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 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 NIXHZmVCeG:ydH;zbZMhSXO|YYm= M1:5elAvPS1{IN88US=> NX:3epF[OTJvNEigbC=> NIrzem1FVVOR NEHrfmRqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCkb4ToJIRwe2VvIHHu[EB1cW2nLTDk[ZBmdmSnboSgcYFvdmW{ M33OR|I2QDZ7MkGw
H1650 MYPBdI9xfG:|aYOgRZN{[Xl? M4PXWVAvPS1{IN88US=> MXixNk01QCCq NIrYfXJFVVOR MYfpcoR2[2W|IHHwc5B1d3OrczDpckBjd3SqIHTvd4UuKGGwZDD0bY1mNSCmZYDlcoRmdnRibXHucoVz NGO3SZMzPTh4OUKxNC=>
H1975 NUDzWnppTnWwY4Tpc44hSXO|YYm= MVKwMlI2NTFizszN MlPXNlQhcA>? MX\EUXNQ MnfObY5pcWKrdIOg[ZhxemW|c3nvckBw\iCjcH;weI9{cXNvcnXsZZRm\CCycn;0[YlvKEKlbD3YUEwhSmOuLUKsJJN2en[rdnnuMEBZUUGS NHHKRlgzPTh4OUKxNC=>
H1650 NVrsZWpQTnWwY4Tpc44hSXO|YYm= MmrRNE4zPS1zIN88US=> NH;4fW8zPCCq Mnv2SG1UVw>? NX7iUHJicW6qaXLpeJMh\XiycnXzd4lwdiCxZjDhdI9xfG:|aYOtdoVt[XSnZDDwdo91\WmwIFLjcE1ZVCxiQnPsMVItKHO3co\peolvNCC[SVHQ NGjsZlQzPTh4OUKxNC=>
H1975 NY\qdlFWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTVNUDPxE1? NI\IXoo1QCCq NWLNeotwTE2VTx?= MVnz[Y5{cXSrenXzJINmdGy|IITvJJRp\SCleYTveI95cWOrdImgc4Yh\XKub4Tpcolj MVSyOVg3QTJzMB?=
H1650 NIi5b3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYGxJO69VQ>? MX[0PEBp M2LkemROW09? NYPPfWhGe2Wwc3n0bZpmeyClZXzsd{B1dyC2aHWgZ5l1d3SxeHnjbZR6KG:oIHXycI91cW6rYh?= MV:yOVg3QTJzMB?=
CD4+ T MYfGeY5kfGmxbjDBd5NigQ>? NES1V3UxNjBzLUGg{txO NH;Pb5I1QCCq NF21d2pFVVOR NIrKbmpz\WS3Y3XzJJRp\SCyaH;zdIhwenmuYYTpc44hdGW4ZXzzJI9nKEqDS{KgZY5lKFOWQWSzxsA> Mn;HNlU2PzJ3M{W=
Caco-2  NWi0S2tbTnWwY4Tpc44hSXO|YYm= MX:wMVEzOCEQvF2= MlLpO{BucW5? NIjHWYFqdmirYnn0d{B1cGmjbXnu[UB2eHSja3Wge4l1cCCjbjDJR|UxyqCxZjCyMlHDqML3TR?= MlLpNlUxPjN4N{K=
Caco-2  MVHGeY5kfGmxbjDBd5NigQ>? NUnrS4RpOTBxNUCvNVAxKM7:TR?= NYnXUFhMOiCq MWDk[YNz\WG|ZYOgeIhmKG[udYigc4YhYzOKXYTobYFucW6nIHHjdo9{eyC2aHWgcY9vd2yjeXXyJJdqfGhiSVO1NEBw\iB4LkZCpO69VQ>? MmHuNlUxPjN4N{K=
HEK293 MSR  NGnreplHfW6ldHnvckBCe3OjeR?= NFXBOIExNTFyIN88US=> MYe3JI1qdg>? NILZNJlqdmirYnn0d{BpXEiWUkKge4l1cCCjbjDJR|UxyqCxZjCxMlLDqML3TR?= MUeyOVA3OzZ5Mh?=
MedB-1 NIjuSmJHfW6ldHnvckBCe3OjeR?= NXv4Z2Y3OS9{IN88US=> NWfyRmJTOjRiaB?= M4\ZbYRm[3KnYYPld{BUXEGWNjDwbI9{eGixconsZZRqd25iY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? M1exO|I1QTd5Nk[4
U2940 MUXGeY5kfGmxbjDBd5NigQ>? NHr5SnQyNzJizszN NVy3RWE1OjRiaB?= M4K1cYRm[3KnYYPld{BUXEGWNjDwbI9{eGixconsZZRqd25iY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? NUfEVXJCOjR7N{e2Olg>
K1106 NEHxcJpHfW6ldHnvckBCe3OjeR?= MUmxM|Ih|ryP MYmyOEBp NX75S5Nb\GWlcnXhd4V{KFOWQWS2JJBpd3OyaH;yfYxifGmxbjDjc45k\W62cnH0bY9vKGSncHXu[IVvfGy7 NGD5c4UzPDl5N{[2PC=>
K562 NFezUYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW[wMVEh|ryP MXi3NkBp MYrpcohq[mm2czDLOVYzKGOnbHygdJJwdGmoZYLheIlwdiCjdDDobYdpKGOxbnPlcpRz[XSrb36= MWKyOFc4PTNyOB?=
MDA-MB-468  M{LIb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVSzJOK2VQ>? MX20PEBp Ml\B[Y5p[W6lZXSgd4lj[2x4IHnu[JVk\WRibH;zd{Bw\iClZXzsJJZq[WKrbHn0feKh M3fmOVI1PjZ{OEG4
MDA-MB-468 NEntR49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrhWFMxNTRizszN MUC0PEBp NWXwSHB2emW|dXz0d{B{cWewaX\pZ4FvfCCub4PzJI9nKH[rYXLpcIl1gSClb33wZZJm\CC2bzDSTU1DWEliYXzvcoU> NFPDRnMzPDZ4MkixPC=>
L428 Mo[4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYSwMVUh|ryP NFXlNVk1QCCq MYLpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 NIO1N3IzPDZzMEiyOy=>
KMH2 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFHQWFAxNTVizszN MVy0PEBp NE\4SWNqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 MXqyOFYyODh{Nx?=
L1236 NXrqfZFbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPxS2gxNTVizszN M4X3[|Q5KGh? NWHDWmlDcW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> M4W3PFI1PjFyOEK3
SUPHD1 NYLiPIJFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPQNE02KM7:TR?= MY[0PEBp MUDpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 NWPnUWJoOjR4MUC4Nlc>
HDLM2 M2TXWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrqPHBJOC13IN88US=> MXW0PEBp M2TQSolvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= M{nzZlI1PjFyOEK3
K1106P MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYSwMVUh|ryP MmG1OFghcA>? NV[zXWVNcW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> MXeyOFYyODh{Nx?=
L428 NWPnRnFISXCxcITvd4l{KEG|c3H5 NHn4VXMxNzBwNkK1M|EvOjVizszN MlzTOFghcA>? NGXDWllqdmS3Y3XzJJRp\SCjcH;weI9{cXQEoB?= NWDXeoxiOjR4MUC4Nlc>
KMH2 NV61dppPSXCxcITvd4l{KEG|c3H5 MVOwM|AvPjJ3L{GuNlUh|ryP Mn7WOFghcA>? MVXpcoR2[2W|IITo[UBieG:ydH;zbZPDqA>? NVPKbm14OjR4MUC4Nlc>
L1236 MVTBdI9xfG:|aYOgRZN{[Xl? NWfOUZBMOC9yLk[yOU8yNjJ3IN88US=> MonlOFghcA>? MX;pcoR2[2W|IITo[UBieG:ydH;zbZPDqA>? MUiyOFYyODh{Nx?=
SUPHD1 M3\JdmFxd3C2b4Ppd{BCe3OjeR?= NHTOPWMxNzBwNkK1M|EvOjVizszN M{PaNVQ5KGh? M3\tTolv\HWlZYOgeIhmKGGyb4D0c5Nqe8Li MkjPNlQ3OTB6Mke=
HDLM2 MWDBdI9xfG:|aYOgRZN{[Xl? NVzveIRGOC9yLk[yOU8yNjJ3IN88US=> MVK0PEBp Mki1bY5lfWOnczD0bIUh[XCxcITvd4l{yqB? M3zyVVI1PjFyOEK3
K1106P NELCT2hCeG:ydH;zbZMhSXO|YYm= NHfER44xNzBwNkK1M|EvOjVizszN Mo\SOFghcA>? MkjlbY5lfWOnczD0bIUh[XCxcITvd4l{yqB? NITDWoIzPDZzMEiyOy=>
L428 MnnjSpVv[3Srb36gRZN{[Xl? NEf5b5YxNTVizszN NInWbIMzPCCq MXTpcohq[mm2czDKRWszN1OWQWSgd4lodmGuaX7n M3TsRlI1PjFyOEK3
KMH2 NYLEeYFxTnWwY4Tpc44hSXO|YYm= MUKwMVUh|ryP NEnhe3YzPCCq M3O2VYlvcGmkaYTzJGpCUzJxU2TBWEB{cWewYXzpcoc> NEPPV|QzPDZzMEiyOy=>
L1236 M17kbWZ2dmO2aX;uJGF{e2G7 MVWwMVUh|ryP MknCNlQhcA>? NVjFXpRIcW6qaXLpeJMhUkGNMj;TWGFVKHOrZ37hcIlv\w>? M4P5XlI1PjFyOEK3
SUPHD1 NIjkd2JHfW6ldHnvckBCe3OjeR?= NHX1PJgxNTVizszN NX31V|g4OjRiaB?= M1ruO4lvcGmkaYTzJGpCUzJxU2TBWEB{cWewYXzpcoc> MWiyOFYyODh{Nx?=
HDLM2 MXfGeY5kfGmxbjDBd5NigQ>? MofVNE02KM7:TR?= NU[0SllFOjRiaB?= MlnSbY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> M2D5UFI1PjFyOEK3
K1106P MlnHSpVv[3Srb36gRZN{[Xl? MlizNE02KM7:TR?= MkflNlQhcA>? MnnqbY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> MlLJNlQ3OTB6Mke=
MM.1S  M1;1WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTFvMzFOwG0> MmG5NlQ2QDRzMEG=
TpoR JAK2 WT M4fQe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTFwNDCoNU4{6oDVMT61LUDPxE1? MXeyOFI2OTd7MB?=
TpoR JAK2 V617F MnXZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGK4dpJKSzVyPUCuPEApOC554pETNE46MSEQvF2= NX7peWRNOjR{NUG3PVA>
TpoR W515L NWTWWYs4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXuyTJVLUUN3ME2wMlghMDBwN,MAl|EvOClizszN NF7xc4MzPDJ3MUe5NC=>
Bcr-abl M17wU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmizTWM2OD1{LkegLFIvOuLCk{OuN{kh|ryP NXfwN4JyOjR{NUG3PVA>
JAK2 TW MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTqNIlKSzVyPUGuPEApOS534pETNk4{MSEQvF2= NYOwT|l{OjR{NUG3PVA>
JAK2 V617F NH;ETmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fsc2lEPTB;MD62JEgxNjckgKOwMlcqKM7:TR?= MmfoNlQzPTF5OUC=
MedB-1 NGLrSWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrvSIFJPCEQvF2= M1LPW|I1NzR6L{eyJIg> MVnEUXNQ MVvpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 MonLNlM5PTJ|Nk[=
K1106 M{Xvbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7KOEDPxE1? M3W0VVI1NzR6L{eyJIg> NVz6Vlh{TE2VTx?= MUXpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 NXPBNnBQOjN6NUKzOlY>
U2940 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXmb3U1KM7:TR?= NEezR3UzPC92OD:3NkBp MVPEUXNQ M2\xe4lvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> NYXK[4ZUOjN6NUKzOlY>
FE-PD MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXewMlA3Oy12IN88US=> MWXJR|UxRTlwNTFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? NUPNWnBjOjN|N{K2Olk>
HEL NILUO5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVKwMlA3Oy12IN88US=> M3e2OWlEPTB;MT61JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= MoDLNlM{PzJ4Nkm=
K-562 NUfjV2lsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTTTYMxNjB4Mz20JO69VQ>? NFS2WmpKSzVyPUKuOUDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= NXPwPJhoOjN|N{K2Olk>
L-82 MlrNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvuSmoxNjB4Mz20JO69VQ>? Mnr2TWM2OD1yLkm4JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= MUOyN|M4OjZ4OR?=
MAC-1 NHv0eJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUewMlA3Oy12IN88US=> MlrRTWM2OD1yLkWyJO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= NH7wc4IzOzN5Mk[2PS=>
MAC-2A NFj4N|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWiwMlA3Oy12IN88US=> MoPVTWM2OD1yLk[5JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= MmD0NlM{PzJ4Nkm=
MAC-2B MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXewMlA3Oy12IN88US=> MXnJR|UxRTBwNUSg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 NITpNZUzOzN5Mk[2PS=>
MY-LA Ml3lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XQZVAvODZ|LUSg{txO MVXJR|UxRTJwMTFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? Ml7mNlM{PzJ4Nkm=
NC-NC M4jnNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU[wMlA3Oy12IN88US=> NGPLb4tKSzVyPUGuNEDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= MWmyN|M4OjZ4OR?=
SE-AX NVi1SINjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHz0dmMxNjB4Mz20JO69VQ>? NGe3dmNKSzVyPUGuOUDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= M2LGPVI{Ozd{Nk[5
SR-786 NIX2Z2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmD0NE4xPjNvNDFOwG0> MkHlTWM2OD12Lk[g{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 MmHSNlM{PzJ4Nkm=
M-MOK  MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX2yOUDDvU4EoB?= MoO3NlQwPDhxN{KgbC=> Mlf6SG1UVw>? Mm\kbY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> M13RZVIyQDV|MUW3
HEL M3njSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTNyNTDuUS=> Mk\sNVg{QTR3NUS=
Ba/F3 JAK2V617F MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTJ5MDDuUS=> M1nIVFE5Ozl2NUW0

... 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 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 (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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID