Fedratinib (TG101348)

For research use only.

Catalog No.S2736 Synonyms: SAR302503

36 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. 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 36 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. 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 M2[yR2Fxd3C2b4Ppd{BCe3OjeR?= Mn20NE42NTJizszN MVOxNk01QCCq MUHEUXNQ MWrpcoR2[2W|IHHwc5B1d3OrczDpckBjd3SqIHTvd4UuKGGwZDD0bY1mNSCmZYDlcoRmdnRibXHucoVz NF7qVoEzPTh4OUKxNC=>
H1650 M2rRVGFxd3C2b4Ppd{BCe3OjeR?= M1mzPFAvPS1{IN88US=> NGH4SncyOi12ODDo NHPQdVRFVVOR NUfqfotncW6mdXPld{BieG:ydH;zbZMhcW5iYn;0bEBld3OnLTDhcoQhfGmvZT2g[IVx\W6mZX70JI1idm6nch?= M2m1dVI2QDZ7MkGw
H1975 Ml;TSpVv[3Srb36gRZN{[Xl? M4fRUFAvOjVvMTFOwG0> M{fBVVI1KGh? NFPZXpRFVVOR NU\qNWFUcW6qaXLpeJMh\XiycnXzd4lwdiCxZjDhdI9xfG:|aYOtdoVt[XSnZDDwdo91\WmwIFLjcE1ZVCxiQnPsMVItKHO3co\peolvNCC[SVHQ MWOyOVg3QTJzMB?=
H1650 NHO3NpZHfW6ldHnvckBCe3OjeR?= NWTTXWozOC5{NT2xJO69VQ>? MXiyOEBp NUHGb4lLTE2VTx?= M13ie4lvcGmkaYTzJIV5eHKnc4Ppc44hd2ZiYYDvdJRwe2m|LYLlcIF1\WRicILveIVqdiCEY3ytXGwtKEKlbD2yMEB{fXK4aY\pckwhYEmDUB?= NVjPZno5OjV6NkmyNVA>
H1975 NX3tdYZ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF62cXkyKM7:TR?= M2LDXVQ5KGh? Mli0SG1UVw>? M{DTUZNmdnOrdHn6[ZMh[2WubIOgeI8hfGinIHP5eI91d3irY3n0fUBw\iCncnzveIlvcWJ? NY\RbpJNOjV6NkmyNVA>
H1650 M173ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDo[IoyKM7:TR?= MVK0PEBp MnTPSG1UVw>? MkDBd4Vve2m2aYrld{Bk\WyuczD0c{B1cGViY4n0c5RwgGmlaYT5JI9nKGW{bH;0bY5q[g>? M2rLXlI2QDZ7MkGw
CD4+ T NYTZOJhWTnWwY4Tpc44hSXO|YYm= MW[wMlAyNTFizszN M2jsdVQ5KGh? NXHQN5pHTE2VTx?= MlTJdoVlfWOnczD0bIUheGixc4Doc5J6dGG2aX;uJIxmfmWuczDv[kBLSUt{IHHu[EBUXEGWM9Mg M4WwXlI2PTd{NUO1
Caco-2  MYfGeY5kfGmxbjDBd5NigQ>? M4nuRlAuOTJyIN88US=> NFnTTXU4KG2rbh?= MWPpcohq[mm2czD0bIlidWmwZTD1dJRic2Vid3n0bEBidiCLQ{WwxsBw\iB{LkJCpOK2VQ>? NYTkcZpxOjVyNkO2O|I>
Caco-2  M3HWNWZ2dmO2aX;uJGF{e2G7 MV[xNE82OC9zMECg{txO MnHnNkBp MnSw[IVkemWjc3XzJJRp\SCobIX4JI9nKFt|SG30bIlidWmwZTDhZ5Jwe3NidHjlJI1wdm:uYYnldkB4cXSqIFnDOVAhd2ZiNj61xsDPxE1? NFi4UJczPTB4M{[3Ni=>
HEK293 MSR  MnfwSpVv[3Srb36gRZN{[Xl? NETXR4IxNTFyIN88US=> NHPSfmE4KG2rbh?= NGPRVlRqdmirYnn0d{BpXEiWUkKge4l1cCCjbjDJR|UxyqCxZjCxMlLDqML3TR?= M13X[lI2ODZ|Nkey
MedB-1 MoX0SpVv[3Srb36gRZN{[Xl? MVOxM|Ih|ryP M37QSFI1KGh? MlrI[IVkemWjc3XzJHNVSVR4IIDoc5NxcG:{eXzheIlwdiClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NF;GNGYzPDl5N{[2PC=>
U2940 NWHiZpl4TnWwY4Tpc44hSXO|YYm= M2fVelEwOiEQvF2= Ml\GNlQhcA>? M3XGS4Rm[3KnYYPld{BUXEGWNjDwbI9{eGixconsZZRqd25iY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? NXHtPIhMOjR7N{e2Olg>
K1106 NGXFT5RHfW6ldHnvckBCe3OjeR?= M1rM[FEwOiEQvF2= MmC5NlQhcA>? NUO0VpVt\GWlcnXhd4V{KFOWQWS2JJBpd3OyaH;yfYxifGmxbjDjc45k\W62cnH0bY9vKGSncHXu[IVvfGy7 MWqyOFk4PzZ4OB?=
K562 M1;GcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUOwMVEh|ryP MVe3NkBp M4DtdolvcGmkaYTzJGs2PjJiY3XscEBxem:uaX\ldoF1cW:wIHH0JIhq\2hiY3;uZ4VvfHKjdHnvci=> M1OyOlI1Pzd3M{C4
MDA-MB-468  MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NULIW41FOyEEtV2= MmD2OFghcA>? NX62ZY9t\W6qYX7j[YQhe2mkY3y2JIlv\HWlZXSgcI9{eyCxZjDj[YxtKH[rYXLpcIl1gcLi MlrMNlQ3PjJ6MUi=
MDA-MB-468 NF[1do9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHP0ZVgxNTRizszN MYO0PEBp NV3weGRJemW|dXz0d{B{cWewaX\pZ4FvfCCub4PzJI9nKH[rYXLpcIl1gSClb33wZZJm\CC2bzDSTU1DWEliYXzvcoU> MojDNlQ3PjJ6MUi=
L428 NULvfG9NT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrZ[WRTOC13IN88US=> MmDoOFghcA>? NIXsW3ZqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 MUKyOFYyODh{Nx?=
KMH2 NYfLZodJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGmzd3QxNTVizszN MXy0PEBp M134N4lvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= M3rUUlI1PjFyOEK3
L1236 M2XyU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTkR|NLOC13IN88US=> M3HRflQ5KGh? M{fvc4lvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= MnzINlQ3OTB6Mke=
SUPHD1 MnHBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVfheZl7OC13IN88US=> M1;VTFQ5KGh? MWHpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 MkfNNlQ3OTB6Mke=
HDLM2 M3fRdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTtNE02KM7:TR?= MlKwOFghcA>? MWLpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 MlewNlQ3OTB6Mke=
K1106P MmLyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrtNE02KM7:TR?= NXftc|BwPDhiaB?= MYTpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 M{nSN|I1PjFyOEK3
L428 M{LNfmFxd3C2b4Ppd{BCe3OjeR?= MVewM|AvPjJ3L{GuNlUh|ryP M3fuWVQ5KGh? M3XR[olv\HWlZYOgeIhmKGGyb4D0c5Nqe8Li NHLlS2wzPDZzMEiyOy=>
KMH2 NX21U5pbSXCxcITvd4l{KEG|c3H5 MoX5NE8xNjZ{NT:xMlI2KM7:TR?= M1jBcVQ5KGh? Moq4bY5lfWOnczD0bIUh[XCxcITvd4l{yqB? Mo\nNlQ3OTB6Mke=
L1236 MkDsRZBweHSxc3nzJGF{e2G7 Ml7KNE8xNjZ{NT:xMlI2KM7:TR?= Mk\MOFghcA>? NV\4[4RTcW6mdXPld{B1cGViYYDvdJRwe2m|wrC= MX[yOFYyODh{Nx?=
SUPHD1 MXTBdI9xfG:|aYOgRZN{[Xl? M3yxS|AwOC54MkWvNU4zPSEQvF2= M3\0[FQ5KGh? NYDLTGk{cW6mdXPld{B1cGViYYDvdJRwe2m|wrC= Mo[zNlQ3OTB6Mke=
HDLM2 MUnBdI9xfG:|aYOgRZN{[Xl? MVOwM|AvPjJ3L{GuNlUh|ryP NGrpdpM1QCCq NYnYZlRWcW6mdXPld{B1cGViYYDvdJRwe2m|wrC= NF3rOG4zPDZzMEiyOy=>
K1106P Mnm1RZBweHSxc3nzJGF{e2G7 MWewM|AvPjJ3L{GuNlUh|ryP NHvEWXM1QCCq MXfpcoR2[2W|IITo[UBieG:ydH;zbZPDqA>? NVHaO5ZKOjR4MUC4Nlc>
L428 MofuSpVv[3Srb36gRZN{[Xl? MmrBNE02KM7:TR?= MY[yOEBp NGL4RmJqdmirYnn0d{BLSUt{L2PURXQhe2mpbnHsbY5o NIjjUIEzPDZzMEiyOy=>
KMH2 M2q4WmZ2dmO2aX;uJGF{e2G7 Ml;HNE02KM7:TR?= NWC3TpV{OjRiaB?= NHLBU3VqdmirYnn0d{BLSUt{L2PURXQhe2mpbnHsbY5o NFPIcZMzPDZzMEiyOy=>
L1236 MX7GeY5kfGmxbjDBd5NigQ>? M3vtflAuPSEQvF2= MUGyOEBp NULCSHJHcW6qaXLpeJMhUkGNMj;TWGFVKHOrZ37hcIlv\w>? NUfDbIlzOjR4MUC4Nlc>
SUPHD1 MlKzSpVv[3Srb36gRZN{[Xl? M{\sNFAuPSEQvF2= M4P2[VI1KGh? M136S4lvcGmkaYTzJGpCUzJxU2TBWEB{cWewYXzpcoc> NWfYVo5QOjR4MUC4Nlc>
HDLM2 NUPDeXJDTnWwY4Tpc44hSXO|YYm= MnTkNE02KM7:TR?= NIXrWYIzPCCq M1qxdIlvcGmkaYTzJGpCUzJxU2TBWEB{cWewYXzpcoc> M2D2PFI1PjFyOEK3
K1106P M3fEXWZ2dmO2aX;uJGF{e2G7 NHnDTVYxNTVizszN NXW0bYZKOjRiaB?= M4XneIlvcGmkaYTzJGpCUzJxU2TBWEB{cWewYXzpcoc> NHLLcHAzPDZzMEiyOy=>
MM.1S  MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmWyTWM2OD1zLUOg{txO MYmyOFU5PDFyMR?=
TpoR JAK2 WT Mo[4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HtXWlEPTB;MT60JEgyNjQkgKOxMlUqKM7:TR?= NHuxVYgzPDJ3MUe5NC=>
TpoR JAK2 V617F MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LHb2lEPTB;MD64JEgxNjgkgKOwMlkqKM7:TR?= NHLpO|EzPDJ3MUe5NC=>
TpoR W515L M2HYfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGK2V2RKSzVyPUCuPEApOC554pETNU4xMSEQvF2= M3:zdFI1OjVzN{mw
Bcr-abl M{XHd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MliwTWM2OD1{LkegLFIvOuLCk{OuN{kh|ryP NFzYeGgzPDJ3MUe5NC=>
JAK2 TW MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fue2lEPTB;MT64JEgyNjYkgKOyMlMqKM7:TR?= M1zGWVI1OjVzN{mw
JAK2 V617F M{G0O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTBwNjCoNE436oDVMD63LUDPxE1? NELRZ3AzPDJ3MUe5NC=>
MedB-1 NWH4XG9VT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX[0JO69VQ>? MmnFNlQwPDhxN{KgbC=> M17FZWROW09? NIjERVFqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 NF7jSVAzOzh3MkO2Oi=>
K1106 M4DONGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUm0JO69VQ>? NEjMOVgzPC92OD:3NkBp MnWxSG1UVw>? NFO0PItqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 NIj0[IIzOzh3MkO2Oi=>
U2940 MmfLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\aenc1KM7:TR?= M{TmSlI1NzR6L{eyJIg> MoXTSG1UVw>? NUfQOmtFcW6qaXLpeJMh[2WubDDndo94fGhidHnt[UBl\XCnbnTlcpRtgQ>? Mnz6NlM5PTJ|Nk[=
FE-PD NEex[plIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYewMlA3Oy12IN88US=> NXLYRo1oUUN3ME25MlUh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NInNdm4zOzN5Mk[2PS=>
HEL NFT5PHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPNcmgxNjB4Mz20JO69VQ>? MlnQTWM2OD1zLkWg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 MVGyN|M4OjZ4OR?=
K-562 M1;5VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYmwMlA3Oy12IN88US=> NUGxTlc2UUN3ME2yMlUh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NVrWTplmOjN|N{K2Olk>
L-82 Mk\wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXqwMlA3Oy12IN88US=> NUiwVGFEUUN3ME2wMlk5KM7:TTygbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MXuyN|M4OjZ4OR?=
MAC-1 M2npUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIewVVExNjB4Mz20JO69VQ>? MXLJR|UxRTBwNUKg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 NGT2b|IzOzN5Mk[2PS=>
MAC-2A NUG4XlZsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rxTVAvODZ|LUSg{txO NWOxTpBOUUN3ME2wMlY6KM7:TTygbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MYSyN|M4OjZ4OR?=
MAC-2B NYS3bHpmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXmwMlA3Oy12IN88US=> NHO3TWVKSzVyPUCuOVQh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NYPZUI9vOjN|N{K2Olk>
MY-LA Mn3JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTSNE4xPjNvNDFOwG0> M2rBXGlEPTB;Mj6xJO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= MYmyN|M4OjZ4OR?=
NC-NC NF:5WJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUe4fndQOC5yNkOtOEDPxE1? M4f4VWlEPTB;MT6wJO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= MXmyN|M4OjZ4OR?=
SE-AX NFHKPY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LzOFAvODZ|LUSg{txO MYrJR|UxRTFwNTFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? NH3WTY8zOzN5Mk[2PS=>
SR-786 M3;XR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm[4NE4xPjNvNDFOwG0> NISySJlKSzVyPUSuOkDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= NULiRotWOjN|N{K2Olk>
M-MOK  MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITEepAzPSEEtV5CpC=> MmXDNlQwPDhxN{KgbC=> NH7PbJVFVVOR NIjsVFdqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 M3rTO|IyQDV|MUW3
HEL NXXWcFVtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2i1emlEPTB;M{C1JI5O MmXlNVg{QTR3NUS=
Ba/F3 JAK2V617F NIfjeXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13OemlEPTB;MkewJI5O Mn;INVg{QTR3NUS=

... 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
  • 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

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 (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% 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
NCT03983239 Recruiting Drug: Fedratinib|Drug: Rifampin|Drug: Efavirenz Healthy Volunteers Celgene|Impact Biomedicines Inc. a wholly owned subsidiary of Celgene Corporation December 15 2019 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
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.

  • * Indicates a Required Field

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