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.

Size Price Stock Quantity  
In DMSO USD 220 In stock
USD 110 In stock
USD 170 In stock
USD 370 In stock
USD 570 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

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 M1XuZWFxd3C2b4Ppd{BCe3OjeR?= M3vtelAvPS1{IN88US=> M2q5fVEzNTR6IHi= MXnEUXNQ NInRdIVqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCkb4ToJIRwe2VvIHHu[EB1cW2nLTDk[ZBmdmSnboSgcYFvdmW{ NGnZUW8zPTh4OUKxNC=>
H1650 MXLBdI9xfG:|aYOgRZN{[Xl? MWiwMlUuOiEQvF2= MkK2NVIuPDhiaB?= NXfG[WtYTE2VTx?= M1jDSYlv\HWlZYOgZZBweHSxc3nzJIlvKGKxdHig[I9{\S1iYX7kJJRqdWVvIHTldIVv\GWwdDDtZY5v\XJ? MUWyOVg3QTJzMB?=
H1975 M4DN[2Z2dmO2aX;uJGF{e2G7 MkO2NE4zPS1zIN88US=> NFy0[JUzPCCq MX3EUXNQ NHTSUYJqdmirYnn0d{BmgHC{ZYPzbY9vKG:oIHHwc5B1d3Orcz3y[YxifGWmIIDyc5RmcW5iQnPsMXhNNCCEY3ytNkwhe3W{dnn2bY4tKFiLQWC= NIjBT|gzPTh4OUKxNC=>
H1650 NUGwVnhZTnWwY4Tpc44hSXO|YYm= MkK3NE4zPS1zIN88US=> NEXrT4MzPCCq NHLRbW9FVVOR MYPpcohq[mm2czDlfJBz\XO|aX;uJI9nKGGyb4D0c5Nqey2{ZXzheIVlKHC{b4TlbY4hSmOuLWjMMEBD[2xvMjygd5Vzfmm4aX6sJHhKSVB? M1XTe|I2QDZ7MkGw
H1975 M3z2UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEK0VJUyKM7:TR?= M{XGflQ5KGh? M3vWWWROW09? M1:zZ5NmdnOrdHn6[ZMh[2WubIOgeI8hfGinIHP5eI91d3irY3n0fUBw\iCncnzveIlvcWJ? NYnWXoRjOjV6NkmyNVA>
H1650 M2LJe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlraNUDPxE1? NUL3RY5HPDhiaB?= NGPne5NFVVOR Mk\Zd4Vve2m2aYrld{Bk\WyuczD0c{B1cGViY4n0c5RwgGmlaYT5JI9nKGW{bH;0bY5q[g>? NF7QPZkzPTh4OUKxNC=>
CD4+ T Ml\BSpVv[3Srb36gRZN{[Xl? MmL1NE4xOS1zIN88US=> NHnhOHI1QCCq NUf3PXNWTE2VTx?= NVnvOI4{emWmdXPld{B1cGVicHjvd5Bpd3K7bHH0bY9vKGyndnXsd{Bw\iCMQVuyJIFv\CCVVFHUN:Kh M{HTXFI2PTd{NUO1
Caco-2  NXrtbm41TnWwY4Tpc44hSXO|YYm= Ml;5NE0yOjBizszN MU[3JI1qdg>? NEHVNGRqdmirYnn0d{B1cGmjbXnu[UB2eHSja3Wge4l1cCCjbjDJR|UxyqCxZjCyMlHDqML3TR?= Mnj0NlUxPjN4N{K=
Caco-2  M{PGd2Z2dmO2aX;uJGF{e2G7 NI\ue5oyOC93MD:xNFAh|ryP M13C[|IhcA>? MVPk[YNz\WG|ZYOgeIhmKG[udYigc4YhYzOKXYTobYFucW6nIHHjdo9{eyC2aHWgcY9vd2yjeXXyJJdqfGhiSVO1NEBw\iB4LkZCpO69VQ>? MnzzNlUxPjN4N{K=
HEK293 MSR  MVPGeY5kfGmxbjDBd5NigQ>? MX6wMVExKM7:TR?= M3T4UlchdWmw NU\pe3M{cW6qaXLpeJMhcFSKVGKyJJdqfGhiYX6gTWM2OMLib3[gNU4zyqEEtV2= MlSxNlUxPjN4N{K=
MedB-1 MojJSpVv[3Srb36gRZN{[Xl? MWmxM|Ih|ryP M13hc|I1KGh? MX\k[YNz\WG|ZYOgV3RCXDZicHjvd5Bpd3K7bHH0bY9vKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> NWPKZ3R[OjR7N{e2Olg>
U2940 MXXGeY5kfGmxbjDBd5NigQ>? NInkNWQyNzJizszN NUnZPW5tOjRiaB?= NES0dm1l\WO{ZXHz[ZMhW1SDVE[gdIhwe3Cqb4L5cIF1cW:wIHPvcoNmdnS{YYTpc44h\GWyZX7k[Y51dHl? NFH3eGgzPDl5N{[2PC=>
K1106 MULGeY5kfGmxbjDBd5NigQ>? NYjn[YREOS9{IN88US=> M1nyc|I1KGh? MoHP[IVkemWjc3XzJHNVSVR4IIDoc5NxcG:{eXzheIlwdiClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 MlHTNlQ6Pzd4Nki=
K562 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYOwMVEh|ryP NVH6V3BVPzJiaB?= NWHEU|lkcW6qaXLpeJMhUzV4MjDj[YxtKHC{b3zp[oVz[XSrb36gZZQhcGmpaDDjc45k\W62cnH0bY9v NIrrUlkzPDd5NUOwPC=>
MDA-MB-468  NYWzWVVtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX:zJOK2VQ>? NHfnc4k1QCCq MUPlcohidmOnZDDzbYJkdDZiaX7keYNm\CCub4PzJI9nKGOnbHygeoli[mmuaYT5xsA> NWnNPG1COjR4NkK4NVg>
MDA-MB-468 NGewV|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnTnNE01KM7:TR?= MmjQOFghcA>? M134UJJme3WudIOgd4lodmmoaXPhcpQhdG:|czDv[kB3cWGkaXzpeJkh[2:vcHHy[YQhfG9iUlmtRnBKKGGub37l NY\hWlJ5OjR4NkK4NVg>
L428 Mn\XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWKwMVUh|ryP MUK0PEBp MVPpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 MWGyOFYyODh{Nx?=
KMH2 NFOyNplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17SUFAuPSEQvF2= NE\QO2I1QCCq MmTabY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= M4fyblI1PjFyOEK3
L1236 NUjOPXdQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13ucVAuPSEQvF2= MmXwOFghcA>? MkjUbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= MXeyOFYyODh{Nx?=
SUPHD1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HlOVAuPSEQvF2= M3jHflQ5KGh? MlrPbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= MXyyOFYyODh{Nx?=
HDLM2 M{jXfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrvdo57OC13IN88US=> NHe2R2c1QCCq MXLpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 M2f2XVI1PjFyOEK3
K1106P NYfPeZRsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnL4NE02KM7:TR?= NHzkOng1QCCq M3XkPYlvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= M3jhZ|I1PjFyOEK3
L428 NYHKXXk5SXCxcITvd4l{KEG|c3H5 NEXLWYsxNzBwNkK1M|EvOjVizszN NWrqb2MzPDhiaB?= MYrpcoR2[2W|IITo[UBieG:ydH;zbZPDqA>? NUL2PZRPOjR4MUC4Nlc>
KMH2 Mne5RZBweHSxc3nzJGF{e2G7 MoHFNE8xNjZ{NT:xMlI2KM7:TR?= NX\MWIhyPDhiaB?= NIW5dnJqdmS3Y3XzJJRp\SCjcH;weI9{cXQEoB?= M4\4WlI1PjFyOEK3
L1236 NUDsSJY{SXCxcITvd4l{KEG|c3H5 NGfFUXUxNzBwNkK1M|EvOjVizszN NYLOVopGPDhiaB?= M1\mb4lv\HWlZYOgeIhmKGGyb4D0c5Nqe8Li NUm2RYQyOjR4MUC4Nlc>
SUPHD1 NWHqNYI{SXCxcITvd4l{KEG|c3H5 NGPQcXIxNzBwNkK1M|EvOjVizszN MljVOFghcA>? MX3pcoR2[2W|IITo[UBieG:ydH;zbZPDqA>? MUeyOFYyODh{Nx?=
HDLM2 M3noeGFxd3C2b4Ppd{BCe3OjeR?= M{DxW|AwOC54MkWvNU4zPSEQvF2= MYO0PEBp Mle5bY5lfWOnczD0bIUh[XCxcITvd4l{yqB? NFLNNHMzPDZzMEiyOy=>
K1106P NHL4XW9CeG:ydH;zbZMhSXO|YYm= MViwM|AvPjJ3L{GuNlUh|ryP M3nkNlQ5KGh? MYHpcoR2[2W|IITo[UBieG:ydH;zbZPDqA>? MlyyNlQ3OTB6Mke=
L428 NYroO202TnWwY4Tpc44hSXO|YYm= M3PFRVAuPSEQvF2= MYeyOEBp MULpcohq[mm2czDKRWszN1OWQWSgd4lodmGuaX7n NHG2Z44zPDZzMEiyOy=>
KMH2 MYHGeY5kfGmxbjDBd5NigQ>? NE\oeWUxNTVizszN NIjwXWMzPCCq M4XJb4lvcGmkaYTzJGpCUzJxU2TBWEB{cWewYXzpcoc> MUSyOFYyODh{Nx?=
L1236 MWXGeY5kfGmxbjDBd5NigQ>? M1nOSFAuPSEQvF2= MX[yOEBp M4[0SIlvcGmkaYTzJGpCUzJxU2TBWEB{cWewYXzpcoc> MmfjNlQ3OTB6Mke=
SUPHD1 MkW3SpVv[3Srb36gRZN{[Xl? M4jHVlAuPSEQvF2= NXjhXYljOjRiaB?= MUfpcohq[mm2czDKRWszN1OWQWSgd4lodmGuaX7n NHTjc2IzPDZzMEiyOy=>
HDLM2 M1HWXmZ2dmO2aX;uJGF{e2G7 NIHnO|cxNTVizszN NUHMbIt5OjRiaB?= NVTjOHdOcW6qaXLpeJMhUkGNMj;TWGFVKHOrZ37hcIlv\w>? M37leFI1PjFyOEK3
K1106P MWjGeY5kfGmxbjDBd5NigQ>? NEHFOVAxNTVizszN NH73[pYzPCCq M1PQcYlvcGmkaYTzJGpCUzJxU2TBWEB{cWewYXzpcoc> M3nSd|I1PjFyOEK3
MM.1S  MnfvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTFvMzFOwG0> MX2yOFU5PDFyMR?=
TpoR JAK2 WT M4H3fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTFwNDCoNU4{6oDVMT61LUDPxE1? NIT6SlkzPDJ3MUe5NC=>
TpoR JAK2 V617F NGPITlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIO0cW1KSzVyPUCuPEApOC554pETNE46MSEQvF2= M2XMPVI1OjVzN{mw
TpoR W515L MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fmUWlEPTB;MD64JEgxNjgkgKOxMlAqKM7:TR?= M{fnVVI1OjVzN{mw
Bcr-abl MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkC2TWM2OD1{LkegLFIvOuLCk{OuN{kh|ryP NXvyZVdFOjR{NUG3PVA>
JAK2 TW NFjKS2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvuXY9pUUN3ME2xMlghMDFwNfMAl|IvOylizszN M1zsUVI1OjVzN{mw
JAK2 V617F NVXTfWYzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFq3OVNKSzVyPUCuOkApOC544pETNE44MSEQvF2= NXjYVYNuOjR{NUG3PVA>
MedB-1 M3W2R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPmRoM1KM7:TR?= NF7pSZIzPC92OD:3NkBp MVHEUXNQ M{HxN4lvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> MY[yN|g2OjN4Nh?=
K1106 M1TGTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LVNFQh|ryP MWmyOE81QC95MjDo Ml\FSG1UVw>? MVjpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 MnK3NlM5PTJ|Nk[=
U2940 NUKzWXQ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGWwNVc1KM7:TR?= NHfIRW8zPC92OD:3NkBp NXTONohnTE2VTx?= MmjVbY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> MnnWNlM5PTJ|Nk[=
FE-PD MoPtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV2wMlA3Oy12IN88US=> MUPJR|UxRTlwNTFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? NG\6NGYzOzN5Mk[2PS=>
HEL NGO2WlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWSwMlA3Oy12IN88US=> MV3JR|UxRTFwNTFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? MXiyN|M4OjZ4OR?=
K-562 NEnkcWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVewMlA3Oy12IN88US=> MXjJR|UxRTJwNTFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? M{HjWFI{Ozd{Nk[5
L-82 MmO3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLaNE4xPjNvNDFOwG0> NH\VT3ZKSzVyPUCuPVgh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MmPyNlM{PzJ4Nkm=
MAC-1 NUC3W4JLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PNWlAvODZ|LUSg{txO M1HRNmlEPTB;MD61NkDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= M1L2SlI{Ozd{Nk[5
MAC-2A MnjJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXKwMlA3Oy12IN88US=> NIi3dW9KSzVyPUCuOlkh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MnT1NlM{PzJ4Nkm=
MAC-2B MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrL[GIxNjB4Mz20JO69VQ>? MnnNTWM2OD1yLkW0JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= M1LqNlI{Ozd{Nk[5
MY-LA NFrDT3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLZbYYxNjB4Mz20JO69VQ>? Mn;mTWM2OD1{LkGg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 NYXnbIRNOjN|N{K2Olk>
NC-NC MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXmwMlA3Oy12IN88US=> MkHmTWM2OD1zLkCg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 NHuyVWIzOzN5Mk[2PS=>
SE-AX NFnWPIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2HSclAvODZ|LUSg{txO MYrJR|UxRTFwNTFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? NYjGb2FCOjN|N{K2Olk>
SR-786 MnPES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPTU4QxNjB4Mz20JO69VQ>? NYX5cZk{UUN3ME20MlYh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 M2PzNlI{Ozd{Nk[5
M-MOK  M2GyU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NISwVXozPSEEtV5CpC=> M1XF[FI1NzR6L{eyJIg> MkTLSG1UVw>? NWXnPWRScW6qaXLpeJMh[2WubDDndo94fGhidHnt[UBl\XCnbnTlcpRtgQ>? NFPlUJMzOTh3M{G1Oy=>
HEL M2juT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHXTWM2OD1|MEWgcm0> MnzxNVg{QTR3NUS=
Ba/F3 JAK2V617F MkH5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPDTWM2OD1{N{Cgcm0> M2ThWVE5Ozl2NUW0

... 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]
- Collapse

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]
- Collapse
  • 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]
- Collapse
  • 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.

  • * Indicates a Required Field

JAK Signaling Pathway Map

JAK Inhibitors with Unique Features

Related JAK Products

Tags: buy Fedratinib (SAR302503, TG101348) | Fedratinib (SAR302503, TG101348) supplier | purchase Fedratinib (SAR302503, TG101348) | Fedratinib (SAR302503, TG101348) cost | Fedratinib (SAR302503, TG101348) manufacturer | order Fedratinib (SAR302503, TG101348) | Fedratinib (SAR302503, TG101348) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID