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 NUjTdpF1SXCxcITvd4l{KEG|c3H5 M37CeVAvPS1{IN88US=> M3L4S|EzNTR6IHi= Ml7HSG1UVw>? M3vtSolv\HWlZYOgZZBweHSxc3nzJIlvKGKxdHig[I9{\S1iYX7kJJRqdWVvIHTldIVv\GWwdDDtZY5v\XJ? M1XEWFI2QDZ7MkGw
H1650 NXrvT3A3SXCxcITvd4l{KEG|c3H5 M4jjb|AvPS1{IN88US=> M4X1flEzNTR6IHi= MlXRSG1UVw>? MXXpcoR2[2W|IHHwc5B1d3OrczDpckBjd3SqIHTvd4UuKGGwZDD0bY1mNSCmZYDlcoRmdnRibXHucoVz MVKyOVg3QTJzMB?=
H1975 NYm2WYVHTnWwY4Tpc44hSXO|YYm= Mn3ONE4zPS1zIN88US=> MkDPNlQhcA>? MV7EUXNQ NYXYS|BIcW6qaXLpeJMh\XiycnXzd4lwdiCxZjDhdI9xfG:|aYOtdoVt[XSnZDDwdo91\WmwIFLjcE1ZVCxiQnPsMVItKHO3co\peolvNCC[SVHQ NEXGfoEzPTh4OUKxNC=>
H1650 MorRSpVv[3Srb36gRZN{[Xl? NGrWZ|MxNjJ3LUGg{txO MmLINlQhcA>? M{PpT2ROW09? Mm[4bY5pcWKrdIOg[ZhxemW|c3nvckBw\iCjcH;weI9{cXNvcnXsZZRm\CCycn;0[YlvKEKlbD3YUEwhSmOuLUKsJJN2en[rdnnuMEBZUUGS NGKxcmozPTh4OUKxNC=>
H1975 NHq0boNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEn6[JYyKM7:TR?= NHryXoY1QCCq MmP0SG1UVw>? NUDycXdWe2Wwc3n0bZpmeyClZXzsd{B1dyC2aHWgZ5l1d3SxeHnjbZR6KG:oIHXycI91cW6rYh?= MoSwNlU5Pjl{MUC=
H1650 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;ZVXIyKM7:TR?= NX7vW5pbPDhiaB?= NY\2bIhtTE2VTx?= NWniVGV7e2Wwc3n0bZpmeyClZXzsd{B1dyC2aHWgZ5l1d3SxeHnjbZR6KG:oIHXycI91cW6rYh?= MXKyOVg3QTJzMB?=
CD4+ T MUTGeY5kfGmxbjDBd5NigQ>? MkPxNE4xOS1zIN88US=> M4nye|Q5KGh? MYPEUXNQ NH7VbHdz\WS3Y3XzJJRp\SCyaH;zdIhwenmuYYTpc44hdGW4ZXzzJI9nKEqDS{KgZY5lKFOWQWSzxsA> NV3JbVZ2OjV3N{K1N|U>
Caco-2  NY\DXYdWTnWwY4Tpc44hSXO|YYm= Ml3hNE0yOjBizszN NU\sTZFmPyCvaX6= M{\NTIlvcGmkaYTzJJRpcWGvaX7lJJVxfGGtZTD3bZRpKGGwIFnDOVDDqG:oIEKuNeKhyrWP MlHVNlUxPjN4N{K=
Caco-2  MUXGeY5kfGmxbjDBd5NigQ>? M37rUFExNzVyL{GwNEDPxE1? NUnkdHlpOiCq MnLz[IVkemWjc3XzJJRp\SCobIX4JI9nKFt|SG30bIlidWmwZTDhZ5Jwe3NidHjlJI1wdm:uYYnldkB4cXSqIFnDOVAhd2ZiNj61xsDPxE1? MYSyOVA3OzZ5Mh?=
HEK293 MSR  NFriSFJHfW6ldHnvckBCe3OjeR?= NWjJ[ZZoOC1zMDFOwG0> NHXkPI84KG2rbh?= NXXrZnNXcW6qaXLpeJMhcFSKVGKyJJdqfGhiYX6gTWM2OMLib3[gNU4zyqEEtV2= NFTjSGUzPTB4M{[3Ni=>
MedB-1 MVnGeY5kfGmxbjDBd5NigQ>? MYGxM|Ih|ryP NX\kO5BVOjRiaB?= M3nVSYRm[3KnYYPld{BUXEGWNjDwbI9{eGixconsZZRqd25iY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? MY[yOFk4PzZ4OB?=
U2940 MXPGeY5kfGmxbjDBd5NigQ>? M{LZNVEwOiEQvF2= NXLj[2FVOjRiaB?= NVLTV|U2\GWlcnXhd4V{KFOWQWS2JJBpd3OyaH;yfYxifGmxbjDjc45k\W62cnH0bY9vKGSncHXu[IVvfGy7 M1HzeVI1QTd5Nk[4
K1106 NHztZZpHfW6ldHnvckBCe3OjeR?= M{PTNlEwOiEQvF2= MVeyOEBp MoTW[IVkemWjc3XzJHNVSVR4IIDoc5NxcG:{eXzheIlwdiClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NXjKRZFTOjR7N{e2Olg>
K562 NUnQWop2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXVUVhROC1zIN88US=> MoDIO|IhcA>? Ml:ybY5pcWKrdIOgT|U3OiClZXzsJJBzd2yrZnXyZZRqd25iYYSgbIlocCClb37j[Y51emG2aX;u NUjkeWhMOjR5N{WzNFg>
MDA-MB-468  NYXEfXJKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnIVHlPOyEEtV2= M4XNe|Q5KGh? NXrmU5FF\W6qYX7j[YQhe2mkY3y2JIlv\HWlZXSgcI9{eyCxZjDj[YxtKH[rYXLpcIl1gcLi NYn0eGdFOjR4NkK4NVg>
MDA-MB-468 Mn3QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFr3Z4MxNTRizszN MoD0OFghcA>? Mo\mdoV{fWy2czDzbYdvcW[rY3HueEBtd3O|IH;mJJZq[WKrbHn0fUBkd22yYYLl[EB1dyCUST3CVGkh[WyxbnW= NX7k[ldtOjR4NkK4NVg>
L428 NWnZUoZiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HGOlAuPSEQvF2= M2TsW|Q5KGh? NGm0WWpqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 MWiyOFYyODh{Nx?=
KMH2 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfpOm0xNTVizszN NG\4T|U1QCCq MUXpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 NWD3UoM2OjR4MUC4Nlc>
L1236 NV3H[ZY{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\GflAuPSEQvF2= M2W4RlQ5KGh? MlzVbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= Mkn2NlQ3OTB6Mke=
SUPHD1 NX7sZoZpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NICxO|QxNTVizszN NXroblhzPDhiaB?= NF24dHNqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 NXnN[2w6OjR4MUC4Nlc>
HDLM2 M3XvT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrUbY91OC13IN88US=> NFXqUpk1QCCq NHnvR5VqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 NG\DbYYzPDZzMEiyOy=>
K1106P MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4jTZVAuPSEQvF2= NFKyZZA1QCCq NW\yT4ttcW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> MkTMNlQ3OTB6Mke=
L428 MWXBdI9xfG:|aYOgRZN{[Xl? M{TNU|AwOC54MkWvNU4zPSEQvF2= NIDGT5k1QCCq MmH5bY5lfWOnczD0bIUh[XCxcITvd4l{yqB? Ml;aNlQ3OTB6Mke=
KMH2 MYHBdI9xfG:|aYOgRZN{[Xl? Mnn6NE8xNjZ{NT:xMlI2KM7:TR?= MnL4OFghcA>? M2rBcolv\HWlZYOgeIhmKGGyb4D0c5Nqe8Li NWrnZY86OjR4MUC4Nlc>
L1236 MYjBdI9xfG:|aYOgRZN{[Xl? MnO1NE8xNjZ{NT:xMlI2KM7:TR?= M1T4WVQ5KGh? Mn3DbY5lfWOnczD0bIUh[XCxcITvd4l{yqB? NFjBe2ozPDZzMEiyOy=>
SUPHD1 MWXBdI9xfG:|aYOgRZN{[Xl? M1foblAwOC54MkWvNU4zPSEQvF2= MVq0PEBp MWnpcoR2[2W|IITo[UBieG:ydH;zbZPDqA>? M17IdFI1PjFyOEK3
HDLM2 NH30W2RCeG:ydH;zbZMhSXO|YYm= MoPhNE8xNjZ{NT:xMlI2KM7:TR?= MkDBOFghcA>? NHjyOGZqdmS3Y3XzJJRp\SCjcH;weI9{cXQEoB?= M{Lt[lI1PjFyOEK3
K1106P NHnuU2ZCeG:ydH;zbZMhSXO|YYm= MlTQNE8xNjZ{NT:xMlI2KM7:TR?= NH3rfGs1QCCq NWHB[WtRcW6mdXPld{B1cGViYYDvdJRwe2m|wrC= MkjTNlQ3OTB6Mke=
L428 NVnQW4pITnWwY4Tpc44hSXO|YYm= M2fDUlAuPSEQvF2= NXLWSId7OjRiaB?= M3XocIlvcGmkaYTzJGpCUzJxU2TBWEB{cWewYXzpcoc> NXTT[mZmOjR4MUC4Nlc>
KMH2 NUTuPWFRTnWwY4Tpc44hSXO|YYm= MVywMVUh|ryP MnXYNlQhcA>? MnPBbY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> M4rNTlI1PjFyOEK3
L1236 MkDkSpVv[3Srb36gRZN{[Xl? Ml\BNE02KM7:TR?= NWLJNWU2OjRiaB?= M1TnWolvcGmkaYTzJGpCUzJxU2TBWEB{cWewYXzpcoc> MVGyOFYyODh{Nx?=
SUPHD1 MV7GeY5kfGmxbjDBd5NigQ>? M4PrU|AuPSEQvF2= NGDxbo0zPCCq MYrpcohq[mm2czDKRWszN1OWQWSgd4lodmGuaX7n M3yxb|I1PjFyOEK3
HDLM2 M3\JemZ2dmO2aX;uJGF{e2G7 MXuwMVUh|ryP NGTMSIgzPCCq MoS4bY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> MYSyOFYyODh{Nx?=
K1106P MVXGeY5kfGmxbjDBd5NigQ>? Mmf2NE02KM7:TR?= M{LKblI1KGh? NFPDcXRqdmirYnn0d{BLSUt{L2PURXQhe2mpbnHsbY5o M1HkcFI1PjFyOEK3
MM.1S  NUjtepdLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;3[2lEPTB;MT2zJO69VQ>? NWTmOoVsOjR3OESxNFE>
TpoR JAK2 WT MnXQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDF[o5KSzVyPUGuOEApOS5|4pETNU42MSEQvF2= NVTvRVBWOjR{NUG3PVA>
TpoR JAK2 V617F NF20eWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mkf1TWM2OD1yLkigLFAvP+LCk{CuPUkh|ryP MXWyOFI2OTd7MB?=
TpoR W515L MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnOzTWM2OD1yLkigLFAvP+LCk{GuNEkh|ryP NFLKZYczPDJ3MUe5NC=>
Bcr-abl M{jzNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4K3dWlEPTB;Mj63JEgzNjMkgKOzMlMqKM7:TR?= NV;KOWVwOjR{NUG3PVA>
JAK2 TW MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M324SmlEPTB;MT64JEgyNjYkgKOyMlMqKM7:TR?= NUXuOoV{OjR{NUG3PVA>
JAK2 V617F NUXVTHo4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHK1WlZKSzVyPUCuOkApOC544pETNE44MSEQvF2= MWSyOFI2OTd7MB?=
MedB-1 NHrPSVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M171OlQh|ryP NGXXe3ozPC92OD:3NkBp M2jjNWROW09? MYTpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 NWXZcGNsOjN6NUKzOlY>
K1106 NIrxVplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvqO2w1KM7:TR?= M2DQT|I1NzR6L{eyJIg> M2TiWGROW09? NIPK[mJqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 MoX3NlM5PTJ|Nk[=
U2940 M{LCNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\2OEDPxE1? NFXlSpgzPC92OD:3NkBp M{LCS2ROW09? NY\uWWU6cW6qaXLpeJMh[2WubDDndo94fGhidHnt[UBl\XCnbnTlcpRtgQ>? NE\RUYczOzh3MkO2Oi=>
FE-PD NHjufpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37C[lAvODZ|LUSg{txO NWjCRmtSUUN3ME25MlUh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NWHxVWF{OjN|N{K2Olk>
HEL MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXSwMlA3Oy12IN88US=> MmnTTWM2OD1zLkWg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 Mo\XNlM{PzJ4Nkm=
K-562 NFnrcGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXyXXIxNjB4Mz20JO69VQ>? MlnXTWM2OD1{LkWg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 Ml3CNlM{PzJ4Nkm=
L-82 M1HrTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLzNE4xPjNvNDFOwG0> NX\CZ4tmUUN3ME2wMlk5KM7:TTygbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> M2faelI{Ozd{Nk[5
MAC-1 MlrYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDkNE4xPjNvNDFOwG0> M4TvcGlEPTB;MD61NkDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= NIfvVZAzOzN5Mk[2PS=>
MAC-2A NHT5bXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjNZXExNjB4Mz20JO69VQ>? NWjxUnlqUUN3ME2wMlY6KM7:TTygbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> M1zpRlI{Ozd{Nk[5
MAC-2B MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUe5TJd5OC5yNkOtOEDPxE1? NWrBSYIzUUN3ME2wMlU1KM7:TTygbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MX6yN|M4OjZ4OR?=
MY-LA Mm\KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYCwMlA3Oy12IN88US=> NWr1Z|FHUUN3ME2yMlEh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 M2T2elI{Ozd{Nk[5
NC-NC MlS4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TGVFAvODZ|LUSg{txO MYfJR|UxRTFwMDFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? MljiNlM{PzJ4Nkm=
SE-AX NET1bmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLLNE4xPjNvNDFOwG0> MW\JR|UxRTFwNTFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? NGfMdHUzOzN5Mk[2PS=>
SR-786 Mmn2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHy3cnAxNjB4Mz20JO69VQ>? M2f6XmlEPTB;ND62JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= M{K4XVI{Ozd{Nk[5
M-MOK  M3j4TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPKNlUhyrWPwrC= NEXMO4gzPC92OD:3NkBp NED5SHBFVVOR M3fIZ4lvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> NV;KUXBnOjF6NUOxOVc>
HEL M3j4PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;4SWF7UUN3ME2zNFUhdk1? MXmxPFM6PDV3NB?=
Ba/F3 JAK2V617F MlHQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkD0TWM2OD1{N{Cgcm0> NXrtRnJSOTh|OUS1OVQ>

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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

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