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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In DMSO USD 220 In stock
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3 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.

    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

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 MVvBdI9xfG:|aYOgRZN{[Xl? NWXGbZdSOC53LUKg{txO NYPVOoNFOTJvNEigbC=> MlfJSG1UVw>? MWDpcoR2[2W|IHHwc5B1d3OrczDpckBjd3SqIHTvd4UuKGGwZDD0bY1mNSCmZYDlcoRmdnRibXHucoVz NGHGT5MzPTh4OUKxNC=>
H1650 MmPnRZBweHSxc3nzJGF{e2G7 NGDMTGgxNjVvMjFOwG0> MkX0NVIuPDhiaB?= NHjrblZFVVOR MYXpcoR2[2W|IHHwc5B1d3OrczDpckBjd3SqIHTvd4UuKGGwZDD0bY1mNSCmZYDlcoRmdnRibXHucoVz NWDuPVZyOjV6NkmyNVA>
H1975 MkDKSpVv[3Srb36gRZN{[Xl? M4DKXlAvOjVvMTFOwG0> M4\ZZ|I1KGh? Moe4SG1UVw>? NGDGOWNqdmirYnn0d{BmgHC{ZYPzbY9vKG:oIHHwc5B1d3Orcz3y[YxifGWmIIDyc5RmcW5iQnPsMXhNNCCEY3ytNkwhe3W{dnn2bY4tKFiLQWC= NXLnRY4{OjV6NkmyNVA>
H1650 MXrGeY5kfGmxbjDBd5NigQ>? MUOwMlI2NTFizszN NXnPOWtDOjRiaB?= MWDEUXNQ NFS1[lhqdmirYnn0d{BmgHC{ZYPzbY9vKG:oIHHwc5B1d3Orcz3y[YxifGWmIIDyc5RmcW5iQnPsMXhNNCCEY3ytNkwhe3W{dnn2bY4tKFiLQWC= MofjNlU5Pjl{MUC=
H1975 NHPoNYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYCxJO69VQ>? M2XpUVQ5KGh? MUDEUXNQ MlPkd4Vve2m2aYrld{Bk\WyuczD0c{B1cGViY4n0c5RwgGmlaYT5JI9nKGW{bH;0bY5q[g>? Mkf6NlU5Pjl{MUC=
H1650 NFLLXHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInuWmsyKM7:TR?= M2PnWVQ5KGh? NYD0S4syTE2VTx?= MUfz[Y5{cXSrenXzJINmdGy|IITvJJRp\SCleYTveI95cWOrdImgc4Yh\XKub4Tpcolj NHvIPXIzPTh4OUKxNC=>
CD4+ T MlPsSpVv[3Srb36gRZN{[Xl? MoP6NE4xOS1zIN88US=> MUW0PEBp NHXubpdFVVOR NYHkZmF3emWmdXPld{B1cGVicHjvd5Bpd3K7bHH0bY9vKGyndnXsd{Bw\iCMQVuyJIFv\CCVVFHUN:Kh MUWyOVU4OjV|NR?=
Caco-2  NIH3PINHfW6ldHnvckBCe3OjeR?= MmC3NE0yOjBizszN NXPleGh4PyCvaX6= M3:2e4lvcGmkaYTzJJRpcWGvaX7lJJVxfGGtZTD3bZRpKGGwIFnDOVDDqG:oIEKuNeKhyrWP NFTTPVMzPTB4M{[3Ni=>
Caco-2  MnXpSpVv[3Srb36gRZN{[Xl? M3vLcVExNzVyL{GwNEDPxE1? M4LDe|IhcA>? M3XXXIRm[3KnYYPld{B1cGViZnz1fEBw\iCdM1jdeIhq[W2rbnWgZYNzd3O|IITo[UBud26xbHH5[ZIhf2m2aDDJR|UxKG:oIE[uOeKh|ryP NUP1VJpxOjVyNkO2O|I>
HEK293 MSR  MWrGeY5kfGmxbjDBd5NigQ>? NV20PWFwOC1zMDFOwG0> NVr2Um86PyCvaX6= NUPuPW1pcW6qaXLpeJMhcFSKVGKyJJdqfGhiYX6gTWM2OMLib3[gNU4zyqEEtV2= NH31VpkzPTB4M{[3Ni=>
MedB-1 NH;NVoxHfW6ldHnvckBCe3OjeR?= NInXb5oyNzJizszN MmDiNlQhcA>? MVvk[YNz\WG|ZYOgV3RCXDZicHjvd5Bpd3K7bHH0bY9vKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> MVWyOFk4PzZ4OB?=
U2940 Moi5SpVv[3Srb36gRZN{[Xl? MlTENU8zKM7:TR?= MUiyOEBp M1ixboRm[3KnYYPld{BUXEGWNjDwbI9{eGixconsZZRqd25iY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? M{L4SFI1QTd5Nk[4
K1106 MYjGeY5kfGmxbjDBd5NigQ>? M3f5N|EwOiEQvF2= MUGyOEBp Ml2z[IVkemWjc3XzJHNVSVR4IIDoc5NxcG:{eXzheIlwdiClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NWPKcoE1OjR7N{e2Olg>
K562 NXrMcGlWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2P0cVAuOSEQvF2= M4rlPFczKGh? MkXzbY5pcWKrdIOgT|U3OiClZXzsJJBzd2yrZnXyZZRqd25iYYSgbIlocCClb37j[Y51emG2aX;u MnvGNlQ4PzV|MEi=
MDA-MB-468  M33ZSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUezJOK2VQ>? MknJOFghcA>? MnLn[Y5p[W6lZXSgd4lj[2x4IHnu[JVk\WRibH;zd{Bw\iClZXzsJJZq[WKrbHn0feKh NY\X[YZbOjR4NkK4NVg>
MDA-MB-468 NHj1PGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIq3N|MxNTRizszN MkLjOFghcA>? NFLsVJpz\XO3bITzJJNq\26rZnnjZY51KGyxc4Ogc4YhfmmjYnnsbZR6KGOxbYDhdoVlKHSxIGLJMWJRUSCjbH;u[S=> Mm[4NlQ3PjJ6MUi=
L428 MnrMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXSwMVUh|ryP NITq[ZU1QCCq MnfVbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= MWeyOFYyODh{Nx?=
KMH2 M{LKZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEf1ZpQxNTVizszN NYrLWXFiPDhiaB?= M4fkWolvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= MXmyOFYyODh{Nx?=
L1236 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXTPWk2OC13IN88US=> NG\QZZE1QCCq NX7xSIpPcW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> M2DUe|I1PjFyOEK3
SUPHD1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17ERlAuPSEQvF2= M2PSUVQ5KGh? Mn;zbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= MXGyOFYyODh{Nx?=
HDLM2 NFrSPItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{n2UlAuPSEQvF2= NIXiS5g1QCCq M3X4bIlvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= NIrZbYUzPDZzMEiyOy=>
K1106P MkLBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;2OlAuPSEQvF2= MVi0PEBp NXrF[3pGcW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> NVL1c3RPOjR4MUC4Nlc>
L428 M2j3NmFxd3C2b4Ppd{BCe3OjeR?= M2TZXVAwOC54MkWvNU4zPSEQvF2= NFz3R|E1QCCq M3XSWYlv\HWlZYOgeIhmKGGyb4D0c5Nqe8Li MUKyOFYyODh{Nx?=
KMH2 M3v0WWFxd3C2b4Ppd{BCe3OjeR?= NE\rfFQxNzBwNkK1M|EvOjVizszN MYO0PEBp MoHTbY5lfWOnczD0bIUh[XCxcITvd4l{yqB? MWCyOFYyODh{Nx?=
L1236 NXTNN|ZzSXCxcITvd4l{KEG|c3H5 MWiwM|AvPjJ3L{GuNlUh|ryP NXnl[HNZPDhiaB?= M2P5TIlv\HWlZYOgeIhmKGGyb4D0c5Nqe8Li NFXQVZEzPDZzMEiyOy=>
SUPHD1 MVjBdI9xfG:|aYOgRZN{[Xl? MXmwM|AvPjJ3L{GuNlUh|ryP NX\rfW9CPDhiaB?= NVXCUGQ3cW6mdXPld{B1cGViYYDvdJRwe2m|wrC= MlnxNlQ3OTB6Mke=
HDLM2 NVjoW481SXCxcITvd4l{KEG|c3H5 MV:wM|AvPjJ3L{GuNlUh|ryP NUHE[YpZPDhiaB?= M{Hp[4lv\HWlZYOgeIhmKGGyb4D0c5Nqe8Li Ml;mNlQ3OTB6Mke=
K1106P M1rQOGFxd3C2b4Ppd{BCe3OjeR?= NEXidYYxNzBwNkK1M|EvOjVizszN MkG0OFghcA>? MkS0bY5lfWOnczD0bIUh[XCxcITvd4l{yqB? M{Lrc|I1PjFyOEK3
L428 NUL3SJZCTnWwY4Tpc44hSXO|YYm= M4LkflAuPSEQvF2= MU[yOEBp MWLpcohq[mm2czDKRWszN1OWQWSgd4lodmGuaX7n M2PIZVI1PjFyOEK3
KMH2 MXTGeY5kfGmxbjDBd5NigQ>? MWWwMVUh|ryP NIHW[3ozPCCq NITxPGFqdmirYnn0d{BLSUt{L2PURXQhe2mpbnHsbY5o NHTVSlQzPDZzMEiyOy=>
L1236 NGLzenhHfW6ldHnvckBCe3OjeR?= NX;DdHc1OC13IN88US=> NXz5SJJjOjRiaB?= NF:4OoJqdmirYnn0d{BLSUt{L2PURXQhe2mpbnHsbY5o NXvGWY9EOjR4MUC4Nlc>
SUPHD1 MlL3SpVv[3Srb36gRZN{[Xl? MXGwMVUh|ryP M3rkVlI1KGh? NVrkVpMxcW6qaXLpeJMhUkGNMj;TWGFVKHOrZ37hcIlv\w>? MmHzNlQ3OTB6Mke=
HDLM2 MY\GeY5kfGmxbjDBd5NigQ>? NVfZfIpMOC13IN88US=> NUPCc5Y5OjRiaB?= NVjPZ5BMcW6qaXLpeJMhUkGNMj;TWGFVKHOrZ37hcIlv\w>? NGTrflkzPDZzMEiyOy=>
K1106P MYnGeY5kfGmxbjDBd5NigQ>? M1HSXVAuPSEQvF2= MoTkNlQhcA>? NGf2Vo9qdmirYnn0d{BLSUt{L2PURXQhe2mpbnHsbY5o NVrL[GJqOjR4MUC4Nlc>
MM.1S  MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfXcXZKSzVyPUGtN{DPxE1? MW[yOFU5PDFyMR?=
TpoR JAK2 WT M1\lXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTFwNDCoNU4{6oDVMT61LUDPxE1? NH\TTG0zPDJ3MUe5NC=>
TpoR JAK2 V617F MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M135PWlEPTB;MD64JEgxNjgkgKOwMlkqKM7:TR?= Mn;0NlQzPTF5OUC=
TpoR W515L MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1X6VmlEPTB;MD64JEgxNjgkgKOxMlAqKM7:TR?= NWS0eW5JOjR{NUG3PVA>
Bcr-abl MnLlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17SWGlEPTB;Mj63JEgzNjMkgKOzMlMqKM7:TR?= NFroVpAzPDJ3MUe5NC=>
JAK2 TW NXrETVY1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoeyTWM2OD1zLkigLFEvPeLCk{KuN{kh|ryP NESxVZczPDJ3MUe5NC=>
JAK2 V617F NVHuVVhqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{f3[2lEPTB;MD62JEgxNjckgKOwMlcqKM7:TR?= MVqyOFI2OTd7MB?=
MedB-1 NFjNWI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzUSnhLPCEQvF2= MWWyOE81QC95MjDo NEHseIVFVVOR NFfFbWJqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 MlXNNlM5PTJ|Nk[=
K1106 NIjveFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYq0JO69VQ>? M1nKblI1NzR6L{eyJIg> NFzNPJpFVVOR MWXpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 MWiyN|g2OjN4Nh?=
U2940 MoLHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorWOEDPxE1? MlfUNlQwPDhxN{KgbC=> NXrrSYwxTE2VTx?= Mly5bY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> M4r0dFI{QDV{M{[2
FE-PD NFXHd|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHm0UYUxNjB4Mz20JO69VQ>? MlXHTWM2OD17LkWg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 NGXufJczOzN5Mk[2PS=>
HEL NH2zVodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUSwMlA3Oy12IN88US=> NYKxWGRLUUN3ME2xMlUh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NFXWc4UzOzN5Mk[2PS=>
K-562 NVnHe4RDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPMNE4xPjNvNDFOwG0> NYjXdop{UUN3ME2yMlUh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NHfDe4kzOzN5Mk[2PS=>
L-82 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfIe5hZOC5yNkOtOEDPxE1? M1HqemlEPTB;MD65PEDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= NHTVUokzOzN5Mk[2PS=>
MAC-1 MlPOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nUS|AvODZ|LUSg{txO NY\ueIp2UUN3ME2wMlUzKM7:TTygbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NUPVOlh3OjN|N{K2Olk>
MAC-2A M4Wzb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYewMlA3Oy12IN88US=> MX7JR|UxRTBwNkmg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 M1nNOlI{Ozd{Nk[5
MAC-2B NF7jeHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3f5OFAvODZ|LUSg{txO M1S0e2lEPTB;MD61OEDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= NIDyN|kzOzN5Mk[2PS=>
MY-LA M1PyVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;mNE4xPjNvNDFOwG0> NWT4UJBpUUN3ME2yMlEh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NXz5c5pFOjN|N{K2Olk>
NC-NC M13LUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnBSoQ{OC5yNkOtOEDPxE1? Ml\mTWM2OD1zLkCg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 MnW0NlM{PzJ4Nkm=
SE-AX Mn7tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFT3bWIxNjB4Mz20JO69VQ>? M3flV2lEPTB;MT61JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= M4LLTlI{Ozd{Nk[5
SR-786 MnL2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vKeFAvODZ|LUSg{txO NGi2[3NKSzVyPUSuOkDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= NGPsTnozOzN5Mk[2PS=>
M-MOK  M{Tt[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjGNlUhyrWPwrC= M1HpZlI1NzR6L{eyJIg> NXv0T|hiTE2VTx?= M2T3NYlvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> NGL5V5UzOTh3M{G1Oy=>
HEL MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;WVmlEPTB;M{C1JI5O MlvVNVg{QTR3NUS=
Ba/F3 JAK2V617F NGGwNmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jMTGlEPTB;MkewJI5O NHjaXZUyQDN7NEW1OC=>

... 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 <1 mg/mL
Ethanol <1 mg/mL
In vivo 1% DMSO+30% polyethylene glycol+1% Tween 80 30 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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 (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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID