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 M{jkZWFxd3C2b4Ppd{BCe3OjeR?= M3fvfVAvPS1{IN88US=> MUSxNk01QCCq MVvEUXNQ NV3D[ndscW6mdXPld{BieG:ydH;zbZMhcW5iYn;0bEBld3OnLTDhcoQhfGmvZT2g[IVx\W6mZX70JI1idm6nch?= M1fx[FI2QDZ7MkGw
H1650 NH3H[FVCeG:ydH;zbZMhSXO|YYm= MXOwMlUuOiEQvF2= MnHCNVIuPDhiaB?= MUDEUXNQ Ml7SbY5lfWOnczDhdI9xfG:|aYOgbY4h[m:2aDDkc5NmNSCjbnSgeIlu\S1iZHXw[Y5l\W62IH3hco5meg>? NXnPTIFkOjV6NkmyNVA>
H1975 MmjVSpVv[3Srb36gRZN{[Xl? MV:wMlI2NTFizszN M3eyOlI1KGh? NIj2PGdFVVOR NFXLNoJqdmirYnn0d{BmgHC{ZYPzbY9vKG:oIHHwc5B1d3Orcz3y[YxifGWmIIDyc5RmcW5iQnPsMXhNNCCEY3ytNkwhe3W{dnn2bY4tKFiLQWC= NXjwSGtKOjV6NkmyNVA>
H1650 MVfGeY5kfGmxbjDBd5NigQ>? MX:wMlI2NTFizszN NELGdFQzPCCq MWjEUXNQ MXnpcohq[mm2czDlfJBz\XO|aX;uJI9nKGGyb4D0c5Nqey2{ZXzheIVlKHC{b4TlbY4hSmOuLWjMMEBD[2xvMjygd5Vzfmm4aX6sJHhKSVB? NV[4SmJrOjV6NkmyNVA>
H1975 Mn\1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTPNUDPxE1? M{DuVFQ5KGh? NWe2WoZtTE2VTx?= NE[y[WN{\W6|aYTpfoV{KGOnbHzzJJRwKHSqZTDjfZRwfG:6aXPpeJkhd2ZiZYLsc5Rqdmmk MVGyOVg3QTJzMB?=
H1650 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DvWlEh|ryP MkTBOFghcA>? MYXEUXNQ M1Hr[pNmdnOrdHn6[ZMh[2WubIOgeI8hfGinIHP5eI91d3irY3n0fUBw\iCncnzveIlvcWJ? NHT0dHYzPTh4OUKxNC=>
CD4+ T M3qyOGZ2dmO2aX;uJGF{e2G7 M1TxOlAvODFvMTFOwG0> MkT3OFghcA>? MXzEUXNQ NUX6PVQ5emWmdXPld{B1cGVicHjvd5Bpd3K7bHH0bY9vKGyndnXsd{Bw\iCMQVuyJIFv\CCVVFHUN:Kh M2r2VVI2PTd{NUO1
Caco-2  NGS3fI1HfW6ldHnvckBCe3OjeR?= MXOwMVEzOCEQvF2= M2jVe|chdWmw NH;CXIhqdmirYnn0d{B1cGmjbXnu[UB2eHSja3Wge4l1cCCjbjDJR|UxyqCxZjCyMlHDqML3TR?= M1XiVlI2ODZ|Nkey
Caco-2  M362T2Z2dmO2aX;uJGF{e2G7 NGqwOHIyOC93MD:xNFAh|ryP Mn3xNkBp MVjk[YNz\WG|ZYOgeIhmKG[udYigc4YhYzOKXYTobYFucW6nIHHjdo9{eyC2aHWgcY9vd2yjeXXyJJdqfGhiSVO1NEBw\iB4LkZCpO69VQ>? NXu5[ZJoOjVyNkO2O|I>
HEK293 MSR  NHHjdGVHfW6ldHnvckBCe3OjeR?= M2TOcFAuOTBizszN MYK3JI1qdg>? NGm1TI1qdmirYnn0d{BpXEiWUkKge4l1cCCjbjDJR|UxyqCxZjCxMlLDqML3TR?= MVOyOVA3OzZ5Mh?=
MedB-1 M3e3dGZ2dmO2aX;uJGF{e2G7 M1uzN|EwOiEQvF2= NFPhcXQzPCCq NHH1b|Nl\WO{ZXHz[ZMhW1SDVE[gdIhwe3Cqb4L5cIF1cW:wIHPvcoNmdnS{YYTpc44h\GWyZX7k[Y51dHl? Mm\GNlQ6Pzd4Nki=
U2940 MoG5SpVv[3Srb36gRZN{[Xl? MWCxM|Ih|ryP MUWyOEBp NXLIXFN[\GWlcnXhd4V{KFOWQWS2JJBpd3OyaH;yfYxifGmxbjDjc45k\W62cnH0bY9vKGSncHXu[IVvfGy7 NE\MbIUzPDl5N{[2PC=>
K1106 M2C2cWZ2dmO2aX;uJGF{e2G7 Mom4NU8zKM7:TR?= NVrqW4JWOjRiaB?= NY[2e4Vn\GWlcnXhd4V{KFOWQWS2JJBpd3OyaH;yfYxifGmxbjDjc45k\W62cnH0bY9vKGSncHXu[IVvfGy7 NFnLS2gzPDl5N{[2PC=>
K562 MlvHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXmwMVEh|ryP MkTuO|IhcA>? MULpcohq[mm2czDLOVYzKGOnbHygdJJwdGmoZYLheIlwdiCjdDDobYdpKGOxbnPlcpRz[XSrb36= Mkm5NlQ4PzV|MEi=
MDA-MB-468  MmrrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUSzJOK2VQ>? MlzSOFghcA>? MY\lcohidmOnZDDzbYJkdDZiaX7keYNm\CCub4PzJI9nKGOnbHygeoli[mmuaYT5xsA> MkXBNlQ3PjJ6MUi=
MDA-MB-468 MlKwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvzNE01KM7:TR?= NFjuZXQ1QCCq NFvZWVVz\XO3bITzJJNq\26rZnnjZY51KGyxc4Ogc4YhfmmjYnnsbZR6KGOxbYDhdoVlKHSxIGLJMWJRUSCjbH;u[S=> MVGyOFY3OjhzOB?=
L428 M3j4RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHvfmIxNTVizszN MXe0PEBp M2PFV4lvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= Mn;aNlQ3OTB6Mke=
KMH2 NHy0SotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELXUmsxNTVizszN NV3hfFZ4PDhiaB?= MWLpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 NVf3Z|c5OjR4MUC4Nlc>
L1236 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHGN4oyOC13IN88US=> MkTrOFghcA>? M4\hNolvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= Mof5NlQ3OTB6Mke=
SUPHD1 NIi3OHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33VO|AuPSEQvF2= M1HXe|Q5KGh? MXHpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 MYKyOFYyODh{Nx?=
HDLM2 MoKwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrrcGV2OC13IN88US=> M1HJcVQ5KGh? NXTFUFF2cW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> MmrONlQ3OTB6Mke=
K1106P NGDaW3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVr6RoY{OC13IN88US=> Mof4OFghcA>? Mne1bY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= NVG4cJJQOjR4MUC4Nlc>
L428 Mn3yRZBweHSxc3nzJGF{e2G7 Mm\3NE8xNjZ{NT:xMlI2KM7:TR?= NX\SblJUPDhiaB?= MYjpcoR2[2W|IITo[UBieG:ydH;zbZPDqA>? MoG1NlQ3OTB6Mke=
KMH2 MX;BdI9xfG:|aYOgRZN{[Xl? NYjtUYN5OC9yLk[yOU8yNjJ3IN88US=> NGriW4M1QCCq M1T4Tolv\HWlZYOgeIhmKGGyb4D0c5Nqe8Li NILwbYQzPDZzMEiyOy=>
L1236 NUDp[5VISXCxcITvd4l{KEG|c3H5 NV\1TlNPOC9yLk[yOU8yNjJ3IN88US=> NInMbYo1QCCq M4XDVIlv\HWlZYOgeIhmKGGyb4D0c5Nqe8Li NWPmU4M5OjR4MUC4Nlc>
SUPHD1 MXvBdI9xfG:|aYOgRZN{[Xl? MXGwM|AvPjJ3L{GuNlUh|ryP MUi0PEBp MV3pcoR2[2W|IITo[UBieG:ydH;zbZPDqA>? MXKyOFYyODh{Nx?=
HDLM2 MUXBdI9xfG:|aYOgRZN{[Xl? NUfUUnJKOC9yLk[yOU8yNjJ3IN88US=> MXO0PEBp NELWW4JqdmS3Y3XzJJRp\SCjcH;weI9{cXQEoB?= NWj5c4VlOjR4MUC4Nlc>
K1106P MW\BdI9xfG:|aYOgRZN{[Xl? M{T3[VAwOC54MkWvNU4zPSEQvF2= M1HsZ|Q5KGh? NInRTJZqdmS3Y3XzJJRp\SCjcH;weI9{cXQEoB?= MYiyOFYyODh{Nx?=
L428 NXvoS4lLTnWwY4Tpc44hSXO|YYm= MnfmNE02KM7:TR?= NEi3cW4zPCCq M{fmVolvcGmkaYTzJGpCUzJxU2TBWEB{cWewYXzpcoc> NUOwNlh2OjR4MUC4Nlc>
KMH2 M{n1ZWZ2dmO2aX;uJGF{e2G7 MUiwMVUh|ryP NFmzSXEzPCCq NFnuUm9qdmirYnn0d{BLSUt{L2PURXQhe2mpbnHsbY5o NHzFUWkzPDZzMEiyOy=>
L1236 M4TH[WZ2dmO2aX;uJGF{e2G7 M1fjfFAuPSEQvF2= NXnUVJpYOjRiaB?= NHr4dJlqdmirYnn0d{BLSUt{L2PURXQhe2mpbnHsbY5o MUWyOFYyODh{Nx?=
SUPHD1 NVrUd5prTnWwY4Tpc44hSXO|YYm= MoWyNE02KM7:TR?= NUfF[IVoOjRiaB?= MoXvbY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> MYWyOFYyODh{Nx?=
HDLM2 Mn;vSpVv[3Srb36gRZN{[Xl? NH;6fGExNTVizszN NWHVUoZDOjRiaB?= MnzHbY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> MoPCNlQ3OTB6Mke=
K1106P Mn;tSpVv[3Srb36gRZN{[Xl? M4ruPFAuPSEQvF2= NYfhRottOjRiaB?= M1W1UIlvcGmkaYTzJGpCUzJxU2TBWEB{cWewYXzpcoc> MUiyOFYyODh{Nx?=
MM.1S  NYDiTI9yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTFvMzFOwG0> Ml;xNlQ2QDRzMEG=
TpoR JAK2 WT NVzBRVFjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzQbXJGUUN3ME2xMlQhMDFwM,MAl|EvPSlizszN NXzIVWp6OjR{NUG3PVA>
TpoR JAK2 V617F MkTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLuTWM2OD1yLkigLFAvP+LCk{CuPUkh|ryP MVqyOFI2OTd7MB?=
TpoR W515L NVTNUZN2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGm0XnhKSzVyPUCuPEApOC554pETNU4xMSEQvF2= MWqyOFI2OTd7MB?=
Bcr-abl MnLHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1u4WGlEPTB;Mj63JEgzNjMkgKOzMlMqKM7:TR?= NWn2[|dLOjR{NUG3PVA>
JAK2 TW M1ezcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHTcFJKSzVyPUGuPEApOS534pETNk4{MSEQvF2= NVnhfpZtOjR{NUG3PVA>
JAK2 V617F MnLpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGLpOVZKSzVyPUCuOkApOC544pETNE44MSEQvF2= NYS2RmI4OjR{NUG3PVA>
MedB-1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXK0JO69VQ>? NFHVOVQzPC92OD:3NkBp M1nNTmROW09? NGLYSFJqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 NGjYXpczOzh3MkO2Oi=>
K1106 NIrq[Y1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjqNpZUPCEQvF2= MnzDNlQwPDhxN{KgbC=> MV7EUXNQ MVTpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 NUnuS3VKOjN6NUKzOlY>
U2940 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LaOFQh|ryP NF;CNoozPC92OD:3NkBp M3P4RmROW09? MkLpbY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> M3zaUVI{QDV{M{[2
FE-PD M{HRXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvENE4xPjNvNDFOwG0> Mlq3TWM2OD17LkWg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 NIXNXHkzOzN5Mk[2PS=>
HEL M1THcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjZU5oxNjB4Mz20JO69VQ>? M2jEOGlEPTB;MT61JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= M2HQVFI{Ozd{Nk[5
K-562 M4XLR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mkf5NE4xPjNvNDFOwG0> M4fLcWlEPTB;Mj61JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= NHP1OXgzOzN5Mk[2PS=>
L-82 MlTJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUGwMlA3Oy12IN88US=> NIHZRZBKSzVyPUCuPVgh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NVi3S5FCOjN|N{K2Olk>
MAC-1 NX3uWlF4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHubVV3OC5yNkOtOEDPxE1? MlHkTWM2OD1yLkWyJO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= M4foVFI{Ozd{Nk[5
MAC-2A NFG3eo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\XPFAvODZ|LUSg{txO M1\sS2lEPTB;MD62PUDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= M2roV|I{Ozd{Nk[5
MAC-2B M3TCPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXOwMlA3Oy12IN88US=> NYD0dIJYUUN3ME2wMlU1KM7:TTygbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NHTxd5QzOzN5Mk[2PS=>
MY-LA NHTIVYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XL[lAvODZ|LUSg{txO NYniSI96UUN3ME2yMlEh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MVWyN|M4OjZ4OR?=
NC-NC NEPTWGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnnd5ZoOC5yNkOtOEDPxE1? M1juS2lEPTB;MT6wJO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= M1z5bVI{Ozd{Nk[5
SE-AX M1nxV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXmwMlA3Oy12IN88US=> NEO1SoNKSzVyPUGuOUDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= NE\yPY8zOzN5Mk[2PS=>
SR-786 MmLrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXSTVFQOC5yNkOtOEDPxE1? M{LFc2lEPTB;ND62JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= M17zeFI{Ozd{Nk[5
M-MOK  NWPudZozT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWWyOUDDvU4EoB?= MnHkNlQwPDhxN{KgbC=> NWjHeW94TE2VTx?= NWfhdIVIcW6qaXLpeJMh[2WubDDndo94fGhidHnt[UBl\XCnbnTlcpRtgQ>? MojENlE5PTNzNUe=
HEL Mkf6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfoTWM2OD1|MEWgcm0> MXSxPFM6PDV3NB?=
Ba/F3 JAK2V617F M{HzR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrjTWM2OD1{N{Cgcm0> Ml\rNVg{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
  • 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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