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 NX3Seml{SXCxcITvd4l{KEG|c3H5 M{[ybVAvPS1{IN88US=> M4DtW|EzNTR6IHi= MX\EUXNQ M37nR4lv\HWlZYOgZZBweHSxc3nzJIlvKGKxdHig[I9{\S1iYX7kJJRqdWVvIHTldIVv\GWwdDDtZY5v\XJ? NGPzcXgzPTh4OUKxNC=>
H1650 NEH0OWlCeG:ydH;zbZMhSXO|YYm= NFPsNZAxNjVvMjFOwG0> MVmxNk01QCCq Mk\JSG1UVw>? MlHybY5lfWOnczDhdI9xfG:|aYOgbY4h[m:2aDDkc5NmNSCjbnSgeIlu\S1iZHXw[Y5l\W62IH3hco5meg>? NYDybJM1OjV6NkmyNVA>
H1975 NGfENldHfW6ldHnvckBCe3OjeR?= Mn7aNE4zPS1zIN88US=> Mn70NlQhcA>? NIr1dJpFVVOR NFfBR3ZqdmirYnn0d{BmgHC{ZYPzbY9vKG:oIHHwc5B1d3Orcz3y[YxifGWmIIDyc5RmcW5iQnPsMXhNNCCEY3ytNkwhe3W{dnn2bY4tKFiLQWC= M3K2NFI2QDZ7MkGw
H1650 MXXGeY5kfGmxbjDBd5NigQ>? MWWwMlI2NTFizszN MnTkNlQhcA>? NVjZRZM2TE2VTx?= Mke0bY5pcWKrdIOg[ZhxemW|c3nvckBw\iCjcH;weI9{cXNvcnXsZZRm\CCycn;0[YlvKEKlbD3YUEwhSmOuLUKsJJN2en[rdnnuMEBZUUGS NV;1bIxpOjV6NkmyNVA>
H1975 NWD4Oph1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmG1NUDPxE1? NF:yeJg1QCCq MoHMSG1UVw>? Ml\Dd4Vve2m2aYrld{Bk\WyuczD0c{B1cGViY4n0c5RwgGmlaYT5JI9nKGW{bH;0bY5q[g>? NYThSG5vOjV6NkmyNVA>
H1650 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzPd5NLOSEQvF2= MVy0PEBp M{PMXGROW09? MojJd4Vve2m2aYrld{Bk\WyuczD0c{B1cGViY4n0c5RwgGmlaYT5JI9nKGW{bH;0bY5q[g>? MX2yOVg3QTJzMB?=
CD4+ T NXra[HI6TnWwY4Tpc44hSXO|YYm= NUX6SWJbOC5yMT2xJO69VQ>? Mk\1OFghcA>? NGrOd4lFVVOR MlvvdoVlfWOnczD0bIUheGixc4Doc5J6dGG2aX;uJIxmfmWuczDv[kBLSUt{IHHu[EBUXEGWM9Mg NFPVVYczPTV5MkWzOS=>
Caco-2  Ml;0SpVv[3Srb36gRZN{[Xl? MUOwMVEzOCEQvF2= MljUO{BucW5? MmTmbY5pcWKrdIOgeIhq[W2rbnWgeZB1[WunIIfpeIgh[W5iSVO1NOKhd2ZiMj6xxsDDvU1? NXe5fZdZOjVyNkO2O|I>
Caco-2  M3jGOmZ2dmO2aX;uJGF{e2G7 NV2yN5puOTBxNUCvNVAxKM7:TR?= NX7YWot{OiCq MUPk[YNz\WG|ZYOgeIhmKG[udYigc4YhYzOKXYTobYFucW6nIHHjdo9{eyC2aHWgcY9vd2yjeXXyJJdqfGhiSVO1NEBw\iB4LkZCpO69VQ>? M3\6U|I2ODZ|Nkey
HEK293 MSR  M2e5[WZ2dmO2aX;uJGF{e2G7 MlLpNE0yOCEQvF2= Mmj1O{BucW5? MnHObY5pcWKrdIOgbHRJXFJ{IIfpeIgh[W5iSVO1NOKhd2ZiMT6yxsDDvU1? M1LIdFI2ODZ|Nkey
MedB-1 Moq1SpVv[3Srb36gRZN{[Xl? NHzuemEyNzJizszN NVPDSZFDOjRiaB?= MWXk[YNz\WG|ZYOgV3RCXDZicHjvd5Bpd3K7bHH0bY9vKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> M{TsOVI1QTd5Nk[4
U2940 M3;tWWZ2dmO2aX;uJGF{e2G7 NYjpR3I5OS9{IN88US=> MUSyOEBp NIDwTVRl\WO{ZXHz[ZMhW1SDVE[gdIhwe3Cqb4L5cIF1cW:wIHPvcoNmdnS{YYTpc44h\GWyZX7k[Y51dHl? NEXkOnIzPDl5N{[2PC=>
K1106 NInKWodHfW6ldHnvckBCe3OjeR?= MkKzNU8zKM7:TR?= MYOyOEBp M{XFSYRm[3KnYYPld{BUXEGWNjDwbI9{eGixconsZZRqd25iY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? NVvyTlYyOjR7N{e2Olg>
K562 MmjoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mne0NE0yKM7:TR?= MU[3NkBp MmfibY5pcWKrdIOgT|U3OiClZXzsJJBzd2yrZnXyZZRqd25iYYSgbIlocCClb37j[Y51emG2aX;u NWPN[2pROjR5N{WzNFg>
MDA-MB-468  M1XkSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFX3OmE{KML3TR?= NXfldI1kPDhiaB?= M3vhT4VvcGGwY3XkJJNq[mOuNjDpcoR2[2WmIHzvd5Mhd2ZiY3XscEB3cWGkaXzpeJnDqA>? MkTsNlQ3PjJ6MUi=
MDA-MB-468 MkHXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF7iVGMxNTRizszN M2LLdFQ5KGh? M2nUOJJme3WudIOgd4lodmmoaXPhcpQhdG:|czDv[kB3cWGkaXzpeJkh[2:vcHHy[YQhfG9iUlmtRnBKKGGub37l MYmyOFY3OjhzOB?=
L428 NV3n[HZkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1fEbFAuPSEQvF2= MU[0PEBp NUXvSpFicW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> M2LEWFI1PjFyOEK3
KMH2 M4S0UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlW0NE02KM7:TR?= M2HOTVQ5KGh? MnPMbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= MkCyNlQ3OTB6Mke=
