Fedratinib (TG101348)

For research use only.

Catalog No.S2736 Synonyms: SAR302503

53 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 53 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 Mk\YRZBweHSxc3nzJGF{e2G7 Mlj4NE42NTJizszN NXTsV2NNOTJvNEigbC=> MUPEUXNQ M2XoXYlv\HWlZYOgZZBweHSxc3nzJIlvKGKxdHig[I9{\S1iYX7kJJRqdWVvIHTldIVv\GWwdDDtZY5v\XJ? NWXzcVBmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4OlkzOTBpPkK1PFY6OjFyPD;hQi=>
H1650 NY\4NYJKSXCxcITvd4l{KEG|c3H5 MX[wMlUuOiEQvF2= Ml3rNVIuPDhiaB?= NITyPWxFVVOR NFnIfmNqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCkb4ToJIRwe2VvIHHu[EB1cW2nLTDk[ZBmdmSnboSgcYFvdmW{ M1PHWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OE[5NlExLz5{NUi2PVIyODxxYU6=
H1975 MkLKSpVv[3Srb36gRZN{[Xl? NW\ZR4Y3OC5{NT2xJO69VQ>? M2HJSlI1KGh? NF7IS|VFVVOR M1Lxb4lvcGmkaYTzJIV5eHKnc4Ppc44hd2ZiYYDvdJRwe2m|LYLlcIF1\WRicILveIVqdiCEY3ytXGwtKEKlbD2yMEB{fXK4aY\pckwhYEmDUB?= MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh4OUKxNEc,OjV6NkmyNVA9N2F-
H1650 M3vTN2Z2dmO2aX;uJGF{e2G7 MWqwMlI2NTFizszN NUHYTZhOOjRiaB?= M4TFfmROW09? MofXbY5pcWKrdIOg[ZhxemW|c3nvckBw\iCjcH;weI9{cXNvcnXsZZRm\CCycn;0[YlvKEKlbD3YUEwhSmOuLUKsJJN2en[rdnnuMEBZUUGS NEjlNmk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUi2PVIyOCd-MkW4OlkzOTB:L3G+
H1975 NHjhPGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\YNUDPxE1? MojrOFghcA>? MlzaSG1UVw>? MXXz[Y5{cXSrenXzJINmdGy|IITvJJRp\SCleYTveI95cWOrdImgc4Yh\XKub4Tpcolj MlHsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6NkmyNVAoRjJ3OE[5NlExRC:jPh?=
H1650 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\6SYVHOSEQvF2= M4DLOlQ5KGh? MnrGSG1UVw>? M4HOeJNmdnOrdHn6[ZMh[2WubIOgeI8hfGinIHP5eI91d3irY3n0fUBw\iCncnzveIlvcWJ? NXTnb2FYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4OlkzOTBpPkK1PFY6OjFyPD;hQi=>
CD4+ T MULGeY5kfGmxbjDBd5NigQ>? MkHtNE4xOS1zIN88US=> MljEOFghcA>? MonuSG1UVw>? M4\vT5Jm\HWlZYOgeIhmKHCqb4PwbI9zgWyjdHnvckBt\X[nbIOgc4YhUkGNMjDhcoQhW1SDVERCpC=> NGC2UVg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUW3NlU{PSd-MkW1O|I2OzV:L3G+
Caco-2  NWDJ[o1pTnWwY4Tpc44hSXO|YYm= NHP0R4ExNTF{MDFOwG0> Ml\WO{BucW5? NEXrfWVqdmirYnn0d{B1cGmjbXnu[UB2eHSja3Wge4l1cCCjbjDJR|UxyqCxZjCyMlHDqML3TR?= NIjNRXU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC2N|Y4Oid-MkWwOlM3PzJ:L3G+
Caco-2  NYDofWJbTnWwY4Tpc44hSXO|YYm= NX3sUGg3OTBxNUCvNVAxKM7:TR?= NH;Sc4UzKGh? NEC0PIRl\WO{ZXHz[ZMhfGinIH\seZghd2ZiW{PIYZRpcWGvaX7lJIFkem:|czD0bIUhdW:wb3zhfYVzKHerdHigTWM2OCCxZjC2MlXDqM7:TR?= NFGx[JU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC2N|Y4Oid-MkWwOlM3PzJ:L3G+
HEK293 MSR  NF\VcpNHfW6ldHnvckBCe3OjeR?= NHK3SHIxNTFyIN88US=> NYLO[2p3PyCvaX6= MYPpcohq[mm2czDoWGhVWjJid3n0bEBidiCLQ{WwxsBw\iBzLkNCpOK2VQ>? M2i5XVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3ME[zOlczLz5{NUC2N|Y4OjxxYU6=
MedB-1 NVvBR5NtTnWwY4Tpc44hSXO|YYm= MVexM|Ih|ryP NYOyOXZsOjRiaB?= MYrk[YNz\WG|ZYOgV3RCXDZicHjvd5Bpd3K7bHH0bY9vKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> MnnUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7N{e2OlgoRjJ2OUe3OlY5RC:jPh?=
U2940 NGr4d4pHfW6ldHnvckBCe3OjeR?= MX[xM|Ih|ryP NUT5R3RrOjRiaB?= MkGx[IVkemWjc3XzJHNVSVR4IIDoc5NxcG:{eXzheIlwdiClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 MlXtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7N{e2OlgoRjJ2OUe3OlY5RC:jPh?=
K1106 MUPGeY5kfGmxbjDBd5NigQ>? NIXCWXMyNzJizszN M1;pdVI1KGh? MX;k[YNz\WG|ZYOgV3RCXDZicHjvd5Bpd3K7bHH0bY9vKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> MkjoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7N{e2OlgoRjJ2OUe3OlY5RC:jPh?=
K562 M{HX[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnENpZzOC1zIN88US=> NGm0cIY4OiCq M1LzZ4lvcGmkaYTzJGs2PjJiY3XscEBxem:uaX\ldoF1cW:wIHH0JIhq\2hiY3;uZ4VvfHKjdHnvci=> MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd5NUOwPEc,OjR5N{WzNFg9N2F-
MDA-MB-468  NXrvVGdOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7IWJJnOyEEtV2= NWDPPZJ2PDhiaB?= M134eYVvcGGwY3XkJJNq[mOuNjDpcoR2[2WmIHzvd5Mhd2ZiY3XscEB3cWGkaXzpeJnDqA>? MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ4MkixPEc,OjR4NkK4NVg9N2F-
MDA-MB-468 M1TQO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHwNE01KM7:TR?= MWi0PEBp NW\0bnlPemW|dXz0d{B{cWewaX\pZ4FvfCCub4PzJI9nKH[rYXLpcIl1gSClb33wZZJm\CC2bzDSTU1DWEliYXzvcoU> NFTxWpk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[2NlgyQCd-MkS2OlI5OTh:L3G+
L428 NXLIdWVLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfUboJTOC13IN88US=> NHe0[4o1QCCq NYnvfIxpcW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> M3[yd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkGwPFI4Lz5{NE[xNFgzPzxxYU6=
KMH2 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUOwMVUh|ryP M1rLOVQ5KGh? NF7UcmpqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 NXq5b2RHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2NVA5OjdpPkK0OlExQDJ5PD;hQi=>
L1236 NHPGXmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jWcVAuPSEQvF2= NFTXVGo1QCCq NFy0XmFqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 M12zWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkGwPFI4Lz5{NE[xNFgzPzxxYU6=
SUPHD1 Mn\MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{Kw[|AuPSEQvF2= NELsO5E1QCCq NUiwWXBKcW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> M{DwZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkGwPFI4Lz5{NE[xNFgzPzxxYU6=
HDLM2 M2HnZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHa[nROOC13IN88US=> NW[0emlSPDhiaB?= NFTMO2VqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZzMEiyO{c,OjR4MUC4Nlc9N2F-
K1106P NUGyfJJrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPMcXU{OC13IN88US=> MUC0PEBp NX7X[3B[cW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> NH3KO2U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[xNFgzPyd-MkS2NVA5Ojd:L3G+
L428 NIrMdlVCeG:ydH;zbZMhSXO|YYm= NY[1e4hMOC9yLk[yOU8yNjJ3IN88US=> M1qwcVQ5KGh? MoL3bY5lfWOnczD0bIUh[XCxcITvd4l{yqB? MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZzMEiyO{c,OjR4MUC4Nlc9N2F-
KMH2 Mn65RZBweHSxc3nzJGF{e2G7 MWmwM|AvPjJ3L{GuNlUh|ryP M1;UNVQ5KGh? NUfCbHFHcW6mdXPld{B1cGViYYDvdJRwe2m|wrC= MoXxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4MUC4NlcoRjJ2NkGwPFI4RC:jPh?=
L1236 NGLrW2pCeG:ydH;zbZMhSXO|YYm= M3zYOVAwOC54MkWvNU4zPSEQvF2= M{LuNVQ5KGh? MWHpcoR2[2W|IITo[UBieG:ydH;zbZPDqA>? M4[3S|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkGwPFI4Lz5{NE[xNFgzPzxxYU6=
SUPHD1 NEjOOm1CeG:ydH;zbZMhSXO|YYm= NUnuTZMxOC9yLk[yOU8yNjJ3IN88US=> MnzQOFghcA>? M{[xO4lv\HWlZYOgeIhmKGGyb4D0c5Nqe8Li MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZzMEiyO{c,OjR4MUC4Nlc9N2F-
HDLM2 M{\1PWFxd3C2b4Ppd{BCe3OjeR?= MVqwM|AvPjJ3L{GuNlUh|ryP NEfZeHE1QCCq NW\4blhscW6mdXPld{B1cGViYYDvdJRwe2m|wrC= NUn5fmRCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2NVA5OjdpPkK0OlExQDJ5PD;hQi=>
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KMH2 MVXGeY5kfGmxbjDBd5NigQ>? M4PXWlAuPSEQvF2= NEOyXW0zPCCq M3fYWIlvcGmkaYTzJGpCUzJxU2TBWEB{cWewYXzpcoc> NImwSm49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[xNFgzPyd-MkS2NVA5Ojd:L3G+
L1236 NFvxOoxHfW6ldHnvckBCe3OjeR?= NHLCbngxNTVizszN M2rZ[lI1KGh? NFvRcHNqdmirYnn0d{BLSUt{L2PURXQhe2mpbnHsbY5o MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZzMEiyO{c,OjR4MUC4Nlc9N2F-
SUPHD1 NW[1NWF[TnWwY4Tpc44hSXO|YYm= MmnPNE02KM7:TR?= M1jJZlI1KGh? MYrpcohq[mm2czDKRWszN1OWQWSgd4lodmGuaX7n NFn3ZoU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[xNFgzPyd-MkS2NVA5Ojd:L3G+
HDLM2 NH7te49HfW6ldHnvckBCe3OjeR?= MmXENE02KM7:TR?= MmXpNlQhcA>? M4S0W4lvcGmkaYTzJGpCUzJxU2TBWEB{cWewYXzpcoc> MmnLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4MUC4NlcoRjJ2NkGwPFI4RC:jPh?=
K1106P NV;CN5pJTnWwY4Tpc44hSXO|YYm= MoPpNE02KM7:TR?= MUOyOEBp MmLYbY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> NEe4XHg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[xNFgzPyd-MkS2NVA5Ojd:L3G+
MM.1S  M{noTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTFvMzFOwG0> NHHTW|Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW4OFExOSd-MkS1PFQyODF:L3G+
TpoR JAK2 WT MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTFwNDCoNU4{6oDVMT61LUDPxE1? MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJ3MUe5NEc,OjR{NUG3PVA9N2F-
TpoR JAK2 V617F NUnQWmk1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTEbFB{UUN3ME2wMlghMDBwN,MAl|AvQSlizszN NVLDe2NxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyOVE4QTBpPkK0NlUyPzlyPD;hQi=>
TpoR W515L MmrNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\wTWM2OD1yLkigLFAvP+LCk{GuNEkh|ryP NWLtRmJoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyOVE4QTBpPkK0NlUyPzlyPD;hQi=>
Bcr-abl NFXtZo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTJwNzCoNk4z6oDVMz6zLUDPxE1? M4DUcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MkWxO|kxLz5{NEK1NVc6ODxxYU6=
JAK2 TW MnHmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjVUlNWUUN3ME2xMlghMDFwNfMAl|IvOylizszN NHTSd4M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEK1NVc6OCd-MkSyOVE4QTB:L3G+
JAK2 V617F MoLwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PFU2lEPTB;MD62JEgxNjckgKOwMlcqKM7:TR?= NHjY[Jc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEK1NVc6OCd-MkSyOVE4QTB:L3G+
MedB-1 NYj2e|ZCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jKUFQh|ryP MX6yOE81QC95MjDo NIG4e2RFVVOR NYm1SZlycW6qaXLpeJMh[2WubDDndo94fGhidHnt[UBl\XCnbnTlcpRtgQ>? MlHVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6NUKzOlYoRjJ|OEWyN|Y3RC:jPh?=
K1106 NGe1Z5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDTWlZtPCEQvF2= Mn\4NlQwPDhxN{KgbC=> M{D2RWROW09? MnvJbY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh3MkO2Okc,OjN6NUKzOlY9N2F-
U2940 NVS0SpZqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{P4SlQh|ryP NF3mToMzPC92OD:3NkBp MXvEUXNQ M{PQPIlvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh3MkO2Okc,OjN6NUKzOlY9N2F-
FE-PD MmHES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFGwO3ExNjB4Mz20JO69VQ>? MULJR|UxRTlwNTFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? M1LrTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{eyOlY6Lz5{M{O3NlY3QTxxYU6=
HEL NYTiXI5XT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIe5O2oxNjB4Mz20JO69VQ>? MULJR|UxRTFwNTFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? M1jLeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{eyOlY6Lz5{M{O3NlY3QTxxYU6=
K-562 M2XK[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnre2QxNjB4Mz20JO69VQ>? NXjCZW94UUN3ME2yMlUh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NVHZWXFqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzO|I3PjlpPkKzN|czPjZ7PD;hQi=>
L-82 MlzSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWiwSlFIOC5yNkOtOEDPxE1? NUDtVHpmUUN3ME2wMlk5KM7:TTygbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MofiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|N{K2OlkoRjJ|M{eyOlY6RC:jPh?=
MAC-1 NHfpZZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFKyWWsxNjB4Mz20JO69VQ>? NGfHT3hKSzVyPUCuOVIh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MoDsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|N{K2OlkoRjJ|M{eyOlY6RC:jPh?=
MAC-2A NX7ye5FnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13rUVAvODZ|LUSg{txO NUf6enpDUUN3ME2wMlY6KM7:TTygbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MlLzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|N{K2OlkoRjJ|M{eyOlY6RC:jPh?=
MAC-2B NEPrVW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVSwMlA3Oy12IN88US=> NVnOeVNvUUN3ME2wMlU1KM7:TTygbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MnnNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|N{K2OlkoRjJ|M{eyOlY6RC:jPh?=
MY-LA NFHNNYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\TXFAvODZ|LUSg{txO NHLjXW1KSzVyPUKuNUDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= M1zTTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{eyOlY6Lz5{M{O3NlY3QTxxYU6=
NC-NC NUjtc|N2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfyR5QxNjB4Mz20JO69VQ>? NHHLNVRKSzVyPUGuNEDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= Mli1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|N{K2OlkoRjJ|M{eyOlY6RC:jPh?=
SE-AX M{C4Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXewMlA3Oy12IN88US=> MlXiTWM2OD1zLkWg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 NFvLfnY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O3NlY3QSd-MkOzO|I3Pjl:L3G+
SR-786 MkXzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnLRpUxNjB4Mz20JO69VQ>? NXu5cGs6UUN3ME20MlYh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN5Mk[2PUc,OjN|N{K2Olk9N2F-
M-MOK  MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jwWFI2KML3TdMg M{fDRlI1NzR6L{eyJIg> NFzDZo1FVVOR NHjOTGxqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 MlGyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF6NUOxOVcoRjJzOEWzNVU4RC:jPh?=
HEL MoHqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;6eI5KSzVyPUOwOUBvVQ>? MojJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh|OUS1OVQoRjF6M{m0OVU1RC:jPh?=
Ba/F3 JAK2V617F M1fvT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTJ5MDDuUS=> NXXBfpdbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUizPVQ2PTRpPkG4N|k1PTV2PD;hQi=>
MV4-11 NFTlZphCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NGXsXHk4OiCqcoO= NWjLO2NrSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNWlQuOTFiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JINmdGy2aYTldk1jdHWnIHHzd4F6NCCHQ{WwJF0hOC5yN{mg{txONg>? Mm[2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OECyOlEoRjJ6MkiwNlYyRC:jPh?=
MM1S MVjBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M3rnelczKGi{cx?= MnG1RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPTUHTJINmdGy|IHHmeIVzKDd{IHjyd{BjgSC2conwZY4h[my3ZTDlfINtfXOrb36gZZN{[XluIFnDOVAhRSBzIN88UU4> NHPnOZQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEK4NFI3OSd-MkiyPFAzPjF:L3G+
NB1643 MlnMdWhVWyCjc4PhfS=> M17UZZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQkG2OFMh[2WubIO= MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-MC MnHSdWhVWyCjc4PhfS=> NY\4UYtzeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uVUNiY3XscJM> MlPwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=

... 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
NCT04702464 Not yet recruiting Drug: Fedratinib|Drug: Fluconazole Healthy Volunteers Celgene|Impact Biomedicines Inc. a wholly owned subsidiary of Celgene Corporation January 8 2021 Phase 1
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
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