Fedratinib (SAR302503, TG101348)

製品コードS2736

Fedratinib (SAR302503, TG101348)化学構造

分子量(MW):524.68

Fedratinib (SAR302503, TG101348) is a selective inhibitor of JAK2 with IC50 of 3 nM in cell-free assays, 35- and 334-fold more selective for JAK2 versus JAK1 and JAK3. Phase 2.

サイズ 価格(税別)  
JPY 36520.00
JPY 18260.00
JPY 28220.00
JPY 61420.00
JPY 94620.00

カスタマーフィードバック(4)

  • Colony-forming assay results showing that the Jak2 inhibitor TG101348 reduces CFU-GM colonies generated from mutant fetal liver R2 cells. Results from 4 independent control or mutant fetal livers treated with TG101348 or dimethylsulfoxide (DMSO) are shown (mean ?SD). ***P < .001.

    Blood 2014 123(20), 3175-84. Fedratinib (SAR302503, TG101348) purchased from Selleck.

    Effects of JAK2, STAT3, and STAT1 inhibitor on surface and total expression of PD-L1 in the lung adenocarcinoma cell line HCC4006. JAK2 inhibition suppresses surface and whole expression of PD-L1 in HCC4006 cells. HCC4006 cells were treated for 48 hours with the JAK2 pharmacological inhibitor TG101348 (200 nM or 500 nM) or DMSO. Surface (A) and total (B) expression of PD-L1 were evaluated by flow cytometry. Results are representative of five independent experiments. STAT3 inhibition suppresses total expression of PD-L1 in HCC4006 cells but has no effect on surface expression of PD-L1. HCC4006 cells were treated for 48 hours with the STAT3 pharmacological inhibitor BP-1-102 (0.5 μM or 5 μM) or DMSO. Surface (C) and total (D) expression of PD-L1 were evaluated by flow cytometry. Results are representative of four independent experiments. Asterisks indicate statistically significant differences between the experimental and DMSO-treated cells (*p < 0.05, **p < 0.01, ***p < 0.001).

    J Thorac Oncol, 2016, 11(1):62-71. Fedratinib (SAR302503, TG101348) purchased from Selleck.

  • Janus kinase (JAK) 1/2 inhibitors increase vesicular stomatitis virus-green fluorescent protein (VSV-GFP) susceptibility in SCC25 cells. Representative photographs of VSV infection in treated cells with and without JAK1/2 inhibitors.

    Cancer Gene Ther 2013 20, 582-9. Fedratinib (SAR302503, TG101348) purchased from Selleck.

    Claude HAAN Université du Luxembour. Fedratinib (SAR302503, TG101348) purchased from Selleck.

製品安全説明書

JAK阻害剤の選択性比較

生物活性

製品説明 Fedratinib (SAR302503, TG101348) is a selective inhibitor of JAK2 with IC50 of 3 nM in cell-free assays, 35- and 334-fold more selective for JAK2 versus JAK1 and JAK3. Phase 2.
ターゲット
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
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
H1975 MYTBdI9xfG:|aYOgRZN{[Xl? MnOwNE42NTJizszN MUexNk01QCCq Ml3xSG1UVw>? NFXGcpNqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCkb4ToJIRwe2VvIHHu[EB1cW2nLTDk[ZBmdmSnboSgcYFvdmW{ NHTkNG8zPTh4OUKxNC=>
H1650 MXfBdI9xfG:|aYOgRZN{[Xl? MkPvNE42NTJizszN M4\weFEzNTR6IHi= M{G0eWROW09? M{XrSYlv\HWlZYOgZZBweHSxc3nzJIlvKGKxdHig[I9{\S1iYX7kJJRqdWVvIHTldIVv\GWwdDDtZY5v\XJ? MkXwNlU5Pjl{MUC=
H1975 M2XsVWZ2dmO2aX;uJGF{e2G7 NIDh[o0xNjJ3LUGg{txO NWPjb|RIOjRiaB?= M2\CXmROW09? MXnpcohq[mm2czDlfJBz\XO|aX;uJI9nKGGyb4D0c5Nqey2{ZXzheIVlKHC{b4TlbY4hSmOuLWjMMEBD[2xvMjygd5Vzfmm4aX6sJHhKSVB? NY\ncGJQOjV6NkmyNVA>
H1650 MXrGeY5kfGmxbjDBd5NigQ>? MkTDNE4zPS1zIN88US=> NHPKd|EzPCCq NIXJN3lFVVOR M1L4dolvcGmkaYTzJIV5eHKnc4Ppc44hd2ZiYYDvdJRwe2m|LYLlcIF1\WRicILveIVqdiCEY3ytXGwtKEKlbD2yMEB{fXK4aY\pckwhYEmDUB?= MmnJNlU5Pjl{MUC=
H1975 NIfHOZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLpVFMyKM7:TR?= NGfPeGg1QCCq NGXpboFFVVOR MXXz[Y5{cXSrenXzJINmdGy|IITvJJRp\SCleYTveI95cWOrdImgc4Yh\XKub4Tpcolj MlTSNlU5Pjl{MUC=
H1650 M17mfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXGxJO69VQ>? M3jXTVQ5KGh? Mn3JSG1UVw>? M3r6bpNmdnOrdHn6[ZMh[2WubIOgeI8hfGinIHP5eI91d3irY3n0fUBw\iCncnzveIlvcWJ? MnLoNlU5Pjl{MUC=
CD4+ T MmLlSpVv[3Srb36gRZN{[Xl? MWiwMlAyNTFizszN NInDXXE1QCCq NFPjVYRFVVOR M{XPfJJm\HWlZYOgeIhmKHCqb4PwbI9zgWyjdHnvckBt\X[nbIOgc4YhUkGNMjDhcoQhW1SDVERCpC=> MYmyOVU4OjV|NR?=
Caco-2  NV;uRWdoTnWwY4Tpc44hSXO|YYm= M3jvVlAuOTJyIN88US=> Mo\2O{BucW5? MVrpcohq[mm2czD0bIlidWmwZTD1dJRic2Vid3n0bEBidiCLQ{WwxsBw\iB{LkJCpOK2VQ>? M4niVFI2ODZ|Nkey
Caco-2  NFXoOGZHfW6ldHnvckBCe3OjeR?= M3jsR|ExNzVyL{GwNEDPxE1? MVKyJIg> M3PyTYRm[3KnYYPld{B1cGViZnz1fEBw\iCdM1jdeIhq[W2rbnWgZYNzd3O|IITo[UBud26xbHH5[ZIhf2m2aDDJR|UxKG:oIE[uOeKh|ryP NE[xPJYzPTB4M{[3Ni=>
HEK293 MSR  NEjxcYVHfW6ldHnvckBCe3OjeR?= NV3JbmszOC1zMDFOwG0> MmHyO{BucW5? M{DRdIlvcGmkaYTzJIhVUFSUMjD3bZRpKGGwIFnDOVDDqG:oIEGuNuKhyrWP M3yz[|I2ODZ|Nkey
MedB-1 NIXje4hHfW6ldHnvckBCe3OjeR?= M1nzXlEwOiEQvF2= MoDvNlQhcA>? M{X5[4Rm[3KnYYPld{BUXEGWNjDwbI9{eGixconsZZRqd25iY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? NFXhWGczPDl5N{[2PC=>
U2940 M1GyO2Z2dmO2aX;uJGF{e2G7 MX6xM|Ih|ryP MVSyOEBp MUfk[YNz\WG|ZYOgV3RCXDZicHjvd5Bpd3K7bHH0bY9vKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> MY[yOFk4PzZ4OB?=
K1106 NGjTVmxHfW6ldHnvckBCe3OjeR?= M2DpeFEwOiEQvF2= NXvLXnRpOjRiaB?= NEjWVmVl\WO{ZXHz[ZMhW1SDVE[gdIhwe3Cqb4L5cIF1cW:wIHPvcoNmdnS{YYTpc44h\GWyZX7k[Y51dHl? MViyOFk4PzZ4OB?=
K562 M2fqWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrRXoUxNTFizszN M4DRTlczKGh? MVTpcohq[mm2czDLOVYzKGOnbHygdJJwdGmoZYLheIlwdiCjdDDobYdpKGOxbnPlcpRz[XSrb36= NX\2blZ1OjR5N{WzNFg>
MDA-MB-468  NXPtUZhwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vKWFMhyrWP NHnZSWE1QCCq MWLlcohidmOnZDDzbYJkdDZiaX7keYNm\CCub4PzJI9nKGOnbHygeoli[mmuaYT5xsA> MX6yOFY3OjhzOB?=
MDA-MB-468 NWHSWpFqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEO0cI8xNTRizszN NFHzelc1QCCq NGHrWG9z\XO3bITzJJNq\26rZnnjZY51KGyxc4Ogc4YhfmmjYnnsbZR6KGOxbYDhdoVlKHSxIGLJMWJRUSCjbH;u[S=> MYSyOFY3OjhzOB?=
L428 NELnOHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXsNE02KM7:TR?= NXL2[Yt{PDhiaB?= M1;ob4lvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= MX[yOFYyODh{Nx?=
KMH2 NVK0OJVqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\MNE02KM7:TR?= MnrjOFghcA>? MVjpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 NFTLT2ozPDZzMEiyOy=>
L1236 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVuwMVUh|ryP M37wNlQ5KGh? MYTpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 MlvTNlQ3OTB6Mke=
SUPHD1 NGqw[G5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGT2XmgxNTVizszN NH22S4E1QCCq MnzObY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= MnnFNlQ3OTB6Mke=
HDLM2 MkHIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXKNE02KM7:TR?= M1jTW|Q5KGh? MUfpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 MYqyOFYyODh{Nx?=
K1106P MnzJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX76Vo42OC13IN88US=> NUDrOYhZPDhiaB?= MlfObY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= NUDIdXFJOjR4MUC4Nlc>
L428 MWnBdI9xfG:|aYOgRZN{[Xl? NVLWTY97OC9yLk[yOU8yNjJ3IN88US=> MWK0PEBp MX;pcoR2[2W|IITo[UBieG:ydH;zbZPDqA>? NHzhSIEzPDZzMEiyOy=>
KMH2 NYDNTZI{SXCxcITvd4l{KEG|c3H5 M2Owe|AwOC54MkWvNU4zPSEQvF2= MUG0PEBp NUn5S2twcW6mdXPld{B1cGViYYDvdJRwe2m|wrC= NIXM[ZAzPDZzMEiyOy=>
L1236 M372dWFxd3C2b4Ppd{BCe3OjeR?= MnK3NE8xNjZ{NT:xMlI2KM7:TR?= MWe0PEBp MY\pcoR2[2W|IITo[UBieG:ydH;zbZPDqA>? NGnQUnczPDZzMEiyOy=>
SUPHD1 NV3YOYhUSXCxcITvd4l{KEG|c3H5 MnLINE8xNjZ{NT:xMlI2KM7:TR?= NHfGd281QCCq MoribY5lfWOnczD0bIUh[XCxcITvd4l{yqB? MnTJNlQ3OTB6Mke=
HDLM2 NUm0SVRQSXCxcITvd4l{KEG|c3H5 MUCwM|AvPjJ3L{GuNlUh|ryP M1q2flQ5KGh? M3;kcIlv\HWlZYOgeIhmKGGyb4D0c5Nqe8Li M4fQRlI1PjFyOEK3
K1106P NWPUSVVsSXCxcITvd4l{KEG|c3H5 NHXTRZQxNzBwNkK1M|EvOjVizszN MUO0PEBp MkH3bY5lfWOnczD0bIUh[XCxcITvd4l{yqB? NWrQdZZsOjR4MUC4Nlc>
L428 Mo\oSpVv[3Srb36gRZN{[Xl? Ml;zNE02KM7:TR?= NXq3fpVTOjRiaB?= MYHpcohq[mm2czDKRWszN1OWQWSgd4lodmGuaX7n MnWzNlQ3OTB6Mke=
KMH2 MU\GeY5kfGmxbjDBd5NigQ>? MWKwMVUh|ryP M{DNS|I1KGh? MnXIbY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> M2T4cFI1PjFyOEK3
L1236 M2rWOmZ2dmO2aX;uJGF{e2G7 NIDuU4UxNTVizszN MYiyOEBp NIHLXWdqdmirYnn0d{BLSUt{L2PURXQhe2mpbnHsbY5o MYOyOFYyODh{Nx?=
SUPHD1 MYHGeY5kfGmxbjDBd5NigQ>? M13uUVAuPSEQvF2= Mn3qNlQhcA>? NUfMSGdocW6qaXLpeJMhUkGNMj;TWGFVKHOrZ37hcIlv\w>? M4PXOlI1PjFyOEK3
HDLM2 NIPtV3VHfW6ldHnvckBCe3OjeR?= MmLtNE02KM7:TR?= M3fJbVI1KGh? MVnpcohq[mm2czDKRWszN1OWQWSgd4lodmGuaX7n MYSyOFYyODh{Nx?=
K1106P NHX5UnFHfW6ldHnvckBCe3OjeR?= MVywMVUh|ryP NIrBSFgzPCCq MUfpcohq[mm2czDKRWszN1OWQWSgd4lodmGuaX7n MlfPNlQ3OTB6Mke=
MM.1S  MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjPdFdCUUN3ME2xMVMh|ryP Mnu5NlQ2QDRzMEG=
TpoR JAK2 WT NXPWVGpXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXWUpE3UUN3ME2xMlQhMDFwM,MAl|EvPSlizszN MmPyNlQzPTF5OUC=
TpoR JAK2 V617F NUTHTI9[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3OxeGlEPTB;MD64JEgxNjgkgKOwMlkqKM7:TR?= MVeyOFI2OTd7MB?=
TpoR W515L MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTBwODCoNE446oDVMT6wLUDPxE1? NUXGXZRqOjR{NUG3PVA>
Bcr-abl MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2nYNWlEPTB;Mj63JEgzNjMkgKOzMlMqKM7:TR?= NVrPcmQ3OjR{NUG3PVA>
JAK2 TW MoW0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILiTIJKSzVyPUGuPEApOS534pETNk4{MSEQvF2= M1;he|I1OjVzN{mw
JAK2 V617F MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jpNWlEPTB;MD62JEgxNjckgKOwMlcqKM7:TR?= MWWyOFI2OTd7MB?=
MedB-1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXoZmg1KM7:TR?= NH7JeGMzPC92OD:3NkBp NEHaemdFVVOR M{LneIlvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> NGnSVW8zOzh3MkO2Oi=>
K1106 M3fPNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX:0JO69VQ>? MYSyOE81QC95MjDo NUTSPIpHTE2VTx?= MXrpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 MWOyN|g2OjN4Nh?=
U2940 NGXMN4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWL1SJlIPCEQvF2= NV\kTmMzOjRxNEivO|IhcA>? MXnEUXNQ NV\iW5V5cW6qaXLpeJMh[2WubDDndo94fGhidHnt[UBl\XCnbnTlcpRtgQ>? MXWyN|g2OjN4Nh?=
FE-PD MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVKwMlA3Oy12IN88US=> MYHJR|UxRTlwNTFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? NHizcVUzOzN5Mk[2PS=>
HEL M4rVPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVmwMlA3Oy12IN88US=> M2GyRWlEPTB;MT61JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= NIPVVJgzOzN5Mk[2PS=>
K-562 NGLRbnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTzdVh7OC5yNkOtOEDPxE1? M3ez[WlEPTB;Mj61JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= NGi5[pMzOzN5Mk[2PS=>
L-82 MkTmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDJd4cxNjB4Mz20JO69VQ>? M3vwdWlEPTB;MD65PEDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= MUOyN|M4OjZ4OR?=
MAC-1 NXPHU45tT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWewMlA3Oy12IN88US=> NEfub5ZKSzVyPUCuOVIh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NEj5emYzOzN5Mk[2PS=>
MAC-2A MkfXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\FdWMxNjB4Mz20JO69VQ>? MnWwTWM2OD1yLk[5JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= M4Dt[FI{Ozd{Nk[5
MAC-2B MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnCcXV[OC5yNkOtOEDPxE1? NF3BfoxKSzVyPUCuOVQh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NF[5RmEzOzN5Mk[2PS=>
MY-LA NYf5W|BoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3XRclAvODZ|LUSg{txO MYfJR|UxRTJwMTFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? MXeyN|M4OjZ4OR?=
NC-NC MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPSNE4xPjNvNDFOwG0> NWe1WVkxUUN3ME2xMlAh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NWnUT2R1OjN|N{K2Olk>
SE-AX NX23NIl2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFX5RnIxNjB4Mz20JO69VQ>? NYjxTpVDUUN3ME2xMlUh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NFjnbXEzOzN5Mk[2PS=>
SR-786 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVj1cFNuOC5yNkOtOEDPxE1? M1TLUGlEPTB;ND62JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= M{LXRVI{Ozd{Nk[5
M-MOK  M4jN[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHQXI11OjViwsXNxsA> NYf1XpN2OjRxNEivO|IhcA>? MmH3SG1UVw>? MV3pcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 Mk\nNlE5PTNzNUe=
HEL MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXPVIR6UUN3ME2zNFUhdk1? MWCxPFM6PDV3NB?=
Ba/F3 JAK2V617F NV\adpg5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlj0TWM2OD1{N{Cgcm0> MVWxPFM6PDV3NB?=

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
+ 展開

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.
細胞試験: [1]
+ 展開
  • 細胞株: EpoBa/F3 JAK2V617F, Ba/F3p210, HEL, and K562
  • 濃度: Dissolved in DMSO, final concentrations ~10 μM
  • 反応時間: 72 hours
  • 実験の流れ: 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.
    (参考用のみ)
動物試験:[1]
+ 展開
  • 動物モデル: C57BL/6 mice injected intravenously with whole bone marrow expressing JAK2V617F
  • 製剤: Dissolved in DMSO, and diluted in saline
  • 投薬量: ~120 mg/kg
  • 投与方法: Oral gavage twice daily (b.i.d.)
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 100 mg/mL (190.59 mM)
Water Insoluble
Ethanol Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
1% DMSO+30% polyethylene glycol+1% Tween 80
混合させたのち直ちに使用することを推奨します。
30 mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 524.68
化学式

C27H36N6O3S

CAS No. 936091-26-8
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01836705 Completed Neoplasm Malignant Sanofi May 2013 Phase 1
NCT01762462 Completed Hepatic Impairment Sanofi December 2012 Phase 1
NCT01763190 Completed Renal Impairment Sanofi November 2012 Phase 1
NCT01692366 Completed Myelofibrosis Sanofi November 2012 Phase 2
NCT01585623 Completed Solid Tumor Sanofi June 2012 Phase 1
NCT01523171 Completed Hematopoietic Neoplasm Sanofi April 2012 Phase 2

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

JAKシグナル伝達経路

JAK Inhibitors with Unique Features

相関JAK製品

Tags: Fedratinib (SAR302503, TG101348)を買う | Fedratinib (SAR302503, TG101348) ic50 | Fedratinib (SAR302503, TG101348)供給者 | Fedratinib (SAR302503, TG101348)を購入する | Fedratinib (SAR302503, TG101348)費用 | Fedratinib (SAR302503, TG101348)生産者 | オーダーFedratinib (SAR302503, TG101348) | Fedratinib (SAR302503, TG101348)化学構造 | Fedratinib (SAR302503, TG101348)分子量 | Fedratinib (SAR302503, TG101348)代理店
×
細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID