Fedratinib (TG101348)

For research use only.

Catalog No.S2736 Synonyms: SAR302503

48 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 48 publications

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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? Ml7BNE42NTJizszN MlzENVIuPDhiaB?= M2DEOGROW09? MmXYbY5lfWOnczDhdI9xfG:|aYOgbY4h[m:2aDDkc5NmNSCjbnSgeIlu\S1iZHXw[Y5l\W62IH3hco5meg>? NYPVVmg2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4OlkzOTBpPkK1PFY6OjFyPD;hQi=>
H1650 M{PL[WFxd3C2b4Ppd{BCe3OjeR?= MWGwMlUuOiEQvF2= MnPjNVIuPDhiaB?= M{jId2ROW09? MlPFbY5lfWOnczDhdI9xfG:|aYOgbY4h[m:2aDDkc5NmNSCjbnSgeIlu\S1iZHXw[Y5l\W62IH3hco5meg>? MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh4OUKxNEc,OjV6NkmyNVA9N2F-
H1975 MVvGeY5kfGmxbjDBd5NigQ>? MYmwMlI2NTFizszN NXzLfY5uOjRiaB?= MWfEUXNQ M1rK[IlvcGmkaYTzJIV5eHKnc4Ppc44hd2ZiYYDvdJRwe2m|LYLlcIF1\WRicILveIVqdiCEY3ytXGwtKEKlbD2yMEB{fXK4aY\pckwhYEmDUB?= NXzhZ2tXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4OlkzOTBpPkK1PFY6OjFyPD;hQi=>
H1650 MlPjSpVv[3Srb36gRZN{[Xl? NX;zOWp1OC5{NT2xJO69VQ>? M{TxfVI1KGh? M1\Jc2ROW09? M1XGZYlvcGmkaYTzJIV5eHKnc4Ppc44hd2ZiYYDvdJRwe2m|LYLlcIF1\WRicILveIVqdiCEY3ytXGwtKEKlbD2yMEB{fXK4aY\pckwhYEmDUB?= NGjyTpE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUi2PVIyOCd-MkW4OlkzOTB:L3G+
H1975 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXRd|FEOSEQvF2= MYO0PEBp MkTvSG1UVw>? MVzz[Y5{cXSrenXzJINmdGy|IITvJJRp\SCleYTveI95cWOrdImgc4Yh\XKub4Tpcolj NUTFSIxJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4OlkzOTBpPkK1PFY6OjFyPD;hQi=>
H1650 NYq5WmdHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkiyNUDPxE1? NYfZfJNvPDhiaB?= M{HZTmROW09? M3PZXZNmdnOrdHn6[ZMh[2WubIOgeI8hfGinIHP5eI91d3irY3n0fUBw\iCncnzveIlvcWJ? MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh4OUKxNEc,OjV6NkmyNVA9N2F-
CD4+ T NGi2dmpHfW6ldHnvckBCe3OjeR?= MYmwMlAyNTFizszN M2nuXVQ5KGh? NWCxSnB7TE2VTx?= NGjkPYdz\WS3Y3XzJJRp\SCyaH;zdIhwenmuYYTpc44hdGW4ZXzzJI9nKEqDS{KgZY5lKFOWQWSzxsA> MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTV5MkWzOUc,OjV3N{K1N|U9N2F-
Caco-2  Ml\xSpVv[3Srb36gRZN{[Xl? MkjYNE0yOjBizszN M{DZOVchdWmw NH3tPWZqdmirYnn0d{B1cGmjbXnu[UB2eHSja3Wge4l1cCCjbjDJR|UxyqCxZjCyMlHDqML3TR?= M3nNfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3ME[zOlczLz5{NUC2N|Y4OjxxYU6=
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HEK293 MSR  M37qZWZ2dmO2aX;uJGF{e2G7 NFzr[2IxNTFyIN88US=> MmXWO{BucW5? M1jRWIlvcGmkaYTzJIhVUFSUMjD3bZRpKGGwIFnDOVDDqG:oIEGuNuKhyrWP M3vqfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3ME[zOlczLz5{NUC2N|Y4OjxxYU6=
MedB-1 NGW5ZodHfW6ldHnvckBCe3OjeR?= MmP0NU8zKM7:TR?= M{WycFI1KGh? Ml[3[IVkemWjc3XzJHNVSVR4IIDoc5NxcG:{eXzheIlwdiClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl5N{[2PEc,OjR7N{e2Olg9N2F-
U2940 M2nO[2Z2dmO2aX;uJGF{e2G7 NHjjbnYyNzJizszN Mn3BNlQhcA>? M4XTOYRm[3KnYYPld{BUXEGWNjDwbI9{eGixconsZZRqd25iY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? NGLQcY49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm3O|Y3QCd-MkS5O|c3Pjh:L3G+
K1106 M1jpO2Z2dmO2aX;uJGF{e2G7 NHzXO5AyNzJizszN MVGyOEBp M4fxcoRm[3KnYYPld{BUXEGWNjDwbI9{eGixconsZZRqd25iY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? NF23fYE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm3O|Y3QCd-MkS5O|c3Pjh:L3G+
K562 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUWwMVEh|ryP NHnmclM4OiCq Ml76bY5pcWKrdIOgT|U3OiClZXzsJJBzd2yrZnXyZZRqd25iYYSgbIlocCClb37j[Y51emG2aX;u MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd5NUOwPEc,OjR5N{WzNFg9N2F-
MDA-MB-468  M3X5[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnKN{DDvU1? NX:yTJpwPDhiaB?= NYK0Zm14\W6qYX7j[YQhe2mkY3y2JIlv\HWlZXSgcI9{eyCxZjDj[YxtKH[rYXLpcIl1gcLi NH\LR209[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[2NlgyQCd-MkS2OlI5OTh:L3G+
MDA-MB-468 M{DqbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrVNE01KM7:TR?= M1LDWlQ5KGh? MVLy[ZN2dHS|IIPp[45q\mmlYX70JIxwe3Nib3[geoli[mmuaYT5JINwdXCjcnXkJJRwKFKLLVLQTUBidG:wZR?= MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ4MkixPEc,OjR4NkK4NVg9N2F-
L428 MnTpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTBNE02KM7:TR?= MXe0PEBp M3XkfYlvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= NXTldJVqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2NVA5OjdpPkK0OlExQDJ5PD;hQi=>
KMH2 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrjOVIxNTVizszN NX;6TZRKPDhiaB?= NUe0UXpkcW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> NHrQNmI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[xNFgzPyd-MkS2NVA5Ojd:L3G+
L1236 M1nqbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\6Z5JLOC13IN88US=> NWLOcXpTPDhiaB?= M333[4lvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= M3PjOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkGwPFI4Lz5{NE[xNFgzPzxxYU6=
SUPHD1 MkHlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXu3OJRPOC13IN88US=> NHrwR5c1QCCq NHv0fnJqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 NFO2WZU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[xNFgzPyd-MkS2NVA5Ojd:L3G+
HDLM2 NF3veY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\NV|AuPSEQvF2= MW[0PEBp NUPIbotpcW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZzMEiyO{c,OjR4MUC4Nlc9N2F-
K1106P NGXzPJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmO1NE02KM7:TR?= MVG0PEBp NITTTYpqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 NXzIToIxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2NVA5OjdpPkK0OlExQDJ5PD;hQi=>
L428 Mo[wRZBweHSxc3nzJGF{e2G7 NXzEUnRmOC9yLk[yOU8yNjJ3IN88US=> MmDSOFghcA>? NYjkSJQycW6mdXPld{B1cGViYYDvdJRwe2m|wrC= NEX2WI49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[xNFgzPyd-MkS2NVA5Ojd:L3G+
KMH2 MVzBdI9xfG:|aYOgRZN{[Xl? NVzsNFNFOC9yLk[yOU8yNjJ3IN88US=> NV;sNYNIPDhiaB?= NUnKNJZNcW6mdXPld{B1cGViYYDvdJRwe2m|wrC= MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZzMEiyO{c,OjR4MUC4Nlc9N2F-
L1236 M37zcWFxd3C2b4Ppd{BCe3OjeR?= MoXFNE8xNjZ{NT:xMlI2KM7:TR?= M17NWlQ5KGh? M2\K[Ylv\HWlZYOgeIhmKGGyb4D0c5Nqe8Li NFy3OmE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[xNFgzPyd-MkS2NVA5Ojd:L3G+
SUPHD1 MmDvRZBweHSxc3nzJGF{e2G7 MVSwM|AvPjJ3L{GuNlUh|ryP MV60PEBp MUnpcoR2[2W|IITo[UBieG:ydH;zbZPDqA>? M1qxbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkGwPFI4Lz5{NE[xNFgzPzxxYU6=
HDLM2 MXHBdI9xfG:|aYOgRZN{[Xl? MkfCNE8xNjZ{NT:xMlI2KM7:TR?= NIH2R4I1QCCq MXrpcoR2[2W|IITo[UBieG:ydH;zbZPDqA>? NGD6Unc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[xNFgzPyd-MkS2NVA5Ojd:L3G+
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KMH2 MWrGeY5kfGmxbjDBd5NigQ>? NUjERYM4OC13IN88US=> M{OyXlI1KGh? M4LLVYlvcGmkaYTzJGpCUzJxU2TBWEB{cWewYXzpcoc> MkHRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4MUC4NlcoRjJ2NkGwPFI4RC:jPh?=
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SUPHD1 MULGeY5kfGmxbjDBd5NigQ>? NIXkS|gxNTVizszN MVuyOEBp NVPEeIVjcW6qaXLpeJMhUkGNMj;TWGFVKHOrZ37hcIlv\w>? M3n5TFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkGwPFI4Lz5{NE[xNFgzPzxxYU6=
HDLM2 MWLGeY5kfGmxbjDBd5NigQ>? M3PGU|AuPSEQvF2= MmnrNlQhcA>? M3L5XYlvcGmkaYTzJGpCUzJxU2TBWEB{cWewYXzpcoc> MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZzMEiyO{c,OjR4MUC4Nlc9N2F-
K1106P MXXGeY5kfGmxbjDBd5NigQ>? M1K1d|AuPSEQvF2= MmDMNlQhcA>? NIe1W3RqdmirYnn0d{BLSUt{L2PURXQhe2mpbnHsbY5o MmGxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4MUC4NlcoRjJ2NkGwPFI4RC:jPh?=
MM.1S  MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTFvMzFOwG0> NV[0SJlQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1PFQyODFpPkK0OVg1OTBzPD;hQi=>
TpoR JAK2 WT MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHn2[FVKSzVyPUGuOEApOS5|4pETNU42MSEQvF2= MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJ3MUe5NEc,OjR{NUG3PVA9N2F-
TpoR JAK2 V617F NY\kb|hHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vKRWlEPTB;MD64JEgxNjgkgKOwMlkqKM7:TR?= MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJ3MUe5NEc,OjR{NUG3PVA9N2F-
TpoR W515L NFPFXZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTBwODCoNE446oDVMT6wLUDPxE1? Mnz6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR{NUG3PVAoRjJ2MkWxO|kxRC:jPh?=
Bcr-abl NHzTUJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7I[45KSzVyPUKuO{ApOi5{4pETN{4{MSEQvF2= M{fx[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MkWxO|kxLz5{NEK1NVc6ODxxYU6=
JAK2 TW NUf0d4xXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEL5UpFKSzVyPUGuPEApOS534pETNk4{MSEQvF2= MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJ3MUe5NEc,OjR{NUG3PVA9N2F-
JAK2 V617F M{jBfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHNcFdRUUN3ME2wMlYhMDBwNvMAl|AvPylizszN MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJ3MUe5NEc,OjR{NUG3PVA9N2F-
MedB-1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHucpQ1KM7:TR?= NUDIWGdrOjRxNEivO|IhcA>? MUPEUXNQ M{LUVolvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> NVyxc29lRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OVI{PjZpPkKzPFUzOzZ4PD;hQi=>
K1106 M4TLUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{TodlQh|ryP MWOyOE81QC95MjDo M2jQTmROW09? NIrJcIRqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 NGjaeWM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i1NlM3Pid-MkO4OVI{PjZ:L3G+
U2940 M3TsTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17Q[|Qh|ryP MVOyOE81QC95MjDo M1fsfWROW09? Mnu4bY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> NYX3UZpJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OVI{PjZpPkKzPFUzOzZ4PD;hQi=>
FE-PD MmfmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWiwMlA3Oy12IN88US=> MYjJR|UxRTlwNTFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? NXrOPYdVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzO|I3PjlpPkKzN|czPjZ7PD;hQi=>
HEL MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHn2SGYxNjB4Mz20JO69VQ>? MYPJR|UxRTFwNTFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? M172eVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{eyOlY6Lz5{M{O3NlY3QTxxYU6=
K-562 NHjKTVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWr1S5BHOC5yNkOtOEDPxE1? M{f2emlEPTB;Mj61JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= NYHZ[YZvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzO|I3PjlpPkKzN|czPjZ7PD;hQi=>
L-82 M{HiT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDWPFlbOC5yNkOtOEDPxE1? NEfncFlKSzVyPUCuPVgh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN5Mk[2PUc,OjN|N{K2Olk9N2F-
MAC-1 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXSwMlA3Oy12IN88US=> NUTkUGFLUUN3ME2wMlUzKM7:TTygbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> M2nWXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{eyOlY6Lz5{M{O3NlY3QTxxYU6=
MAC-2A NIjr[pFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXiwMlA3Oy12IN88US=> MmLvTWM2OD1yLk[5JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= MmrFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|N{K2OlkoRjJ|M{eyOlY6RC:jPh?=
MAC-2B MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX:wSZRbOC5yNkOtOEDPxE1? NHTYTGxKSzVyPUCuOVQh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NYfJ[3F[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzO|I3PjlpPkKzN|czPjZ7PD;hQi=>
MY-LA NVewe211T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDBNE4xPjNvNDFOwG0> NIXjUoJKSzVyPUKuNUDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= NXf5WVlYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzO|I3PjlpPkKzN|czPjZ7PD;hQi=>
NC-NC NVLQNoRWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rR[FAvODZ|LUSg{txO Mkn6TWM2OD1zLkCg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 M2TyV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{eyOlY6Lz5{M{O3NlY3QTxxYU6=
SE-AX M3HpN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXSwMlA3Oy12IN88US=> M1jrdGlEPTB;MT61JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= NGDI[mw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O3NlY3QSd-MkOzO|I3Pjl:L3G+
SR-786 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\1WVAvODZ|LUSg{txO NGPYWIhKSzVyPUSuOkDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= NUnZZ5VtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzO|I3PjlpPkKzN|czPjZ7PD;hQi=>
M-MOK  M{nCS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHWNodsOjViwsXNxsA> NIO5XYUzPC92OD:3NkBp MlrqSG1UVw>? MlS1bY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> M{izd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOEWzNVU4Lz5{MUi1N|E2PzxxYU6=
HEL NUXPe2lqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\UTWM2OD1|MEWgcm0> M1zQVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6M{m0OVU1Lz5zOEO5OFU2PDxxYU6=
Ba/F3 JAK2V617F NF60XlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTJ5MDDuUS=> NXfrOnBpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUizPVQ2PTRpPkG4N|k1PTV2PD;hQi=>
MV4-11 MXzBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MoHLO|IhcHK| NFHOSW5CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3WOE0yOSClZXzsd{Bi\nSncjC3NkBpenNiYomgZ4VtdHSrdHXyMYJtfWViYYPzZZktKEWFNUCgQUAxNjB5OTFOwG0v Mm\tQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OECyOlEoRjJ6MkiwNlYyRC:jPh?=
MM1S NFLnSVZCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M2X6OVczKGi{cx?= M4D5[WFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTV2xV{Bk\WyuczDh[pRmeiB5MjDodpMh[nlidIL5dIFvKGKudXWg[ZhkdHW|aX;uJIF{e2G7LDDJR|UxKD1iMTFOwG0v NYjpVJR5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyPFAzPjFpPkK4NlgxOjZzPD;hQi=>
NB1643 M{nUe5FJXFNiYYPzZZk> NHzYTYRyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKxOlQ{KGOnbHzz MnLyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC M3Kz[ZFJXFNiYYPzZZk> M4ToN5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMW1EKGOnbHzz M13jXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=

... 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
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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID