Fedratinib (TG101348)

For research use only.

Catalog No.S2736 Synonyms: SAR302503

45 publications

Fedratinib (TG101348) Chemical Structure

CAS No. 936091-26-8

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. Fedratinib also inhibits FMS-like tyrosine kinase 3 (FLT3) and RET (c-RET) with IC50 of 15 nM and 48 nM, respectively. Fedratinib has potential antineoplastic activity. Fedratinib inhibits proliferation and induces apoptosis. Phase 2.

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Selleck's Fedratinib (TG101348) has been cited by 45 publications

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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. Fedratinib also inhibits FMS-like tyrosine kinase 3 (FLT3) and RET (c-RET) with IC50 of 15 nM and 48 nM, respectively. Fedratinib has potential antineoplastic activity. Fedratinib inhibits proliferation and induces apoptosis. 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 MXnBdI9xfG:|aYOgRZN{[Xl? NWC4cWI6OC53LUKg{txO M3fLOFEzNTR6IHi= MXjEUXNQ NET4c5pqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCkb4ToJIRwe2VvIHHu[EB1cW2nLTDk[ZBmdmSnboSgcYFvdmW{ NFu3TXUzPTh4OUKxNC=>
H1650 MUjBdI9xfG:|aYOgRZN{[Xl? MmPQNE42NTJizszN M4K5dlEzNTR6IHi= M1rTZmROW09? MV;pcoR2[2W|IHHwc5B1d3OrczDpckBjd3SqIHTvd4UuKGGwZDD0bY1mNSCmZYDlcoRmdnRibXHucoVz MlTlNlU5Pjl{MUC=
H1975 NI\aU|JHfW6ldHnvckBCe3OjeR?= M3\vflAvOjVvMTFOwG0> M123TVI1KGh? MX7EUXNQ M{\1U4lvcGmkaYTzJIV5eHKnc4Ppc44hd2ZiYYDvdJRwe2m|LYLlcIF1\WRicILveIVqdiCEY3ytXGwtKEKlbD2yMEB{fXK4aY\pckwhYEmDUB?= M{jERlI2QDZ7MkGw
H1650 M37v[mZ2dmO2aX;uJGF{e2G7 NIX0RmsxNjJ3LUGg{txO NGf0dZIzPCCq MUfEUXNQ NGLEVIlqdmirYnn0d{BmgHC{ZYPzbY9vKG:oIHHwc5B1d3Orcz3y[YxifGWmIIDyc5RmcW5iQnPsMXhNNCCEY3ytNkwhe3W{dnn2bY4tKFiLQWC= NF;YfI4zPTh4OUKxNC=>
H1975 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvoT2UyKM7:TR?= MVy0PEBp NEHRbHZFVVOR NX7PWHoxe2Wwc3n0bZpmeyClZXzsd{B1dyC2aHWgZ5l1d3SxeHnjbZR6KG:oIHXycI91cW6rYh?= NHvOOVczPTh4OUKxNC=>
H1650 Mn[2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7ofFZ2OSEQvF2= NIHT[Gc1QCCq NUPBOGZZTE2VTx?= NGS4bnF{\W6|aYTpfoV{KGOnbHzzJJRwKHSqZTDjfZRwfG:6aXPpeJkhd2ZiZYLsc5Rqdmmk MmfKNlU5Pjl{MUC=
CD4+ T M1jTTWZ2dmO2aX;uJGF{e2G7 NHG0dY4xNjBzLUGg{txO NHLBSVQ1QCCq Ml6xSG1UVw>? MlfudoVlfWOnczD0bIUheGixc4Doc5J6dGG2aX;uJIxmfmWuczDv[kBLSUt{IHHu[EBUXEGWM9Mg MUeyOVU4OjV|NR?=
Caco-2  M4n5cmZ2dmO2aX;uJGF{e2G7 NFzjTJMxNTF{MDFOwG0> NGPSU4U4KG2rbh?= M1rNOolvcGmkaYTzJJRpcWGvaX7lJJVxfGGtZTD3bZRpKGGwIFnDOVDDqG:oIEKuNeKhyrWP MX6yOVA3OzZ5Mh?=
Caco-2  NELHWmpHfW6ldHnvckBCe3OjeR?= NGiwZ3YyOC93MD:xNFAh|ryP NYLrTJFZOiCq NUTycWo2\GWlcnXhd4V{KHSqZTDmcJV5KG:oIGuzTH11cGmjbXnu[UBi[3Kxc4OgeIhmKG2xbn;sZZlmeiC5aYToJGlEPTBib3[gOk42yqEQvF2= NVzJUHNZOjVyNkO2O|I>
