Fedratinib (TG101348)

Catalog No.S2736 Synonyms: SAR302503

For research use only.

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.

Fedratinib (TG101348) Chemical Structure

CAS No. 936091-26-8

Selleck's Fedratinib (TG101348) has been cited by 63 publications

Purity & Quality Control

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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 M3jZN2Fxd3C2b4Ppd{BCe3OjeR?= MYOwMlUuOiEQvF2= MmLiNVIuPDhiaB?= NHHLW5BFVVOR M4e1PIlv\HWlZYOgZZBweHSxc3nzJIlvKGKxdHig[I9{\S1iYX7kJJRqdWVvIHTldIVv\GWwdDDtZY5v\XJ? NHnp[mg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUi2PVIyOCd-MkW4OlkzOTB:L3G+
H1650 NYex[HZoSXCxcITvd4l{KEG|c3H5 MmG5NE42NTJizszN M2fMNFEzNTR6IHi= NIjOWGdFVVOR NVXS[mJ[cW6mdXPld{BieG:ydH;zbZMhcW5iYn;0bEBld3OnLTDhcoQhfGmvZT2g[IVx\W6mZX70JI1idm6nch?= M4D2fVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OE[5NlExLz5{NUi2PVIyODxxYU6=
H1975 NVXUZZBVTnWwY4Tpc44hSXO|YYm= M3fIcVAvOjVvMTFOwG0> NET2RmczPCCq NX:0e2d6TE2VTx?= MVTpcohq[mm2czDlfJBz\XO|aX;uJI9nKGGyb4D0c5Nqey2{ZXzheIVlKHC{b4TlbY4hSmOuLWjMMEBD[2xvMjygd5Vzfmm4aX6sJHhKSVB? M1zieVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OE[5NlExLz5{NUi2PVIyODxxYU6=
H1650 NWTlcldlTnWwY4Tpc44hSXO|YYm= NFPXbVQxNjJ3LUGg{txO NGnENoUzPCCq M1PFemROW09? NUDpeJpWcW6qaXLpeJMh\XiycnXzd4lwdiCxZjDhdI9xfG:|aYOtdoVt[XSnZDDwdo91\WmwIFLjcE1ZVCxiQnPsMVItKHO3co\peolvNCC[SVHQ NUKzZmE4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4OlkzOTBpPkK1PFY6OjFyPD;hQi=>
H1975 MmDHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYKxJO69VQ>? MUm0PEBp M2jX[WROW09? MkDYd4Vve2m2aYrld{Bk\WyuczD0c{B1cGViY4n0c5RwgGmlaYT5JI9nKGW{bH;0bY5q[g>? M1nrd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OE[5NlExLz5{NUi2PVIyODxxYU6=
H1650 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVmxJO69VQ>? M3ewdlQ5KGh? NWLabYZrTE2VTx?= MkjZd4Vve2m2aYrld{Bk\WyuczD0c{B1cGViY4n0c5RwgGmlaYT5JI9nKGW{bH;0bY5q[g>? NIGxbm89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUi2PVIyOCd-MkW4OlkzOTB:L3G+
CD4+ T MUfGeY5kfGmxbjDBd5NigQ>? MkT0NE4xOS1zIN88US=> Mlv1OFghcA>? NVXTSJhXTE2VTx?= NXfPb3lWemWmdXPld{B1cGVicHjvd5Bpd3K7bHH0bY9vKGyndnXsd{Bw\iCMQVuyJIFv\CCVVFHUN:Kh MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTV5MkWzOUc,OjV3N{K1N|U9N2F-
Caco-2  MmrsSpVv[3Srb36gRZN{[Xl? NVO4WJR5OC1zMkCg{txO MWK3JI1qdg>? NUGyXXU3cW6qaXLpeJMhfGirYX3pcoUhfXC2YXvlJJdqfGhiYX6gTWM2OMLib3[gNk4yyqEEtV2= MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB4M{[3Nkc,OjVyNkO2O|I9N2F-
Caco-2  M2HWSWZ2dmO2aX;uJGF{e2G7 NWOzV|hLOTBxNUCvNVAxKM7:TR?= NHy1bFkzKGh? NX\sXHpR\GWlcnXhd4V{KHSqZTDmcJV5KG:oIGuzTH11cGmjbXnu[UBi[3Kxc4OgeIhmKG2xbn;sZZlmeiC5aYToJGlEPTBib3[gOk42yqEQvF2= MkPGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyNkO2O|IoRjJ3ME[zOlczRC:jPh?=
HEK293 MSR  M4jkc2Z2dmO2aX;uJGF{e2G7 M4TxS|AuOTBizszN M2e4WVchdWmw NYK4bpRYcW6qaXLpeJMhcFSKVGKyJJdqfGhiYX6gTWM2OMLib3[gNU4zyqEEtV2= NF\FXWU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC2N|Y4Oid-MkWwOlM3PzJ:L3G+
MedB-1 MV\GeY5kfGmxbjDBd5NigQ>? NXjO[ZZSOS9{IN88US=> MWiyOEBp NF7zSmJl\WO{ZXHz[ZMhW1SDVE[gdIhwe3Cqb4L5cIF1cW:wIHPvcoNmdnS{YYTpc44h\GWyZX7k[Y51dHl? M3q2UVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUe3OlY5Lz5{NEm3O|Y3QDxxYU6=
U2940 NHr4OllHfW6ldHnvckBCe3OjeR?= MXOxM|Ih|ryP MkPXNlQhcA>? MUHk[YNz\WG|ZYOgV3RCXDZicHjvd5Bpd3K7bHH0bY9vKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> M{DOc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUe3OlY5Lz5{NEm3O|Y3QDxxYU6=
K1106 MWDGeY5kfGmxbjDBd5NigQ>? NG\0NVYyNzJizszN NYX3O5BtOjRiaB?= M3TvUYRm[3KnYYPld{BUXEGWNjDwbI9{eGixconsZZRqd25iY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? M2\YbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUe3OlY5Lz5{NEm3O|Y3QDxxYU6=
K562 M1rzVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPHZW5WOC1zIN88US=> NHzVUGU4OiCq NXi2SGo5cW6qaXLpeJMhUzV4MjDj[YxtKHC{b3zp[oVz[XSrb36gZZQhcGmpaDDjc45k\W62cnH0bY9v M2Lw[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2N{e1N|A5Lz5{NEe3OVMxQDxxYU6=
MDA-MB-468  MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnToN{DDvU1? MWW0PEBp MW\lcohidmOnZDDzbYJkdDZiaX7keYNm\CCub4PzJI9nKGOnbHygeoli[mmuaYT5xsA> NEP3clU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[2NlgyQCd-MkS2OlI5OTh:L3G+
MDA-MB-468 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2G1XFAuPCEQvF2= MlfaOFghcA>? NInKcHpz\XO3bITzJJNq\26rZnnjZY51KGyxc4Ogc4YhfmmjYnnsbZR6KGOxbYDhdoVlKHSxIGLJMWJRUSCjbH;u[S=> NUi4XJFKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OlI5OThpPkK0OlYzQDF6PD;hQi=>
L428 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTNWHoxNTVizszN NX74Om0yPDhiaB?= NV\qZW9TcW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> NF7SV5Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[xNFgzPyd-MkS2NVA5Ojd:L3G+
KMH2 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLhNGR[OC13IN88US=> NVLI[Hk2PDhiaB?= MWjpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 NULYO5lHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2NVA5OjdpPkK0OlExQDJ5PD;hQi=>
L1236 MoXZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVOwMVUh|ryP NELLRXQ1QCCq NVLh[oVncW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> M2LSflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkGwPFI4Lz5{NE[xNFgzPzxxYU6=
SUPHD1 M1LMd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7VU4IxNTVizszN NV72fJI1PDhiaB?= M3XobolvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZzMEiyO{c,OjR4MUC4Nlc9N2F-
HDLM2 Mn35S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrFNE02KM7:TR?= Mn7ROFghcA>? M2PHXolvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZzMEiyO{c,OjR4MUC4Nlc9N2F-
K1106P NGnzZm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEHtWocxNTVizszN MXy0PEBp MVjpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 NEP1Xlg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[xNFgzPyd-MkS2NVA5Ojd:L3G+
L428 NF7uTXVCeG:ydH;zbZMhSXO|YYm= MmriNE8xNjZ{NT:xMlI2KM7:TR?= MXK0PEBp MmHtbY5lfWOnczD0bIUh[XCxcITvd4l{yqB? MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZzMEiyO{c,OjR4MUC4Nlc9N2F-
KMH2 NYL0OZY3SXCxcITvd4l{KEG|c3H5 MUCwM|AvPjJ3L{GuNlUh|ryP MnHpOFghcA>? MnHxbY5lfWOnczD0bIUh[XCxcITvd4l{yqB? MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZzMEiyO{c,OjR4MUC4Nlc9N2F-
L1236 MnLuRZBweHSxc3nzJGF{e2G7 Mn63NE8xNjZ{NT:xMlI2KM7:TR?= NGnX[3o1QCCq MnnEbY5lfWOnczD0bIUh[XCxcITvd4l{yqB? MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZzMEiyO{c,OjR4MUC4Nlc9N2F-
SUPHD1 NYrXXG9oSXCxcITvd4l{KEG|c3H5 MYOwM|AvPjJ3L{GuNlUh|ryP NHLjSnU1QCCq NHnacI9qdmS3Y3XzJJRp\SCjcH;weI9{cXQEoB?= NX\tR21URGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2NVA5OjdpPkK0OlExQDJ5PD;hQi=>
HDLM2 MYPBdI9xfG:|aYOgRZN{[Xl? M17rSFAwOC54MkWvNU4zPSEQvF2= M4O3N|Q5KGh? M1rSTolv\HWlZYOgeIhmKGGyb4D0c5Nqe8Li NIHFcHU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[xNFgzPyd-MkS2NVA5Ojd:L3G+
K1106P NUPQfJhLSXCxcITvd4l{KEG|c3H5 M1THZVAwOC54MkWvNU4zPSEQvF2= NVruOotLPDhiaB?= NHv1cJhqdmS3Y3XzJJRp\SCjcH;weI9{cXQEoB?= NELIZ2Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[xNFgzPyd-MkS2NVA5Ojd:L3G+
L428 NXK4S4ZDTnWwY4Tpc44hSXO|YYm= M3\PXFAuPSEQvF2= MlfGNlQhcA>? NHrzdodqdmirYnn0d{BLSUt{L2PURXQhe2mpbnHsbY5o NYPTVIdsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2NVA5OjdpPkK0OlExQDJ5PD;hQi=>
KMH2 M1vNZWZ2dmO2aX;uJGF{e2G7 M{Pv[lAuPSEQvF2= NVzYZ29xOjRiaB?= NHTjfYlqdmirYnn0d{BLSUt{L2PURXQhe2mpbnHsbY5o MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZzMEiyO{c,OjR4MUC4Nlc9N2F-
L1236 NFPSd49HfW6ldHnvckBCe3OjeR?= M3Tte|AuPSEQvF2= Mn[1NlQhcA>? NV\3RmNbcW6qaXLpeJMhUkGNMj;TWGFVKHOrZ37hcIlv\w>? MmLKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4MUC4NlcoRjJ2NkGwPFI4RC:jPh?=
SUPHD1 NUnp[4d[TnWwY4Tpc44hSXO|YYm= NFPldI0xNTVizszN NX2wdGpEOjRiaB?= NVzMb|hqcW6qaXLpeJMhUkGNMj;TWGFVKHOrZ37hcIlv\w>? MkfmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4MUC4NlcoRjJ2NkGwPFI4RC:jPh?=
HDLM2 MX\GeY5kfGmxbjDBd5NigQ>? NFrzemQxNTVizszN MlnnNlQhcA>? MkPhbY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> NGXyfoQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[xNFgzPyd-MkS2NVA5Ojd:L3G+
K1106P NHTiVYVHfW6ldHnvckBCe3OjeR?= NXXFXldKOC13IN88US=> NIrKTlUzPCCq NInOPGRqdmirYnn0d{BLSUt{L2PURXQhe2mpbnHsbY5o NHq0VVQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[xNFgzPyd-MkS2NVA5Ojd:L3G+
MM.1S  NF3ZSVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTFvMzFOwG0> NFTNRnk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW4OFExOSd-MkS1PFQyODF:L3G+
TpoR JAK2 WT M{Pp[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\FXWlEPTB;MT60JEgyNjQkgKOxMlUqKM7:TR?= MmC4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR{NUG3PVAoRjJ2MkWxO|kxRC:jPh?=
TpoR JAK2 V617F MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTBwODCoNE446oDVMD65LUDPxE1? MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJ3MUe5NEc,OjR{NUG3PVA9N2F-
TpoR W515L NWrJTFlNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnFTWM2OD1yLkigLFAvP+LCk{GuNEkh|ryP M2rNXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MkWxO|kxLz5{NEK1NVc6ODxxYU6=
Bcr-abl MkjoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrFTWM2OD1{LkegLFIvOuLCk{OuN{kh|ryP M{PsUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MkWxO|kxLz5{NEK1NVc6ODxxYU6=
JAK2 TW NV64bllUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUm4ZXVQUUN3ME2xMlghMDFwNfMAl|IvOylizszN M{jQOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MkWxO|kxLz5{NEK1NVc6ODxxYU6=
JAK2 V617F M162dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnINZhrUUN3ME2wMlYhMDBwNvMAl|AvPylizszN NWHvd2M3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyOVE4QTBpPkK0NlUyPzlyPD;hQi=>
MedB-1 NV\FXnh1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUj4TIlVPCEQvF2= NID5fHEzPC92OD:3NkBp NFS4NWdFVVOR NGDqWWtqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 MmPYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6NUKzOlYoRjJ|OEWyN|Y3RC:jPh?=
K1106 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3XpcFQh|ryP MV6yOE81QC95MjDo NFzyPWJFVVOR MmXQbY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> M4PqblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OEWyN|Y3Lz5{M{i1NlM3PjxxYU6=
U2940 NF\BSnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7xbJg1KM7:TR?= M2Hx[FI1NzR6L{eyJIg> MoLBSG1UVw>? MXLpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 NX\vSHdVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OVI{PjZpPkKzPFUzOzZ4PD;hQi=>
FE-PD NX:yfmVIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXQcnMxNjB4Mz20JO69VQ>? MVfJR|UxRTlwNTFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? NV\wb4dsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzO|I3PjlpPkKzN|czPjZ7PD;hQi=>
HEL NIn4UWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LGWlAvODZ|LUSg{txO M2PY[mlEPTB;MT61JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN5Mk[2PUc,OjN|N{K2Olk9N2F-
K-562 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUCwMlA3Oy12IN88US=> M3jncGlEPTB;Mj61JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN5Mk[2PUc,OjN|N{K2Olk9N2F-
L-82 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUTUdJlKOC5yNkOtOEDPxE1? M{OxWGlEPTB;MD65PEDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= M3K5cVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{eyOlY6Lz5{M{O3NlY3QTxxYU6=
MAC-1 M3flWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfBNE4xPjNvNDFOwG0> M3iyeGlEPTB;MD61NkDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= MoX6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|N{K2OlkoRjJ|M{eyOlY6RC:jPh?=
MAC-2A M3HkdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXqRpkxNjB4Mz20JO69VQ>? M1HveGlEPTB;MD62PUDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN5Mk[2PUc,OjN|N{K2Olk9N2F-
MAC-2B NHPkW|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13yZ|AvODZ|LUSg{txO Mlf0TWM2OD1yLkW0JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= M4PvVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{eyOlY6Lz5{M{O3NlY3QTxxYU6=
MY-LA MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{WzNVAvODZ|LUSg{txO NEfWWHpKSzVyPUKuNUDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= MkLsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|N{K2OlkoRjJ|M{eyOlY6RC:jPh?=
NC-NC MkTVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX64VZVkOC5yNkOtOEDPxE1? NHzYV4hKSzVyPUGuNEDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= NGD6VYY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O3NlY3QSd-MkOzO|I3Pjl:L3G+
SE-AX MmW4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYThUooxOC5yNkOtOEDPxE1? MYHJR|UxRTFwNTFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? M4HveVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{eyOlY6Lz5{M{O3NlY3QTxxYU6=
SR-786 NWDEcnJmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWqwMlA3Oy12IN88US=> NWOydpd5UUN3ME20MlYh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MkX0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|N{K2OlkoRjJ|M{eyOlY6RC:jPh?=
M-MOK  MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37v[|I2KML3TdMg M4fWOFI1NzR6L{eyJIg> MlzhSG1UVw>? NF3vcFVqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTh3M{G1O{c,OjF6NUOxOVc9N2F-
HEL M3i2Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfTTZFKSzVyPUOwOUBvVQ>? M3zlSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6M{m0OVU1Lz5zOEO5OFU2PDxxYU6=
Ba/F3 JAK2V617F M1Lk[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLSOmxPUUN3ME2yO|Ahdk1? M4XCPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6M{m0OVU1Lz5zOEO5OFU2PDxxYU6=
MV4-11 MYXBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NV7ZfI5mPzJiaILz MWPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2YND2xNUBk\WyuczDh[pRmeiB5MjDodpMh[nliY3XscJRqfGW{LXLseYUh[XO|YYmsJGVEPTBiPTCwMlA4QSEQvF2u M371SVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MkiwNlYyLz5{OEK4NFI3OTxxYU6=
MM1S NX3TUWdrSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= Mn7vO|IhcHK| MkjqRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPTUHTJINmdGy|IHHmeIVzKDd{IHjyd{BjgSC2conwZY4h[my3ZTDlfINtfXOrb36gZZN{[XluIFnDOVAhRSBzIN88UU4> MnvTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OECyOlEoRjJ6MkiwNlYyRC:jPh?=
NB1643 NHTIPGVyUFSVIHHzd4F6 MULxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJzNkSzJINmdGy| Ml3XQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC NGriOldyUFSVIHHzd4F6 MkG5dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO= MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Assay
Methods Test Index PMID
Western blot p-JAK2 / p-STAT1 / p-STAT3 / p-STAT6 / p-STAT5 / JAK2 ; c-Myc / PIM1 24610827
Growth inhibition assay Cell proliferation 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 (from reference)

Kinase Assay:

[1]

  • 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]

  • 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]

  • 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 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04955938 Not yet recruiting Drug: Ivosidenib|Drug: Enasidenib|Drug: Fedratinib IDH Mutation|IDH1 Mutation|IDH2 Gene Mutation|Blood Cancer|Myeloproliferative Neoplasm University of Chicago October 1 2021 Phase 1
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
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

(data from https://clinicaltrials.gov, updated on 2021-09-06)

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

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