L1236 MnHFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfiNXExNTVizszN NYPGRpNbPDhiaB?= MWPpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 NW\4enZkOjR4MUC4Nlc>
SUPHD1 NGnjb2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEm3bYoxNTVizszN NFWwUlc1QCCq MV3pcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 M4roWlI1PjFyOEK3
HDLM2 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILEZowxNTVizszN Mn;JOFghcA>? MVHpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 NWXYcZpTOjR4MUC4Nlc>
K1106P NWXDToJOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUTlR5Q1OC13IN88US=> M{\oSlQ5KGh? MV\pcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 NUfK[pNNOjR4MUC4Nlc>
L428 MnHwRZBweHSxc3nzJGF{e2G7 MlLJNE8xNjZ{NT:xMlI2KM7:TR?= MW[0PEBp MVvpcoR2[2W|IITo[UBieG:ydH;zbZPDqA>? MXSyOFYyODh{Nx?=
KMH2 NULafZI4SXCxcITvd4l{KEG|c3H5 MkP1NE8xNjZ{NT:xMlI2KM7:TR?= MV20PEBp MUDpcoR2[2W|IITo[UBieG:ydH;zbZPDqA>? NV3IRZhGOjR4MUC4Nlc>
L1236 M3LUb2Fxd3C2b4Ppd{BCe3OjeR?= MV6wM|AvPjJ3L{GuNlUh|ryP MmPrOFghcA>? NHXNeVhqdmS3Y3XzJJRp\SCjcH;weI9{cXQEoB?= M4fxS|I1PjFyOEK3
SUPHD1 MWPBdI9xfG:|aYOgRZN{[Xl? MUWwM|AvPjJ3L{GuNlUh|ryP Mn;mOFghcA>? NEj4VZJqdmS3Y3XzJJRp\SCjcH;weI9{cXQEoB?= NX25[GdWOjR4MUC4Nlc>
HDLM2 Ml\kRZBweHSxc3nzJGF{e2G7 NHzvTWoxNzBwNkK1M|EvOjVizszN M1TwPVQ5KGh? M4PNWolv\HWlZYOgeIhmKGGyb4D0c5Nqe8Li MoG3NlQ3OTB6Mke=
K1106P M1;Mc2Fxd3C2b4Ppd{BCe3OjeR?= NX;UO3hCOC9yLk[yOU8yNjJ3IN88US=> NXfqTItkPDhiaB?= M2LMUIlv\HWlZYOgeIhmKGGyb4D0c5Nqe8Li MYmyOFYyODh{Nx?=
L428 NYrs[XVnTnWwY4Tpc44hSXO|YYm= MkLUNE02KM7:TR?= NIjG[|EzPCCq NHHOUZdqdmirYnn0d{BLSUt{L2PURXQhe2mpbnHsbY5o NIfL[24zPDZzMEiyOy=>
KMH2 NXzHUmJCTnWwY4Tpc44hSXO|YYm= NX31UphpOC13IN88US=> MXuyOEBp MojnbY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> MoO3NlQ3OTB6Mke=
L1236 M2TrOWZ2dmO2aX;uJGF{e2G7 NFi4foExNTVizszN Mom4NlQhcA>? MlXlbY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> MoHrNlQ3OTB6Mke=
SUPHD1 MmrxSpVv[3Srb36gRZN{[Xl? NIixPGgxNTVizszN NVrE[pl3OjRiaB?= MmHnbY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> MoWyNlQ3OTB6Mke=
HDLM2 MmPsSpVv[3Srb36gRZN{[Xl? Ml;iNE02KM7:TR?= NECzSXAzPCCq M{nRXYlvcGmkaYTzJGpCUzJxU2TBWEB{cWewYXzpcoc> M{\VcVI1PjFyOEK3
K1106P MUjGeY5kfGmxbjDBd5NigQ>? MXewMVUh|ryP MUiyOEBp MorMbY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> NHiwcWczPDZzMEiyOy=>
MM.1S  NGDXdnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF31TmlKSzVyPUGtN{DPxE1? MU[yOFU5PDFyMR?=
TpoR JAK2 WT NF7NcYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLpfWxpUUN3ME2xMlQhMDFwM,MAl|EvPSlizszN NVvx[|l4OjR{NUG3PVA>
TpoR JAK2 V617F NGTNfHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvpNXJ5UUN3ME2wMlghMDBwN,MAl|AvQSlizszN NXT1R5hEOjR{NUG3PVA>
TpoR W515L MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTBwODCoNE446oDVMT6wLUDPxE1? MkjXNlQzPTF5OUC=
Bcr-abl M1rOe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrsNHpWUUN3ME2yMlchMDJwMvMAl|MvOylizszN M2nBblI1OjVzN{mw
JAK2 TW MkP6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU[wUJFPUUN3ME2xMlghMDFwNfMAl|IvOylizszN M2rxblI1OjVzN{mw
JAK2 V617F MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTBwNjCoNE436oDVMD63LUDPxE1? NEXvZWIzPDJ3MUe5NC=>
MedB-1 NH3ESpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2r6dVQh|ryP NGDGVmIzPC92OD:3NkBp M1SweGROW09? MWDpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 NF7QPGMzOzh3MkO2Oi=>
K1106 NX33NGNKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\q[oo1KM7:TR?= MlPLNlQwPDhxN{KgbC=> NYX4T282TE2VTx?= M33ZNolvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> M1H0SFI{QDV{M{[2
U2940 MkDRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV20JO69VQ>? M4jVd|I1NzR6L{eyJIg> Mo\6SG1UVw>? Ml7ubY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> NWHhTHdVOjN6NUKzOlY>
FE-PD MlvSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{frSVAvODZ|LUSg{txO MYnJR|UxRTlwNTFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? MVuyN|M4OjZ4OR?=
HEL NYjI[VlzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHkNE4xPjNvNDFOwG0> NGftbFdKSzVyPUGuOUDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= MXyyN|M4OjZ4OR?=
K-562 NVnVW4JVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIL5W3kxNjB4Mz20JO69VQ>? NEi1UZFKSzVyPUKuOUDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= MUKyN|M4OjZ4OR?=
L-82 NWrlSFh6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzjVVgxNjB4Mz20JO69VQ>? M3vTUmlEPTB;MD65PEDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= MkHnNlM{PzJ4Nkm=
MAC-1 NELpO2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TYZlAvODZ|LUSg{txO MlPoTWM2OD1yLkWyJO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= NIrMfFczOzN5Mk[2PS=>
MAC-2A MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXYNE4xPjNvNDFOwG0> NXfQWoN2UUN3ME2wMlY6KM7:TTygbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> Mn3jNlM{PzJ4Nkm=
MAC-2B NXTOVYV1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13ZXFAvODZ|LUSg{txO NYLo[HRpUUN3ME2wMlU1KM7:TTygbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MkjhNlM{PzJ4Nkm=
MY-LA NHu3b5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDpN4oxNjB4Mz20JO69VQ>? NHX0Z5pKSzVyPUKuNUDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= MVqyN|M4OjZ4OR?=
NC-NC M1;JS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrTWFc1OC5yNkOtOEDPxE1? M3jTc2lEPTB;MT6wJO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= M2r3PVI{Ozd{Nk[5
SE-AX MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXL0XoF4OC5yNkOtOEDPxE1? M4LTdWlEPTB;MT61JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= M4XNb|I{Ozd{Nk[5
SR-786 M{flPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nJb|AvODZ|LUSg{txO MW\JR|UxRTRwNjFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? MlLJNlM{PzJ4Nkm=
M-MOK  MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7acVEzPSEEtV5CpC=> MX[yOE81QC95MjDo M3y2e2ROW09? Ml34bY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> NFXwTGczOTh3M{G1Oy=>
HEL M1TDWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PaWGlEPTB;M{C1JI5O NW[wdWVFOTh|OUS1OVQ>
Ba/F3 JAK2V617F Mn20S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHzTWM2OD1{N{Cgcm0> NEXZUoYyQDN7NEW1OC=>

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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
NCT03755518 Recruiting Primary Myelofibrosis|Thrombocytosis Celgene|Impact Biomedicines Inc. a wholly owned subsidiary of Celgene Corporation February 28 2019 Phase 3
NCT03755518 Recruiting Primary Myelofibrosis|Thrombocytosis Celgene|Impact Biomedicines Inc. a wholly owned subsidiary of Celgene Corporation February 28 2019 Phase 3
NCT01836705 Completed Neoplasm Malignant Sanofi May 2013 Phase 1
NCT01836705 Completed Neoplasm Malignant Sanofi May 2013 Phase 1
NCT01762462 Completed Hepatic Impairment Sanofi December 2012 Phase 1
NCT01762462 Completed Hepatic Impairment Sanofi December 2012 Phase 1

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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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID