LA MknNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPtNE4xPjNvNDFOwG0> M2nrVWlEPTB;Mj6xJO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= NV;hTWl6OjN|N{K2Olk>
NC-NC MoO2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkT6NE4xPjNvNDFOwG0> MmfjTWM2OD1zLkCg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 M2\QfFI{Ozd{Nk[5
SE-AX NVLncphiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjUVZUxNjB4Mz20JO69VQ>? MVXJR|UxRTFwNTFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? NHPUVoszOzN5Mk[2PS=>
SR-786 NGnO[4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;CNlAvODZ|LUSg{txO MYrJR|UxRTRwNjFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? NGK2RVQzOzN5Mk[2PS=>
M-MOK  M4rWdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV[yOUDDvU4EoB?= NFu0U44zPC92OD:3NkBp MljRSG1UVw>? NFz2em9qdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 M1XreVIyQDV|MUW3
HEL NHTWe|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLXfVZTUUN3ME2zNFUhdk1? MlzMNVg{QTR3NUS=
Ba/F3 JAK2V617F MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnlPWY5UUN3ME2yO|Ahdk1? MlrMNVg{QTR3NUS=

... Click to View More Cell Line Experimental Data

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 N/A

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 (g) = Concentration (mol/L) × Volume (L) × 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 Conditions Sponsor/Collaborators Start Date Phases
NCT03755518 Recruiting Primary Myelofibrosis|Thrombocytosis Celgene|Impact Biomedicines Inc. a wholly owned subsidiary of Celgene Corporation February 28 2019 Phase 3
NCT03755518 Recruiting Primary Myelofibrosis|Thrombocytosis Celgene|Impact Biomedicines Inc. a wholly owned subsidiary of Celgene Corporation February 28 2019 Phase 3
NCT01836705 Completed Neoplasm Malignant Sanofi May 2013 Phase 1
NCT01836705 Completed Neoplasm Malignant Sanofi May 2013 Phase 1
NCT01762462 Completed Hepatic Impairment Sanofi December 2012 Phase 1
NCT01762462 Completed Hepatic Impairment Sanofi December 2012 Phase 1

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.

  • * Indicates a Required Field

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID