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 MVrBdI9xfG:|aYOgRZN{[Xl? NVP4Ulg2OC53LUKg{txO M{PXS|EzNTR6IHi= Ml:0SG1UVw>? NFnxZ3RqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCkb4ToJIRwe2VvIHHu[EB1cW2nLTDk[ZBmdmSnboSgcYFvdmW{ NGDEblMzPTh4OUKxNC=>
H1650 MXfBdI9xfG:|aYOgRZN{[Xl? NHTJN4MxNjVvMjFOwG0> M2XhS|EzNTR6IHi= MVzEUXNQ MYPpcoR2[2W|IHHwc5B1d3OrczDpckBjd3SqIHTvd4UuKGGwZDD0bY1mNSCmZYDlcoRmdnRibXHucoVz NHe2U5YzPTh4OUKxNC=>
H1975 NVTIXotqTnWwY4Tpc44hSXO|YYm= MVqwMlI2NTFizszN NWf3VFFkOjRiaB?= M1XYZmROW09? NVXiRmlucW6qaXLpeJMh\XiycnXzd4lwdiCxZjDhdI9xfG:|aYOtdoVt[XSnZDDwdo91\WmwIFLjcE1ZVCxiQnPsMVItKHO3co\peolvNCC[SVHQ NUmwc5NVOjV6NkmyNVA>
H1650 M2jhXmZ2dmO2aX;uJGF{e2G7 MUOwMlI2NTFizszN MVqyOEBp M{LTN2ROW09? NFjicYxqdmirYnn0d{BmgHC{ZYPzbY9vKG:oIHHwc5B1d3Orcz3y[YxifGWmIIDyc5RmcW5iQnPsMXhNNCCEY3ytNkwhe3W{dnn2bY4tKFiLQWC= M{\sNlI2QDZ7MkGw
H1975 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLWNUDPxE1? M1TsW|Q5KGh? NHvGenZFVVOR MVvz[Y5{cXSrenXzJINmdGy|IITvJJRp\SCleYTveI95cWOrdImgc4Yh\XKub4Tpcolj MX6yOVg3QTJzMB?=
H1650 NWnU[Gw{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVOxJO69VQ>? NH;DXJo1QCCq NYDhVYprTE2VTx?= M{jueZNmdnOrdHn6[ZMh[2WubIOgeI8hfGinIHP5eI91d3irY3n0fUBw\iCncnzveIlvcWJ? NFPqbGgzPTh4OUKxNC=>
CD4+ T M4niWGZ2dmO2aX;uJGF{e2G7 NW\jdGlHOC5yMT2xJO69VQ>? MWS0PEBp NXzWSFRzTE2VTx?= MlH2doVlfWOnczD0bIUheGixc4Doc5J6dGG2aX;uJIxmfmWuczDv[kBLSUt{IHHu[EBUXEGWM9Mg NH\I[5ozPTV5MkWzOS=>
Caco-2  NXvHNHFZTnWwY4Tpc44hSXO|YYm= Mn\lNE0yOjBizszN NV;RS2xkPyCvaX6= MYfpcohq[mm2czD0bIlidWmwZTD1dJRic2Vid3n0bEBidiCLQ{WwxsBw\iB{LkJCpOK2VQ>? MnrzNlUxPjN4N{K=
Caco-2  NXO0do9STnWwY4Tpc44hSXO|YYm= NWjLR2lJOTBxNUCvNVAxKM7:TR?= NV;2OplXOiCq NGLFRWhl\WO{ZXHz[ZMhfGinIH\seZghd2ZiW{PIYZRpcWGvaX7lJIFkem:|czD0bIUhdW:wb3zhfYVzKHerdHigTWM2OCCxZjC2MlXDqM7:TR?= NIC2b5UzPTB4M{[3Ni=>
HEK293 MSR  MYfGeY5kfGmxbjDBd5NigQ>? MnLDNE0yOCEQvF2= MXO3JI1qdg>? NHT3OIdqdmirYnn0d{BpXEiWUkKge4l1cCCjbjDJR|UxyqCxZjCxMlLDqML3TR?= MUGyOVA3OzZ5Mh?=
MedB-1 M{i5O2Z2dmO2aX;uJGF{e2G7 MoS3NU8zKM7:TR?= MonHNlQhcA>? M2m3c4Rm[3KnYYPld{BUXEGWNjDwbI9{eGixconsZZRqd25iY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? NGPMRmQzPDl5N{[2PC=>
U2940 MlHwSpVv[3Srb36gRZN{[Xl? NYDHPFBnOS9{IN88US=> NWrvNFdPOjRiaB?= NHO5c2tl\WO{ZXHz[ZMhW1SDVE[gdIhwe3Cqb4L5cIF1cW:wIHPvcoNmdnS{YYTpc44h\GWyZX7k[Y51dHl? MnvPNlQ6Pzd4Nki=
K1106 MULGeY5kfGmxbjDBd5NigQ>? NH;He|EyNzJizszN NHTFZYczPCCq MnTC[IVkemWjc3XzJHNVSVR4IIDoc5NxcG:{eXzheIlwdiClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NX31fo54OjR7N{e2Olg>
K562 M2XqZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;mbWZMOC1zIN88US=> NWOwSGVpPzJiaB?= M1ywXIlvcGmkaYTzJGs2PjJiY3XscEBxem:uaX\ldoF1cW:wIHH0JIhq\2hiY3;uZ4VvfHKjdHnvci=> NIfrVpUzPDd5NUOwPC=>
MDA-MB-468  NH;hTJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;JW|dwOyEEtV2= NIjKTmw1QCCq NVnCZZRZ\W6qYX7j[YQhe2mkY3y2JIlv\HWlZXSgcI9{eyCxZjDj[YxtKH[rYXLpcIl1gcLi NIr5SWozPDZ4MkixPC=>
MDA-MB-468 Mn7iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHf2XHAxNTRizszN MlXvOFghcA>? M2TmXJJme3WudIOgd4lodmmoaXPhcpQhdG:|czDv[kB3cWGkaXzpeJkh[2:vcHHy[YQhfG9iUlmtRnBKKGGub37l MnTvNlQ3PjJ6MUi=
L428 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1KyfVAuPSEQvF2= NF7kO|c1QCCq NUOxTlQ5cW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> NF;RWZEzPDZzMEiyOy=>
KMH2 NUjWVFA5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV[4PXVxOC13IN88US=> NGD0dHI1QCCq Mm[ybY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= M3vCR|I1PjFyOEK3
L1236 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUKwMVUh|ryP NWfnellUPDhiaB?= MlrmbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= M4OxOlI1PjFyOEK3
SUPHD1 NVnTRYc3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\TW|AuPSEQvF2= NIf4fXM1QCCq MlrUbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= MXWyOFYyODh{Nx?=
HDLM2 NYHpUXMzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjLWHExNTVizszN MlnLOFghcA>? NHzncnRqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 NFfNe5czPDZzMEiyOy=>
K1106P M2CyPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTVNE02KM7:TR?= MnG0OFghcA>? MW\pcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 MnuwNlQ3OTB6Mke=
L428 NFTpXWFCeG:ydH;zbZMhSXO|YYm= MnjJNE8xNjZ{NT:xMlI2KM7:TR?= NX;pcFNnPDhiaB?= NEXsd|JqdmS3Y3XzJJRp\SCjcH;weI9{cXQEoB?= NVXpNHlGOjR4MUC4Nlc>
KMH2 MkHURZBweHSxc3nzJGF{e2G7 NX3mbYRKOC9yLk[yOU8yNjJ3IN88US=> MUG0PEBp NG\0UGxqdmS3Y3XzJJRp\SCjcH;weI9{cXQEoB?= NH3MS3EzPDZzMEiyOy=>
L1236 NWj3cFQ3SXCxcITvd4l{KEG|c3H5 NH71NXQxNzBwNkK1M|EvOjVizszN NWW1e5NlPDhiaB?= NEXQXlJqdmS3Y3XzJJRp\SCjcH;weI9{cXQEoB?= M2TMOFI1PjFyOEK3
SUPHD1 M1L4NmFxd3C2b4Ppd{BCe3OjeR?= NWPBXYFSOC9yLk[yOU8yNjJ3IN88US=> MonTOFghcA>? NXPRXYk3cW6mdXPld{B1cGViYYDvdJRwe2m|wrC= MmrINlQ3OTB6Mke=
HDLM2 MnuzRZBweHSxc3nzJGF{e2G7 MVqwM|AvPjJ3L{GuNlUh|ryP NVvlOFdWPDhiaB?= MlfMbY5lfWOnczD0bIUh[XCxcITvd4l{yqB? MXyyOFYyODh{Nx?=
K1106P M{XkSGFxd3C2b4Ppd{BCe3OjeR?= NF3UVoYxNzBwNkK1M|EvOjVizszN MVS0PEBp MonrbY5lfWOnczD0bIUh[XCxcITvd4l{yqB? NFiwfpczPDZzMEiyOy=>
L428 NVj4OItmTnWwY4Tpc44hSXO|YYm= NETQT40xNTVizszN M1jWZVI1KGh? MnLlbY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> M3XrbFI1PjFyOEK3
KMH2 NFfncHRHfW6ldHnvckBCe3OjeR?= MWWwMVUh|ryP NHfqXXczPCCq MXHpcohq[mm2czDKRWszN1OWQWSgd4lodmGuaX7n NY[1TFdsOjR4MUC4Nlc>
L1236 MojwSpVv[3Srb36gRZN{[Xl? MorDNE02KM7:TR?= MnzUNlQhcA>? MVPpcohq[mm2czDKRWszN1OWQWSgd4lodmGuaX7n MoTnNlQ3OTB6Mke=
SUPHD1 NHOzXI1HfW6ldHnvckBCe3OjeR?= NG[0TY4xNTVizszN NX7LRlVGOjRiaB?= Mn;UbY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> M2fjVlI1PjFyOEK3
HDLM2 M3LTSGZ2dmO2aX;uJGF{e2G7 MWKwMVUh|ryP Ml;ENlQhcA>? MYnpcohq[mm2czDKRWszN1OWQWSgd4lodmGuaX7n MkLsNlQ3OTB6Mke=
K1106P NFzWWo9HfW6ldHnvckBCe3OjeR?= NVrlXmlwOC13IN88US=> MWiyOEBp M2jGNIlvcGmkaYTzJGpCUzJxU2TBWEB{cWewYXzpcoc> MlLYNlQ3OTB6Mke=
MM.1S  NWDxW4FnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2XHTmlEPTB;MT2zJO69VQ>? NU\XTmd7OjR3OESxNFE>
TpoR JAK2 WT MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4jwPWlEPTB;MT60JEgyNjQkgKOxMlUqKM7:TR?= NHHVOGQzPDJ3MUe5NC=>
TpoR JAK2 V617F NVr6UVV1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HjNmlEPTB;MD64JEgxNjgkgKOwMlkqKM7:TR?= MXWyOFI2OTd7MB?=
TpoR W515L MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPtTWM2OD1yLkigLFAvP+LCk{GuNEkh|ryP NGLrcnIzPDJ3MUe5NC=>
Bcr-abl MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUS3c5BRUUN3ME2yMlchMDJwMvMAl|MvOylizszN M4SxdVI1OjVzN{mw
JAK2 TW NFTRSW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PGUmlEPTB;MT64JEgyNjYkgKOyMlMqKM7:TR?= M4DFeVI1OjVzN{mw
JAK2 V617F MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTBwNjCoNE436oDVMD63LUDPxE1? MkPyNlQzPTF5OUC=
MedB-1 MmPLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\ndlQh|ryP M2XEPFI1NzR6L{eyJIg> MXzEUXNQ MmPHbY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> MnnBNlM5PTJ|Nk[=
K1106 NIfwWJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGH0WnU1KM7:TR?= MkmzNlQwPDhxN{KgbC=> NFfDc5FFVVOR MX3pcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 NVPPUJFTOjN6NUKzOlY>
U2940 M1jiTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYC0JO69VQ>? NUj3b|BGOjRxNEivO|IhcA>? M1vSe2ROW09? NGq4NndqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 M{D2UlI{QDV{M{[2
FE-PD NGLvd5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXiNE4xPjNvNDFOwG0> NFjjR2NKSzVyPUmuOUDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= Mn;NNlM{PzJ4Nkm=
HEL M4TXV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\5[lAvODZ|LUSg{txO MVfJR|UxRTFwNTFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? NFLOZ2wzOzN5Mk[2PS=>
K-562 Mk\2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjKNE4xPjNvNDFOwG0> MV7JR|UxRTJwNTFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? NGLyPY8zOzN5Mk[2PS=>
L-82 NXywc28zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGX6T4MxNjB4Mz20JO69VQ>? NFfOfXhKSzVyPUCuPVgh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MWmyN|M4OjZ4OR?=
MAC-1 M1LlPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVywMlA3Oy12IN88US=> MnLzTWM2OD1yLkWyJO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= Mne3NlM{PzJ4Nkm=
MAC-2A M4TsU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVuwMlA3Oy12IN88US=> M3LjW2lEPTB;MD62PUDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= M3nud|I{Ozd{Nk[5
MAC-2B MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnTzNE4xPjNvNDFOwG0> MVPJR|UxRTBwNUSg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 NYW0NZJrOjN|N{K2Olk>
MY-LA M3\vR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrhNE4xPjNvNDFOwG0> NYDWe3hKUUN3ME2yMlEh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NFLhfHIzOzN5Mk[2PS=>
NC-NC NH\sOZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmHWNE4xPjNvNDFOwG0> NGXHeFBKSzVyPUGuNEDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= NVfuXGF4OjN|N{K2Olk>
SE-AX MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrUNE4xPjNvNDFOwG0> MU\JR|UxRTFwNTFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? M4DPUVI{Ozd{Nk[5
SR-786 Mlr5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWO5Z2lyOC5yNkOtOEDPxE1? NWjjbHpKUUN3ME20MlYh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MYOyN|M4OjZ4OR?=
M-MOK  M3jhXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPvZmszPSEEtV5CpC=> MXKyOE81QC95MjDo MWPEUXNQ NX3hZ2U4cW6qaXLpeJMh[2WubDDndo94fGhidHnt[UBl\XCnbnTlcpRtgQ>? M{L1SVIyQDV|MUW3
HEL NEPaR|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7LdlRJUUN3ME2zNFUhdk1? MWWxPFM6PDV3NB?=
Ba/F3 JAK2V617F MnjHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjBU5ZVUUN3ME2yO|Ahdk1? Mn\FNVg{QTR3NUS=

... 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 to the product individually and in order:
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
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