HEK293 MSR  M{TWTWZ2dmO2aX;uJGF{e2G7 MViwMVExKM7:TR?= M2PxU|chdWmw MXXpcohq[mm2czDoWGhVWjJid3n0bEBidiCLQ{WwxsBw\iBzLkNCpOK2VQ>? NH3JNngzPTB4M{[3Ni=>
MedB-1 NYnZOmU6TnWwY4Tpc44hSXO|YYm= NWX4VotpOS9{IN88US=> NEPncmczPCCq NHmwfHZl\WO{ZXHz[ZMhW1SDVE[gdIhwe3Cqb4L5cIF1cW:wIHPvcoNmdnS{YYTpc44h\GWyZX7k[Y51dHl? M1fnOFI1QTd5Nk[4
U2940 NULpfnUxTnWwY4Tpc44hSXO|YYm= MVSxM|Ih|ryP M1TDblI1KGh? NVLaVZBb\GWlcnXhd4V{KFOWQWS2JJBpd3OyaH;yfYxifGmxbjDjc45k\W62cnH0bY9vKGSncHXu[IVvfGy7 M4r0XlI1QTd5Nk[4
K1106 NHzGd|FHfW6ldHnvckBCe3OjeR?= M13IfFEwOiEQvF2= NVfhNW96OjRiaB?= NH;wWWRl\WO{ZXHz[ZMhW1SDVE[gdIhwe3Cqb4L5cIF1cW:wIHPvcoNmdnS{YYTpc44h\GWyZX7k[Y51dHl? M2j2R|I1QTd5Nk[4
K562 NUfOelQ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TzblAuOSEQvF2= M4\NOFczKGh? NXnmeFBscW6qaXLpeJMhUzV4MjDj[YxtKHC{b3zp[oVz[XSrb36gZZQhcGmpaDDjc45k\W62cnH0bY9v NVu3SIxCOjR5N{WzNFg>
MDA-MB-468  MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\oN{DDvU1? NVn1b5RJPDhiaB?= MYHlcohidmOnZDDzbYJkdDZiaX7keYNm\CCub4PzJI9nKGOnbHygeoli[mmuaYT5xsA> NWXJcmlVOjR4NkK4NVg>
MDA-MB-468 M4rSe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDUNG9HOC12IN88US=> MnjLOFghcA>? MUfy[ZN2dHS|IIPp[45q\mmlYX70JIxwe3Nib3[geoli[mmuaYT5JINwdXCjcnXkJJRwKFKLLVLQTUBidG:wZR?= M1XjXlI1PjZ{OEG4
L428 M1nSRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYSwMVUh|ryP MkLPOFghcA>? NVPtNpozcW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> NWn4R3pSOjR4MUC4Nlc>
KMH2 M3\zNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NECxbGoxNTVizszN MV:0PEBp NIOyTHFqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 MXuyOFYyODh{Nx?=
L1236 M4XBOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfId2oxNTVizszN M1\NU|Q5KGh? M1zMSYlvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= MViyOFYyODh{Nx?=
SUPHD1 M2nF[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV2wMVUh|ryP MX20PEBp M{\mdIlvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= NUL2PHF[OjR4MUC4Nlc>
HDLM2 NGTmRlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13seFAuPSEQvF2= MYq0PEBp NWPtVHZicW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> NWq2V|BHOjR4MUC4Nlc>
K1106P MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUewMVUh|ryP NF;mXIs1QCCq NGD2UJNqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 NVvvTZpOOjR4MUC4Nlc>
L428 NYOxTWc1SXCxcITvd4l{KEG|c3H5 MY[wM|AvPjJ3L{GuNlUh|ryP MV:0PEBp M1fv[olv\HWlZYOgeIhmKGGyb4D0c5Nqe8Li M3nNXVI1PjFyOEK3
KMH2 MnnyRZBweHSxc3nzJGF{e2G7 M3LVUlAwOC54MkWvNU4zPSEQvF2= M37KclQ5KGh? NXXBVWh{cW6mdXPld{B1cGViYYDvdJRwe2m|wrC= NYXLVHpsOjR4MUC4Nlc>
L1236 NG\EdlBCeG:ydH;zbZMhSXO|YYm= MmP5NE8xNjZ{NT:xMlI2KM7:TR?= NF3Jfmw1QCCq M4SwSYlv\HWlZYOgeIhmKGGyb4D0c5Nqe8Li NILGVZEzPDZzMEiyOy=>
SUPHD1 MYnBdI9xfG:|aYOgRZN{[Xl? MYqwM|AvPjJ3L{GuNlUh|ryP M2S2fVQ5KGh? MWnpcoR2[2W|IITo[UBieG:ydH;zbZPDqA>? NECwVGMzPDZzMEiyOy=>
HDLM2 NFrIcHlCeG:ydH;zbZMhSXO|YYm= NXP4c5FZOC9yLk[yOU8yNjJ3IN88US=> NXGzenhHPDhiaB?= MVHpcoR2[2W|IITo[UBieG:ydH;zbZPDqA>? MWiyOFYyODh{Nx?=
K1106P MU\BdI9xfG:|aYOgRZN{[Xl? MUiwM|AvPjJ3L{GuNlUh|ryP NGHwZYQ1QCCq NGrOfItqdmS3Y3XzJJRp\SCjcH;weI9{cXQEoB?= NIjZdIEzPDZzMEiyOy=>
L428 MlnNSpVv[3Srb36gRZN{[Xl? M4nqNlAuPSEQvF2= MU[yOEBp M{TGe4lvcGmkaYTzJGpCUzJxU2TBWEB{cWewYXzpcoc> MlXZNlQ3OTB6Mke=
KMH2 M3vKOmZ2dmO2aX;uJGF{e2G7 NWnPd2JEOC13IN88US=> Mn\ONlQhcA>? M{fkWolvcGmkaYTzJGpCUzJxU2TBWEB{cWewYXzpcoc> NYLGSHlmOjR4MUC4Nlc>
L1236 NFraU4RHfW6ldHnvckBCe3OjeR?= MUWwMVUh|ryP NIPleXUzPCCq NGjwZmRqdmirYnn0d{BLSUt{L2PURXQhe2mpbnHsbY5o MYSyOFYyODh{Nx?=
SUPHD1 NEO3RnpHfW6ldHnvckBCe3OjeR?= NYradZRYOC13IN88US=> NGXBbY8zPCCq NF;wSpRqdmirYnn0d{BLSUt{L2PURXQhe2mpbnHsbY5o M1Oye|I1PjFyOEK3
HDLM2 Mkn2SpVv[3Srb36gRZN{[Xl? NUHQNpBkOC13IN88US=> NFS1OJczPCCq M1PVZ4lvcGmkaYTzJGpCUzJxU2TBWEB{cWewYXzpcoc> Moq0NlQ3OTB6Mke=
K1106P M1vlUWZ2dmO2aX;uJGF{e2G7 NGXvfZIxNTVizszN MV[yOEBp M1WwUolvcGmkaYTzJGpCUzJxU2TBWEB{cWewYXzpcoc> NGnSUWszPDZzMEiyOy=>
MM.1S  NVzySINRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7HTWM2OD1zLUOg{txO MmHjNlQ2QDRzMEG=
TpoR JAK2 WT Mn;pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmX4TWM2OD1zLkSgLFEvO+LCk{GuOUkh|ryP NFXJ[nAzPDJ3MUe5NC=>
TpoR JAK2 V617F NFPQbItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnyTWM2OD1yLkigLFAvP+LCk{CuPUkh|ryP M2D1eVI1OjVzN{mw
TpoR W515L M4XFOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTBwODCoNE446oDVMT6wLUDPxE1? MXSyOFI2OTd7MB?=
Bcr-abl NF7TO2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HUS2lEPTB;Mj63JEgzNjMkgKOzMlMqKM7:TR?= NELVPZMzPDJ3MUe5NC=>
JAK2 TW M{j5T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLMTWM2OD1zLkigLFEvPeLCk{KuN{kh|ryP M3HFdlI1OjVzN{mw
JAK2 V617F NUPj[GliT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTBwNjCoNE436oDVMD63LUDPxE1? M4fRXFI1OjVzN{mw
MedB-1 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUf5VXV7PCEQvF2= MnH2NlQwPDhxN{KgbC=> M2PVT2ROW09? Mn3mbY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> NUTU[oRHOjN6NUKzOlY>
K1106 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUO0JO69VQ>? MYOyOE81QC95MjDo NUfjS3FQTE2VTx?= Ml3ybY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> NUTGZm1zOjN6NUKzOlY>
U2940 NGr2[ZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUO0JO69VQ>? NI\iflAzPC92OD:3NkBp MYHEUXNQ M3raWIlvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> M2nZfFI{QDV{M{[2
FE-PD NH7FTJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXSwMlA3Oy12IN88US=> Mn6xTWM2OD17LkWg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 NWXBNW5qOjN|N{K2Olk>
HEL NIfp[pdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;4NE4xPjNvNDFOwG0> MmDHTWM2OD1zLkWg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 NFT5d3MzOzN5Mk[2PS=>
K-562 M3LkPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfo[XNEOC5yNkOtOEDPxE1? MlPITWM2OD1{LkWg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 NIXa[WwzOzN5Mk[2PS=>
L-82 NHXYd3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoX4NE4xPjNvNDFOwG0> NF7FTIpKSzVyPUCuPVgh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NGf1bHgzOzN5Mk[2PS=>
MAC-1 NFvDeolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjqdYpqOC5yNkOtOEDPxE1? M2rHd2lEPTB;MD61NkDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= NYnlNpFvOjN|N{K2Olk>
MAC-2A NFX0VZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\kW|AvODZ|LUSg{txO MoXJTWM2OD1yLk[5JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= NWPvbo9sOjN|N{K2Olk>
MAC-2B MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUmwMlA3Oy12IN88US=> MmjaTWM2OD1yLkW0JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= NWrWNlBNOjN|N{K2Olk>
MY-LA NYTITJJET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVOwMlA3Oy12IN88US=> MkfCTWM2OD1{LkGg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 M{S5VlI{Ozd{Nk[5
NC-NC M4DONmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYruWGp2OC5yNkOtOEDPxE1? M3P1fWlEPTB;MT6wJO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= M3nYUlI{Ozd{Nk[5
SE-AX M2[xcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\WfWxGOC5yNkOtOEDPxE1? NVfoUG1yUUN3ME2xMlUh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NXG4TndxOjN|N{K2Olk>
SR-786 MkfvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXxNE4xPjNvNDFOwG0> MY\JR|UxRTRwNjFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? M3;uOVI{Ozd{Nk[5
M-MOK  M2LVNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV2yOUDDvU4EoB?= NFjSUZAzPC92OD:3NkBp MXHEUXNQ MWXpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 MViyNVg2OzF3Nx?=
HEL NGLpVldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTNyNTDuUS=> MVexPFM6PDV3NB?=
Ba/F3 JAK2V617F MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTJ5MDDuUS=> MnW1NVg{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
  • 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

* 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=CN=C(N=C1NC2=CC(=CC=C2)S(=O)(=O)NC(C)(C)C)NC3=CC=C(C=C3)OCCN4CCCC4

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

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 Recruiting Drug: Fedratinib Healthy Volunteers|Hepatic Impairment Celgene|Impact Biomedicines Inc. a wholly owned subsidiary of Celgene Corporation July 15 2019 Phase 1
NCT03983239 Completed Drug: Fedratinib|Drug: Rifampin|Drug: Efavirenz Healthy Volunteers Celgene|Impact Biomedicines Inc. a wholly owned subsidiary of Celgene Corporation June 21 2019 Phase 1
NCT02596347 Completed 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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID