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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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.

    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.

  • 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.

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 MXzBdI9xfG:|aYOgRZN{[Xl? MYqwMlUuOiEQvF2= MmTCNVIuPDhiaB?= MWLEUXNQ M2Tofolv\HWlZYOgZZBweHSxc3nzJIlvKGKxdHig[I9{\S1iYX7kJJRqdWVvIHTldIVv\GWwdDDtZY5v\XJ? NXy2bYNLOjV6NkmyNVA>
H1650 NGnPSYFCeG:ydH;zbZMhSXO|YYm= MWOwMlUuOiEQvF2= MYGxNk01QCCq MojWSG1UVw>? MljkbY5lfWOnczDhdI9xfG:|aYOgbY4h[m:2aDDkc5NmNSCjbnSgeIlu\S1iZHXw[Y5l\W62IH3hco5meg>? MknkNlU5Pjl{MUC=
H1975 MmTkSpVv[3Srb36gRZN{[Xl? NHq0N|kxNjJ3LUGg{txO NELvb44zPCCq NIfHSWJFVVOR M4DFWolvcGmkaYTzJIV5eHKnc4Ppc44hd2ZiYYDvdJRwe2m|LYLlcIF1\WRicILveIVqdiCEY3ytXGwtKEKlbD2yMEB{fXK4aY\pckwhYEmDUB?= M3zlRVI2QDZ7MkGw
H1650 NF3USWpHfW6ldHnvckBCe3OjeR?= NUDmNlVEOC5{NT2xJO69VQ>? MYCyOEBp NEPM[XJFVVOR M3S0XIlvcGmkaYTzJIV5eHKnc4Ppc44hd2ZiYYDvdJRwe2m|LYLlcIF1\WRicILveIVqdiCEY3ytXGwtKEKlbD2yMEB{fXK4aY\pckwhYEmDUB?= MXGyOVg3QTJzMB?=
H1975 Mkm5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXGxJO69VQ>? NXjlVoVYPDhiaB?= M3W1RWROW09? M{XwbJNmdnOrdHn6[ZMh[2WubIOgeI8hfGinIHP5eI91d3irY3n0fUBw\iCncnzveIlvcWJ? NEjoeoUzPTh4OUKxNC=>
H1650 Mmi4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfHNUDPxE1? NV\qZ2hXPDhiaB?= NUnLW2o6TE2VTx?= NI\l[mx{\W6|aYTpfoV{KGOnbHzzJJRwKHSqZTDjfZRwfG:6aXPpeJkhd2ZiZYLsc5Rqdmmk NGKwXYczPTh4OUKxNC=>
CD4+ T MVXGeY5kfGmxbjDBd5NigQ>? NGO2NGIxNjBzLUGg{txO MXG0PEBp M2LMWWROW09? MlzRdoVlfWOnczD0bIUheGixc4Doc5J6dGG2aX;uJIxmfmWuczDv[kBLSUt{IHHu[EBUXEGWM9Mg MWOyOVU4OjV|NR?=
Caco-2  M3zVXGZ2dmO2aX;uJGF{e2G7 MWqwMVEzOCEQvF2= NXHoXoJCPyCvaX6= MoTrbY5pcWKrdIOgeIhq[W2rbnWgeZB1[WunIIfpeIgh[W5iSVO1NOKhd2ZiMj6xxsDDvU1? MljDNlUxPjN4N{K=
Caco-2  NIm3TIhHfW6ldHnvckBCe3OjeR?= MlrONVAwPTBxMUCwJO69VQ>? NVnpN20yOiCq NWfMbVlb\GWlcnXhd4V{KHSqZTDmcJV5KG:oIGuzTH11cGmjbXnu[UBi[3Kxc4OgeIhmKG2xbn;sZZlmeiC5aYToJGlEPTBib3[gOk42yqEQvF2= MmXSNlUxPjN4N{K=
HEK293 MSR  M1j0XGZ2dmO2aX;uJGF{e2G7 M2\VPVAuOTBizszN NUjRVmo6PyCvaX6= M13pNYlvcGmkaYTzJIhVUFSUMjD3bZRpKGGwIFnDOVDDqG:oIEGuNuKhyrWP M{TOblI2ODZ|Nkey
MedB-1 MXXGeY5kfGmxbjDBd5NigQ>? M2K3Z|EwOiEQvF2= NGTGcZczPCCq NFr0O5Nl\WO{ZXHz[ZMhW1SDVE[gdIhwe3Cqb4L5cIF1cW:wIHPvcoNmdnS{YYTpc44h\GWyZX7k[Y51dHl? M{fkXVI1QTd5Nk[4
U2940 NYjBcFNXTnWwY4Tpc44hSXO|YYm= NYfwZ5ZzOS9{IN88US=> MmX5NlQhcA>? MkPr[IVkemWjc3XzJHNVSVR4IIDoc5NxcG:{eXzheIlwdiClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NF[3XXUzPDl5N{[2PC=>
K1106 NU\XdlFNTnWwY4Tpc44hSXO|YYm= NF31Z3YyNzJizszN MXiyOEBp MVPk[YNz\WG|ZYOgV3RCXDZicHjvd5Bpd3K7bHH0bY9vKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> MXuyOFk4PzZ4OB?=
K562 M1qwO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLyOZYxNTFizszN NWjZSlU2PzJiaB?= NHzNZ3VqdmirYnn0d{BMPTZ{IHPlcIwheHKxbHnm[ZJifGmxbjDheEBpcWeqIHPvcoNmdnS{YYTpc44> NGqxRW4zPDd5NUOwPC=>
MDA-MB-468  MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUOzJOK2VQ>? NYD6Nlh6PDhiaB?= M4r4U4VvcGGwY3XkJJNq[mOuNjDpcoR2[2WmIHzvd5Mhd2ZiY3XscEB3cWGkaXzpeJnDqA>? MnzvNlQ3PjJ6MUi=
MDA-MB-468 NEXOOVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknBNE01KM7:TR?= M3fL[|Q5KGh? MWDy[ZN2dHS|IIPp[45q\mmlYX70JIxwe3Nib3[geoli[mmuaYT5JINwdXCjcnXkJJRwKFKLLVLQTUBidG:wZR?= MXyyOFY3OjhzOB?=
L428 M3z2OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmqwNE02KM7:TR?= NIHT[lc1QCCq NVfZdXhncW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> NV71UYVqOjR4MUC4Nlc>
KMH2 MoPCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXmwMVUh|ryP NYnZRXJkPDhiaB?= M1vETIlvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= MXiyOFYyODh{Nx?=
L1236 M4rtSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fMfVAuPSEQvF2= NYr0NnVvPDhiaB?= NGDwcohqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 NGTMZpMzPDZzMEiyOy=>
SUPHD1 NIfPU3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzwVXExNTVizszN NGfUenU1QCCq M2SyeolvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= M3\VVVI1PjFyOEK3
HDLM2 M1;5VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXGwMVUh|ryP NYqyTnFDPDhiaB?= M2jhSIlvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= MYOyOFYyODh{Nx?=
K1106P MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVywMVUh|ryP MVy0PEBp NEX0NWtqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 M1zDdVI1PjFyOEK3
L428 Mn7qRZBweHSxc3nzJGF{e2G7 M4jNOlAwOC54MkWvNU4zPSEQvF2= M1TsR|Q5KGh? MVzpcoR2[2W|IITo[UBieG:ydH;zbZPDqA>? MWqyOFYyODh{Nx?=
KMH2 Ml7jRZBweHSxc3nzJGF{e2G7 MU[wM|AvPjJ3L{GuNlUh|ryP Mn\UOFghcA>? NUHHeJJ5cW6mdXPld{B1cGViYYDvdJRwe2m|wrC= M1XRSlI1PjFyOEK3
L1236 NV7WOIMySXCxcITvd4l{KEG|c3H5 NVHBRY9COC9yLk[yOU8yNjJ3IN88US=> M1TjdlQ5KGh? NUnxWXRDcW6mdXPld{B1cGViYYDvdJRwe2m|wrC= NXP4SlhvOjR4MUC4Nlc>
SUPHD1 MorQRZBweHSxc3nzJGF{e2G7 NVXnOmp3OC9yLk[yOU8yNjJ3IN88US=> NWPsOnRrPDhiaB?= NWHQfXNVcW6mdXPld{B1cGViYYDvdJRwe2m|wrC= MYqyOFYyODh{Nx?=
HDLM2 NGHHdFVCeG:ydH;zbZMhSXO|YYm= NI\pdmsxNzBwNkK1M|EvOjVizszN M1v4U|Q5KGh? NXjTWW1VcW6mdXPld{B1cGViYYDvdJRwe2m|wrC= MkmwNlQ3OTB6Mke=
K1106P MkLpRZBweHSxc3nzJGF{e2G7 NGPUPXcxNzBwNkK1M|EvOjVizszN NVjY[Jp3PDhiaB?= NIfUeJdqdmS3Y3XzJJRp\SCjcH;weI9{cXQEoB?= MlnBNlQ3OTB6Mke=
L428 MYLGeY5kfGmxbjDBd5NigQ>? NVXUTVd3OC13IN88US=> NH7PTJAzPCCq Mk\pbY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> MoLmNlQ3OTB6Mke=
KMH2 M{HWU2Z2dmO2aX;uJGF{e2G7 NFn1PXQxNTVizszN M1zUZVI1KGh? Mn\nbY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> NFPmVXgzPDZzMEiyOy=>
L1236 MlvhSpVv[3Srb36gRZN{[Xl? M{LvTlAuPSEQvF2= MmH2NlQhcA>? Mn3obY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> NX3NTmRlOjR4MUC4Nlc>
SUPHD1 Mly2SpVv[3Srb36gRZN{[Xl? M4[2fFAuPSEQvF2= MVKyOEBp MnXObY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> MUKyOFYyODh{Nx?=
HDLM2 NFnuSYpHfW6ldHnvckBCe3OjeR?= NWT2OYxHOC13IN88US=> M1nZWFI1KGh? MoLibY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> Mo\RNlQ3OTB6Mke=
K1106P NXWyc4ExTnWwY4Tpc44hSXO|YYm= NEjnS2cxNTVizszN MVqyOEBp MmnMbY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> MUiyOFYyODh{Nx?=
MM.1S  NX:wU2NOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{SybmlEPTB;MT2zJO69VQ>? NEDXR4MzPDV6NEGwNS=>
TpoR JAK2 WT NIewT2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{m4S2lEPTB;MT60JEgyNjQkgKOxMlUqKM7:TR?= MV[yOFI2OTd7MB?=
TpoR JAK2 V617F NIPNToVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonVTWM2OD1yLkigLFAvP+LCk{CuPUkh|ryP MmXlNlQzPTF5OUC=
TpoR W515L NEC1dHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnSdJlXUUN3ME2wMlghMDBwN,MAl|EvOClizszN NIThXI8zPDJ3MUe5NC=>
Bcr-abl M1K3Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTJwNzCoNk4z6oDVMz6zLUDPxE1? M2nGUlI1OjVzN{mw
JAK2 TW MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPETWM2OD1zLkigLFEvPeLCk{KuN{kh|ryP NYTSRZJxOjR{NUG3PVA>
JAK2 V617F NFvvTWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{i5dWlEPTB;MD62JEgxNjckgKOwMlcqKM7:TR?= Ml6xNlQzPTF5OUC=
MedB-1 MoTIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\wOlMxPCEQvF2= Mmn5NlQwPDhxN{KgbC=> NWnsW2V7TE2VTx?= M4XzUIlvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> MmPmNlM5PTJ|Nk[=
K1106 NEDvNnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4CycFQh|ryP NYHPRWx{OjRxNEivO|IhcA>? NELscGtFVVOR NYH5dI9TcW6qaXLpeJMh[2WubDDndo94fGhidHnt[UBl\XCnbnTlcpRtgQ>? NGfHe48zOzh3MkO2Oi=>
U2940 NFy4T2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3[0[lQh|ryP MXGyOE81QC95MjDo NYnrZWp5TE2VTx?= MmXJbY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> M3Ly[|I{QDV{M{[2
FE-PD MlfiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonoNE4xPjNvNDFOwG0> MkfLTWM2OD17LkWg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 NXXxV|BJOjN|N{K2Olk>
HEL MlmzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXywMlA3Oy12IN88US=> M1fsbWlEPTB;MT61JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= NUjDdoxVOjN|N{K2Olk>
K-562 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLFeWlVOC5yNkOtOEDPxE1? MUDJR|UxRTJwNTFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? MW[yN|M4OjZ4OR?=
L-82 M3uxXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVKwMlA3Oy12IN88US=> MlmyTWM2OD1yLkm4JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= NGDkbJozOzN5Mk[2PS=>
MAC-1 NUHNXZJOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWmwMlA3Oy12IN88US=> NFTheo1KSzVyPUCuOVIh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NITPZYgzOzN5Mk[2PS=>
MAC-2A NFzJS|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUWwMlA3Oy12IN88US=> MWLJR|UxRTBwNkmg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 Ml3uNlM{PzJ4Nkm=
MAC-2B NGfR[oZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIi1[GsxNjB4Mz20JO69VQ>? M1OwZ2lEPTB;MD61OEDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= NX7pPJNCOjN|N{K2Olk>
MY-LA M{nKWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPWNE4xPjNvNDFOwG0> MX\JR|UxRTJwMTFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? NFXqT2czOzN5Mk[2PS=>
NC-NC NV:1U4hwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTGNE4xPjNvNDFOwG0> Mn3yTWM2OD1zLkCg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 NWL0co9oOjN|N{K2Olk>
SE-AX NIO4XZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTPW3EyOC5yNkOtOEDPxE1? NH:wepdKSzVyPUGuOUDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= NUXJVmI6OjN|N{K2Olk>
SR-786 NVPxTmZnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojaNE4xPjNvNDFOwG0> NF3XeWRKSzVyPUSuOkDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= M4HpfVI{Ozd{Nk[5
M-MOK  MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fFUFI2KML3TdMg MViyOE81QC95MjDo MmXmSG1UVw>? MYfpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 NXzTNVQ3OjF6NUOxOVc>
HEL Mny2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;BeGJlUUN3ME2zNFUhdk1? MWSxPFM6PDV3NB?=
Ba/F3 JAK2V617F MlvXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHe0VZVKSzVyPUK3NEBvVQ>? NH\ySVAyQDN7NEW1OC=>

... 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 individually and in order:
1% DMSO+30% polyethylene glycol+1% Tween 80
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
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
NCT01836705 Completed Neoplasm Malignant Sanofi May 2013 Phase 1
NCT01762462 Completed Hepatic Impairment Sanofi December 2012 Phase 1
NCT01763190 Completed Renal Impairment Sanofi November 2012 Phase 1
NCT01692366 Completed Myelofibrosis Sanofi November 2012 Phase 2
NCT01585623 Completed Solid Tumor Sanofi June 2012 Phase 1
NCT01523171 Completed 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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID