Fedratinib (TG101348)

For research use only.

Catalog No.S2736 Synonyms: SAR302503

36 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 36 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 NXnaUVlkSXCxcITvd4l{KEG|c3H5 NXPIS2FSOC53LUKg{txO M{\TTFEzNTR6IHi= M3nZZWROW09? M2[wdIlv\HWlZYOgZZBweHSxc3nzJIlvKGKxdHig[I9{\S1iYX7kJJRqdWVvIHTldIVv\GWwdDDtZY5v\XJ? M2D4ZlI2QDZ7MkGw
H1650 M4K0[GFxd3C2b4Ppd{BCe3OjeR?= MoPnNE42NTJizszN MX2xNk01QCCq NVHDOFE{TE2VTx?= NH6wOJFqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCkb4ToJIRwe2VvIHHu[EB1cW2nLTDk[ZBmdmSnboSgcYFvdmW{ MnzFNlU5Pjl{MUC=
H1975 MVjGeY5kfGmxbjDBd5NigQ>? NEXhT|AxNjJ3LUGg{txO NEnwd4kzPCCq MUXEUXNQ M4\xOIlvcGmkaYTzJIV5eHKnc4Ppc44hd2ZiYYDvdJRwe2m|LYLlcIF1\WRicILveIVqdiCEY3ytXGwtKEKlbD2yMEB{fXK4aY\pckwhYEmDUB?= MkjVNlU5Pjl{MUC=
H1650 MXLGeY5kfGmxbjDBd5NigQ>? NGrJcGExNjJ3LUGg{txO MYGyOEBp M2HiXGROW09? NV\2SWhRcW6qaXLpeJMh\XiycnXzd4lwdiCxZjDhdI9xfG:|aYOtdoVt[XSnZDDwdo91\WmwIFLjcE1ZVCxiQnPsMVItKHO3co\peolvNCC[SVHQ MnrDNlU5Pjl{MUC=
H1975 MkH0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{L6VVEh|ryP NHrOW|E1QCCq M1fQXGROW09? NFu1WXV{\W6|aYTpfoV{KGOnbHzzJJRwKHSqZTDjfZRwfG:6aXPpeJkhd2ZiZYLsc5Rqdmmk NYDSXpZiOjV6NkmyNVA>
H1650 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1r2SVEh|ryP NWXNS3YzPDhiaB?= MmfESG1UVw>? MYLz[Y5{cXSrenXzJINmdGy|IITvJJRp\SCleYTveI95cWOrdImgc4Yh\XKub4Tpcolj NGDCelQzPTh4OUKxNC=>
CD4+ T MoTlSpVv[3Srb36gRZN{[Xl? NIP6WGcxNjBzLUGg{txO NIewc4M1QCCq MX3EUXNQ NGHR[Fhz\WS3Y3XzJJRp\SCyaH;zdIhwenmuYYTpc44hdGW4ZXzzJI9nKEqDS{KgZY5lKFOWQWSzxsA> NGrTbHgzPTV5MkWzOS=>
Caco-2  M4jrRmZ2dmO2aX;uJGF{e2G7 NWjiZ4hROC1zMkCg{txO NI\Rbok4KG2rbh?= MmHobY5pcWKrdIOgeIhq[W2rbnWgeZB1[WunIIfpeIgh[W5iSVO1NOKhd2ZiMj6xxsDDvU1? MoW1NlUxPjN4N{K=
Caco-2  MkPGSpVv[3Srb36gRZN{[Xl? M3zvV|ExNzVyL{GwNEDPxE1? MVmyJIg> NX;0WnlH\GWlcnXhd4V{KHSqZTDmcJV5KG:oIGuzTH11cGmjbXnu[UBi[3Kxc4OgeIhmKG2xbn;sZZlmeiC5aYToJGlEPTBib3[gOk42yqEQvF2= M{XRTVI2ODZ|Nkey
HEK293 MSR  M1[5VWZ2dmO2aX;uJGF{e2G7 NXvRU2ViOC1zMDFOwG0> MnrsO{BucW5? M3i4OYlvcGmkaYTzJIhVUFSUMjD3bZRpKGGwIFnDOVDDqG:oIEGuNuKhyrWP M3u1V|I2ODZ|Nkey
MedB-1 NIPq[nRHfW6ldHnvckBCe3OjeR?= NVO4NZMzOS9{IN88US=> MYmyOEBp MYTk[YNz\WG|ZYOgV3RCXDZicHjvd5Bpd3K7bHH0bY9vKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> NED6ToEzPDl5N{[2PC=>
U2940 NUDneG15TnWwY4Tpc44hSXO|YYm= NF;UXHIyNzJizszN MV:yOEBp MVHk[YNz\WG|ZYOgV3RCXDZicHjvd5Bpd3K7bHH0bY9vKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> NGjpVIgzPDl5N{[2PC=>
K1106 M4HZcmZ2dmO2aX;uJGF{e2G7 M3TRNlEwOiEQvF2= NIe4cmMzPCCq MmnD[IVkemWjc3XzJHNVSVR4IIDoc5NxcG:{eXzheIlwdiClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NHXa[Y4zPDl5N{[2PC=>
K562 MkHyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUX6SlNMOC1zIN88US=> M4\0XFczKGh? MnmybY5pcWKrdIOgT|U3OiClZXzsJJBzd2yrZnXyZZRqd25iYYSgbIlocCClb37j[Y51emG2aX;u M1HSVFI1Pzd3M{C4
MDA-MB-468  NI\CSoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzEN{DDvU1? NGG4[4o1QCCq M3jzb4VvcGGwY3XkJJNq[mOuNjDpcoR2[2WmIHzvd5Mhd2ZiY3XscEB3cWGkaXzpeJnDqA>? NIXhNWszPDZ4MkixPC=>
MDA-MB-468 NVT3T2FuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfyNE01KM7:TR?= MofoOFghcA>? M2XUWpJme3WudIOgd4lodmmoaXPhcpQhdG:|czDv[kB3cWGkaXzpeJkh[2:vcHHy[YQhfG9iUlmtRnBKKGGub37l MYeyOFY3OjhzOB?=
L428 NY\zeHM2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWqwMVUh|ryP MV:0PEBp M1fVZ4lvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= NFznTGQzPDZzMEiyOy=>
KMH2 NGjWdJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrkN2MxNTVizszN NGXweGg1QCCq Mnq2bY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= M2DzfFI1PjFyOEK3
L1236 NIL1N4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3Lm[lAuPSEQvF2= M1\QWFQ5KGh? M1PQRolvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= MWOyOFYyODh{Nx?=
SUPHD1 NILmdItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\RfVAuPSEQvF2= NHTkNpY1QCCq M2XWcolvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= M4DhXVI1PjFyOEK3
HDLM2 NX21[49XT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrLNnIxNTVizszN M1zmfVQ5KGh? NVHrTYRqcW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> MmrMNlQ3OTB6Mke=
K1106P NWrM[4h7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4XEVVAuPSEQvF2= NHPJOlU1QCCq MX3pcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 Ml;HNlQ3OTB6Mke=
L428 Mor2RZBweHSxc3nzJGF{e2G7 M4DOelAwOC54MkWvNU4zPSEQvF2= NXfmSmxnPDhiaB?= M{XtSolv\HWlZYOgeIhmKGGyb4D0c5Nqe8Li NHnNOVAzPDZzMEiyOy=>
KMH2 M3TzOmFxd3C2b4Ppd{BCe3OjeR?= MXqwM|AvPjJ3L{GuNlUh|ryP MVO0PEBp MXTpcoR2[2W|IITo[UBieG:ydH;zbZPDqA>? MVmyOFYyODh{Nx?=
L1236 MlXyRZBweHSxc3nzJGF{e2G7 NXqyWZNbOC9yLk[yOU8yNjJ3IN88US=> M1uyOFQ5KGh? MWHpcoR2[2W|IITo[UBieG:ydH;zbZPDqA>? NUjzdoNHOjR4MUC4Nlc>
SUPHD1 NHrRcHhCeG:ydH;zbZMhSXO|YYm= NVuzcYlGOC9yLk[yOU8yNjJ3IN88US=> MV60PEBp MlvZbY5lfWOnczD0bIUh[XCxcITvd4l{yqB? NH;VVZozPDZzMEiyOy=>
HDLM2 M2PSNGFxd3C2b4Ppd{BCe3OjeR?= MnLuNE8xNjZ{NT:xMlI2KM7:TR?= NF;reog1QCCq M2nSS4lv\HWlZYOgeIhmKGGyb4D0c5Nqe8Li MXuyOFYyODh{Nx?=
K1106P MXnBdI9xfG:|aYOgRZN{[Xl? M37rT|AwOC54MkWvNU4zPSEQvF2= NW\HWWNiPDhiaB?= NWO3d3ZCcW6mdXPld{B1cGViYYDvdJRwe2m|wrC= M2nrW|I1PjFyOEK3
L428 MYTGeY5kfGmxbjDBd5NigQ>? M{\k[|AuPSEQvF2= NVrPcoxPOjRiaB?= MVTpcohq[mm2czDKRWszN1OWQWSgd4lodmGuaX7n MoTlNlQ3OTB6Mke=
KMH2 MVnGeY5kfGmxbjDBd5NigQ>? MmfLNE02KM7:TR?= MkG0NlQhcA>? NIfLdHdqdmirYnn0d{BLSUt{L2PURXQhe2mpbnHsbY5o NYrpcI9iOjR4MUC4Nlc>
L1236 MWfGeY5kfGmxbjDBd5NigQ>? MlLLNE02KM7:TR?= NFSzeIIzPCCq NIr1[GtqdmirYnn0d{BLSUt{L2PURXQhe2mpbnHsbY5o MnnxNlQ3OTB6Mke=
SUPHD1 MknGSpVv[3Srb36gRZN{[Xl? MWqwMVUh|ryP MYCyOEBp MY\pcohq[mm2czDKRWszN1OWQWSgd4lodmGuaX7n M1HXbVI1PjFyOEK3
HDLM2 NULhSpM6TnWwY4Tpc44hSXO|YYm= MVqwMVUh|ryP NH34bZczPCCq Mmj1bY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> MlvkNlQ3OTB6Mke=
K1106P M{\u[GZ2dmO2aX;uJGF{e2G7 MU[wMVUh|ryP MkK4NlQhcA>? NXrEUW1NcW6qaXLpeJMhUkGNMj;TWGFVKHOrZ37hcIlv\w>? Mm\JNlQ3OTB6Mke=
MM.1S  MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\oUIszUUN3ME2xMVMh|ryP NE[wflUzPDV6NEGwNS=>
TpoR JAK2 WT M{\Xc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fhfmlEPTB;MT60JEgyNjQkgKOxMlUqKM7:TR?= NHLFbm0zPDJ3MUe5NC=>
TpoR JAK2 V617F MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TzXGlEPTB;MD64JEgxNjgkgKOwMlkqKM7:TR?= NUD3NHN2OjR{NUG3PVA>
TpoR W515L NXTSVnpnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnL6TWM2OD1yLkigLFAvP+LCk{GuNEkh|ryP M3HLbVI1OjVzN{mw
Bcr-abl MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHS0V2lKSzVyPUKuO{ApOi5{4pETN{4{MSEQvF2= NH\RUVMzPDJ3MUe5NC=>
JAK2 TW NHjEU5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DidWlEPTB;MT64JEgyNjYkgKOyMlMqKM7:TR?= Ml6xNlQzPTF5OUC=
JAK2 V617F MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnmVIlOUUN3ME2wMlYhMDBwNvMAl|AvPylizszN M{\nUlI1OjVzN{mw
MedB-1 NHv5dWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELWN|Q1KM7:TR?= NXS1OmJIOjRxNEivO|IhcA>? NV;VeopYTE2VTx?= NH2wcm9qdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 M2jlZVI{QDV{M{[2
K1106 NG[yb|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDzS2VUPCEQvF2= M2nvUFI1NzR6L{eyJIg> Mor2SG1UVw>? NYjDNoRmcW6qaXLpeJMh[2WubDDndo94fGhidHnt[UBl\XCnbnTlcpRtgQ>? MYCyN|g2OjN4Nh?=
U2940 NEK3UpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jtdFQh|ryP NX\5NmszOjRxNEivO|IhcA>? M1LpU2ROW09? NHP0dGJqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 NILZO3kzOzh3MkO2Oi=>
FE-PD NUTnS|lxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\zfIEyOC5yNkOtOEDPxE1? NHn1W5JKSzVyPUmuOUDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= MkXaNlM{PzJ4Nkm=
HEL NHvSeFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7JU3AxNjB4Mz20JO69VQ>? M2PTNmlEPTB;MT61JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= MnTRNlM{PzJ4Nkm=
K-562 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWmwMlA3Oy12IN88US=> MUPJR|UxRTJwNTFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? MnH2NlM{PzJ4Nkm=
L-82 MmPMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfqOZNmOC5yNkOtOEDPxE1? MoHuTWM2OD1yLkm4JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= NFrnSJAzOzN5Mk[2PS=>
MAC-1 Mn\1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVWwMlA3Oy12IN88US=> NFq5PXVKSzVyPUCuOVIh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MYqyN|M4OjZ4OR?=
MAC-2A M2\iSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{TiTVAvODZ|LUSg{txO MVXJR|UxRTBwNkmg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 M{nqdFI{Ozd{Nk[5
MAC-2B NYnkSmlXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWewMlA3Oy12IN88US=> NH7GXlNKSzVyPUCuOVQh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MkH6NlM{PzJ4Nkm=
MY-LA NEXoPG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;Gc4w1OC5yNkOtOEDPxE1? MoXjTWM2OD1{LkGg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 NVz4dmwyOjN|N{K2Olk>
NC-NC NVvvfIJ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrEcWRtOC5yNkOtOEDPxE1? NIjCRmdKSzVyPUGuNEDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= MoXxNlM{PzJ4Nkm=
SE-AX MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzuS4FtOC5yNkOtOEDPxE1? MUPJR|UxRTFwNTFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? MXeyN|M4OjZ4OR?=
SR-786 NY\ISI9KT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fRUlAvODZ|LUSg{txO MUDJR|UxRTRwNjFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? MkLQNlM{PzJ4Nkm=
M-MOK  M2jMbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\Te5czPSEEtV5CpC=> M4TGNlI1NzR6L{eyJIg> MYPEUXNQ NHi2OoxqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 NIXjdJMzOTh3M{G1Oy=>
HEL MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXGTWM2OD1|MEWgcm0> M4TTbVE5Ozl2NUW0
Ba/F3 JAK2V617F M4P3cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PwfWlEPTB;MkewJI5O MnLhNVg{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=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