Fedratinib (TG101348)

For research use only. Not for use in humans.

目录号:S2736 别名: SAR302503 中文名称:费德拉替尼

Fedratinib (TG101348) Chemical Structure

CAS No. 936091-26-8

Fedratinib (SAR302503, TG101348)是一种选择性JAK2抑制剂,在无细胞试验中IC50为3 nM,作用于JAK2比作用于JAK1和JAK3选择性高35和334倍。Fedratinib也可抑制 FMS-like tyrosine kinase 3 (FLT3)Ret,对应的IC50值分别为15 nM和48 nM。Fedratinib有潜在的抗肿瘤活性。Fedratinib可抑制细胞增殖并促进凋亡。Phase 2。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1812.56 现货
RMB 897.44 现货
RMB 1414.65 现货
RMB 3030.91 现货
RMB 4651.14 现货
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客户使用Selleck生产的Fedratinib (TG101348)发表文献42篇:

产品安全说明书

JAK抑制剂选择性比较

生物活性

产品描述 Fedratinib (SAR302503, TG101348)是一种选择性JAK2抑制剂,在无细胞试验中IC50为3 nM,作用于JAK2比作用于JAK1和JAK3选择性高35和334倍。Fedratinib也可抑制 FMS-like tyrosine kinase 3 (FLT3)Ret,对应的IC50值分别为15 nM和48 nM。Fedratinib有潜在的抗肿瘤活性。Fedratinib可抑制细胞增殖并促进凋亡。Phase 2。
靶点
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
体外研究

TG-101348也显著抑制JAK2 V617F, Flt3和Ret,IC50分别为3 nM, 15 nM和48 nM。TG101348对密切相关的JAK3的IC50高300倍以上,对JAK1和TYK2家族抑制效果不强。TG101348抑制有JAK2V617F突变的人红细胞白血病细胞系,以及一种表达人JAK2V617F(的Ba/F3 JAK2V617F)鼠前B细胞系的增殖,IC50分别是305 nM 和270 nM。G-101348也抑制亲本Ba/F3细胞的增殖至一般水平,IC50约为420 nM。TG101348降低STAT5磷酸化的浓度和抑制细胞增殖所需的浓度一致。TG101348以剂量依赖的方式诱导HEL和JAK2V617F Ba/F3细胞的凋亡。TG101348在浓度高达10 μM时对正常人真皮成纤维细胞没有促凋亡活性。[1] TG101348降低GATA-1的表达,这和erythroid-skewing JAK2V617F+祖细胞分化有关,并且抑制STAT5和GATA S310的磷酸化。[2] TG101348抑制HMC-1.1(KITV560G)细胞的增殖,活性低于HMC-1.2 (KITD816V, KITV560G)细胞,IC50分别为740 nM和407 nM。[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
H1975 MV3BdI9xfG:|aYOgRZN{[Xl? MXuwMlUuOiEQvF2= NYr5VpBGOTJvNEigbC=> MYLEUXNQ NXuxW3M{cW6mdXPld{BieG:ydH;zbZMhcW5iYn;0bEBld3OnLTDhcoQhfGmvZT2g[IVx\W6mZX70JI1idm6nch?= NWroRnR6OjV6NkmyNVA>
H1650 MmTFRZBweHSxc3nzJGF{e2G7 MWmwMlUuOiEQvF2= NEOxWYQyOi12ODDo MV\EUXNQ NVX1S|ZwcW6mdXPld{BieG:ydH;zbZMhcW5iYn;0bEBld3OnLTDhcoQhfGmvZT2g[IVx\W6mZX70JI1idm6nch?= MX[yOVg3QTJzMB?=
H1975 NWXWR2VzTnWwY4Tpc44hSXO|YYm= NHTtNGExNjJ3LUGg{txO NUjkdnltOjRiaB?= NWfkS5B1TE2VTx?= NH\SZnFqdmirYnn0d{BmgHC{ZYPzbY9vKG:oIHHwc5B1d3Orcz3y[YxifGWmIIDyc5RmcW5iQnPsMXhNNCCEY3ytNkwhe3W{dnn2bY4tKFiLQWC= MViyOVg3QTJzMB?=
H1650 NXjFVHJjTnWwY4Tpc44hSXO|YYm= NFrZO3ExNjJ3LUGg{txO NHftcVczPCCq NVH3NYJjTE2VTx?= MV7pcohq[mm2czDlfJBz\XO|aX;uJI9nKGGyb4D0c5Nqey2{ZXzheIVlKHC{b4TlbY4hSmOuLWjMMEBD[2xvMjygd5Vzfmm4aX6sJHhKSVB? NXXje4hZOjV6NkmyNVA>
H1975 NVnZSHlXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\1XVEyKM7:TR?= M{\zdlQ5KGh? NX;NU|gzTE2VTx?= Mnq2d4Vve2m2aYrld{Bk\WyuczD0c{B1cGViY4n0c5RwgGmlaYT5JI9nKGW{bH;0bY5q[g>? NWXsc21EOjV6NkmyNVA>
H1650 MonyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHwNUDPxE1? NUftVFRqPDhiaB?= NWTUT41uTE2VTx?= MYTz[Y5{cXSrenXzJINmdGy|IITvJJRp\SCleYTveI95cWOrdImgc4Yh\XKub4Tpcolj M3;PUVI2QDZ7MkGw
CD4+ T MWHGeY5kfGmxbjDBd5NigQ>? MYKwMlAyNTFizszN NEDmUFU1QCCq Mor4SG1UVw>? NUnybWZIemWmdXPld{B1cGVicHjvd5Bpd3K7bHH0bY9vKGyndnXsd{Bw\iCMQVuyJIFv\CCVVFHUN:Kh MkPzNlU2PzJ3M{W=
Caco-2  M37xcWZ2dmO2aX;uJGF{e2G7 NH\FRWgxNTF{MDFOwG0> MkfoO{BucW5? NWnuUVd6cW6qaXLpeJMhfGirYX3pcoUhfXC2YXvlJJdqfGhiYX6gTWM2OMLib3[gNk4yyqEEtV2= NYjrdHpKOjVyNkO2O|I>
Caco-2  NEiwT2lHfW6ldHnvckBCe3OjeR?= MmLtNVAwPTBxMUCwJO69VQ>? MoSzNkBp M3;sWIRm[3KnYYPld{B1cGViZnz1fEBw\iCdM1jdeIhq[W2rbnWgZYNzd3O|IITo[UBud26xbHH5[ZIhf2m2aDDJR|UxKG:oIE[uOeKh|ryP NUL2e3I1OjVyNkO2O|I>
HEK293 MSR  MnXOSpVv[3Srb36gRZN{[Xl? MnXkNE0yOCEQvF2= MnHJO{BucW5? NWq1TINUcW6qaXLpeJMhcFSKVGKyJJdqfGhiYX6gTWM2OMLib3[gNU4zyqEEtV2= NFvac4YzPTB4M{[3Ni=>
MedB-1 M1Xv[GZ2dmO2aX;uJGF{e2G7 M1T3NlEwOiEQvF2= NEi0WHgzPCCq NYnNWo1q\GWlcnXhd4V{KFOWQWS2JJBpd3OyaH;yfYxifGmxbjDjc45k\W62cnH0bY9vKGSncHXu[IVvfGy7 MVuyOFk4PzZ4OB?=
U2940 NFnUXlhHfW6ldHnvckBCe3OjeR?= MmT4NU8zKM7:TR?= MnfSNlQhcA>? NYDrTlFQ\GWlcnXhd4V{KFOWQWS2JJBpd3OyaH;yfYxifGmxbjDjc45k\W62cnH0bY9vKGSncHXu[IVvfGy7 Mnz0NlQ6Pzd4Nki=
K1106 MnjmSpVv[3Srb36gRZN{[Xl? NGnSNm4yNzJizszN M4ezOFI1KGh? M1rzTIRm[3KnYYPld{BUXEGWNjDwbI9{eGixconsZZRqd25iY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? MWSyOFk4PzZ4OB?=
K562 NV3j[VVJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnROnJyOC1zIN88US=> NX\KeHM1PzJiaB?= MYnpcohq[mm2czDLOVYzKGOnbHygdJJwdGmoZYLheIlwdiCjdDDobYdpKGOxbnPlcpRz[XSrb36= M{nZN|I1Pzd3M{C4
MDA-MB-468  M4fteWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX6zJOK2VQ>? NULMdpdnPDhiaB?= NUjkN3Bp\W6qYX7j[YQhe2mkY3y2JIlv\HWlZXSgcI9{eyCxZjDj[YxtKH[rYXLpcIl1gcLi MViyOFY3OjhzOB?=
MDA-MB-468 NXfuRWtxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzaeJExNTRizszN MU[0PEBp NVvPPVY4emW|dXz0d{B{cWewaX\pZ4FvfCCub4PzJI9nKH[rYXLpcIl1gSClb33wZZJm\CC2bzDSTU1DWEliYXzvcoU> NGnrflAzPDZ4MkixPC=>
L428 NGPU[lFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4Pkb|AuPSEQvF2= NWDjNmo{PDhiaB?= M37HfolvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= Mlf4NlQ3OTB6Mke=
KMH2 MluzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWKwMVUh|ryP MlXTOFghcA>? MYnpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 NIXv[IkzPDZzMEiyOy=>
L1236 Ml62S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoK0NE02KM7:TR?= NWTIR5lvPDhiaB?= NGrSc5NqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 M{HJc|I1PjFyOEK3
SUPHD1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUTETGx{OC13IN88US=> M{fQelQ5KGh? M32xS4lvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= NVO3TVY2OjR4MUC4Nlc>
HDLM2 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;IWVAuPSEQvF2= NF\1TFc1QCCq MonXbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= MXOyOFYyODh{Nx?=
K1106P Mm[3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWOwMVUh|ryP NV\LPWZ2PDhiaB?= NFnJNo1qdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 M1jzTFI1PjFyOEK3
L428 NXXseFZOSXCxcITvd4l{KEG|c3H5 MnzsNE8xNjZ{NT:xMlI2KM7:TR?= Mk\pOFghcA>? MknNbY5lfWOnczD0bIUh[XCxcITvd4l{yqB? MX2yOFYyODh{Nx?=
KMH2 NF7tUZlCeG:ydH;zbZMhSXO|YYm= MYKwM|AvPjJ3L{GuNlUh|ryP MlP0OFghcA>? NH;YPHpqdmS3Y3XzJJRp\SCjcH;weI9{cXQEoB?= MUKyOFYyODh{Nx?=
L1236 Mof0RZBweHSxc3nzJGF{e2G7 NXXOb|BYOC9yLk[yOU8yNjJ3IN88US=> NEnlWGg1QCCq NIrKdWpqdmS3Y3XzJJRp\SCjcH;weI9{cXQEoB?= NILzR2ozPDZzMEiyOy=>
SUPHD1 MXfBdI9xfG:|aYOgRZN{[Xl? M{DZcFAwOC54MkWvNU4zPSEQvF2= MXy0PEBp NX3MeGVucW6mdXPld{B1cGViYYDvdJRwe2m|wrC= M2PPNVI1PjFyOEK3
HDLM2 MXzBdI9xfG:|aYOgRZN{[Xl? NH20cm0xNzBwNkK1M|EvOjVizszN NGi4V5M1QCCq M3;sSIlv\HWlZYOgeIhmKGGyb4D0c5Nqe8Li M3Pid|I1PjFyOEK3
K1106P NWHyXJBESXCxcITvd4l{KEG|c3H5 MWiwM|AvPjJ3L{GuNlUh|ryP M13aWFQ5KGh? M3HNUYlv\HWlZYOgeIhmKGGyb4D0c5Nqe8Li NH:4VngzPDZzMEiyOy=>
L428 MX3GeY5kfGmxbjDBd5NigQ>? Mm\yNE02KM7:TR?= NGnFbo4zPCCq M2nG[olvcGmkaYTzJGpCUzJxU2TBWEB{cWewYXzpcoc> NU\HUXBNOjR4MUC4Nlc>
KMH2 MX\GeY5kfGmxbjDBd5NigQ>? NGXpbHkxNTVizszN M3\2VFI1KGh? MWXpcohq[mm2czDKRWszN1OWQWSgd4lodmGuaX7n NYO5NphGOjR4MUC4Nlc>
L1236 MVvGeY5kfGmxbjDBd5NigQ>? MkjaNE02KM7:TR?= NHfo[XAzPCCq NXjJSnlZcW6qaXLpeJMhUkGNMj;TWGFVKHOrZ37hcIlv\w>? NWX1SFVTOjR4MUC4Nlc>
SUPHD1 NWq5XHp{TnWwY4Tpc44hSXO|YYm= M4rp[FAuPSEQvF2= MmTTNlQhcA>? NWjxTItucW6qaXLpeJMhUkGNMj;TWGFVKHOrZ37hcIlv\w>? MWCyOFYyODh{Nx?=
HDLM2 M1LzN2Z2dmO2aX;uJGF{e2G7 NIjYbIgxNTVizszN NE\VR|UzPCCq M4HpVolvcGmkaYTzJGpCUzJxU2TBWEB{cWewYXzpcoc> MoDrNlQ3OTB6Mke=
K1106P NILlbZhHfW6ldHnvckBCe3OjeR?= MlfBNE02KM7:TR?= NGHoV2IzPCCq MWHpcohq[mm2czDKRWszN1OWQWSgd4lodmGuaX7n NWHzTJdMOjR4MUC4Nlc>
MM.1S  M4jsTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTFvMzFOwG0> NELQV3QzPDV6NEGwNS=>
TpoR JAK2 WT M1GxNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XWV2lEPTB;MT60JEgyNjQkgKOxMlUqKM7:TR?= MUCyOFI2OTd7MB?=
TpoR JAK2 V617F NGrmUXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3:yfGlEPTB;MD64JEgxNjgkgKOwMlkqKM7:TR?= MlLqNlQzPTF5OUC=
TpoR W515L NGfRSppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTBwODCoNE446oDVMT6wLUDPxE1? M1\TfFI1OjVzN{mw
Bcr-abl M3PO[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PITmlEPTB;Mj63JEgzNjMkgKOzMlMqKM7:TR?= MnPDNlQzPTF5OUC=
JAK2 TW MlK5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7UWnhKSzVyPUGuPEApOS534pETNk4{MSEQvF2= MWKyOFI2OTd7MB?=
JAK2 V617F NYL3OmVCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3kOYJoUUN3ME2wMlYhMDBwNvMAl|AvPylizszN NYjtR4J{OjR{NUG3PVA>
MedB-1 M123W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvFOEDPxE1? MXSyOE81QC95MjDo MmC1SG1UVw>? MlLYbY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> NXf2VVF4OjN6NUKzOlY>
K1106 Mm\0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFezNJI1KM7:TR?= NVXsNVZ2OjRxNEivO|IhcA>? MUPEUXNQ NELncZlqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 NV3MbVdxOjN6NUKzOlY>
U2940 NIrZe2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjyVXBxPCEQvF2= NVqySZZ1OjRxNEivO|IhcA>? MnvBSG1UVw>? NFqxS5pqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 NFX1OHQzOzh3MkO2Oi=>
FE-PD NETtUVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYKwMlA3Oy12IN88US=> MnvoTWM2OD17LkWg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 MXKyN|M4OjZ4OR?=
HEL M2SzTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfTdnExNjB4Mz20JO69VQ>? NIC5XnVKSzVyPUGuOUDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= NHj4dGkzOzN5Mk[2PS=>
K-562 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjiNE4xPjNvNDFOwG0> Mm\qTWM2OD1{LkWg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 MXSyN|M4OjZ4OR?=
L-82 NX;UOlZjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHFZXUxNjB4Mz20JO69VQ>? NXq3d4E6UUN3ME2wMlk5KM7:TTygbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> Ml\tNlM{PzJ4Nkm=
MAC-1 NV35R5ZPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\CVXhZOC5yNkOtOEDPxE1? NHWxeVdKSzVyPUCuOVIh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MmfHNlM{PzJ4Nkm=
MAC-2A Ml3CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF2wRmExNjB4Mz20JO69VQ>? MmKyTWM2OD1yLk[5JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= NWm3V3FzOjN|N{K2Olk>
MAC-2B NVTEPXFST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPjNE4xPjNvNDFOwG0> NXKxT5JvUUN3ME2wMlU1KM7:TTygbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MorHNlM{PzJ4Nkm=
MY-LA MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmH2NE4xPjNvNDFOwG0> NVizOXVlUUN3ME2yMlEh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NEfVTVczOzN5Mk[2PS=>
NC-NC NGn3RZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWmwMlA3Oy12IN88US=> NEe0UJRKSzVyPUGuNEDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= MWmyN|M4OjZ4OR?=
SE-AX M1r1Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX6wMlA3Oy12IN88US=> Mo\CTWM2OD1zLkWg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 NEjtSWYzOzN5Mk[2PS=>
SR-786 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDKNE4xPjNvNDFOwG0> MkLmTWM2OD12Lk[g{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 NX;pcoIyOjN|N{K2Olk>
M-MOK  NInCPYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWex[lJDOjViwsXNxsA> NW\4NHlOOjRxNEivO|IhcA>? M4X2XGROW09? MVfpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 MlGxNlE5PTNzNUe=
HEL NIW1fFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzQTWM2OD1|MEWgcm0> MlXmNVg{QTR3NUS=
Ba/F3 JAK2V617F M1vaOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nSXmlEPTB;MkewJI5O NVftWnhROTh|OUS1OVQ>

... 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
体内研究

TG101348有治疗JAK2V617F相关的骨髓增生性疾病(MPD)的潜力。在TG101348处理的动物中血细胞比容和白细胞计数有统计学显著减少,以剂量依赖性减少/消除髓外造血,至少在某些情况下,表现为衰减性骨髓纤维化,具有替代终点,包括减少/消除的JAK2V617F疾病负担,抑制内源性红细胞集落的形成相关,在体内抑制JAK-STAT信号转导。有没有明显的毒性并对T细胞数量无影响。[1] TG101348(120 mg/kg)口服显著抑制体内光伏红系祖细胞分化。[2]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:

[1]

- 合并

无细胞激酶活性测定:

TG101348 的IC 50值使用Invitrogen公司的223激酶试剂盒测定,其中包括JAK2和JAK2V617F,或者Carna Biosciences的所有Janus激酶家族成员试剂盒,包括JAK1和TYK2。ATP浓度设定为激酶的Km值。
细胞实验:

[1]

- 合并
  • Cell lines: EpoBa/F3 JAK2V617F, Ba/F3p210, HEL和K562细胞
  • Concentrations: 溶解在DMSO中至终浓度约10 μM
  • Incubation Time: 72小时
  • Method:

    约2×103细胞接种到微量滴定板的孔中,加入含指定浓度抑制剂的100μLRPMI-1640培养基。TG101348温育72小时,50 μL XTT染料加入到每个孔中并孵育4小时,在CO2培养箱中培养。有色甲臜产物用分光光度法在450nm处测定在650nm处校正。50%的抑制作用(IC50)的浓度用GraphPad Prism 4.0软件确定。所有的实验都重复3次,并且结果和未处理的细胞的生长做比较。EpoBa/F3 JAK2V617F,Ba/F3p210,HEL和K562细胞凋亡是用DMSO和TG101348浓度的增加诱导来确定。


    (Only for Reference)
动物实验:

[1]

- 合并
  • Animal Models: C57BL / 6小鼠静脉注射表达JAK2V617F的全骨髓
  • Dosages: 约120 mg/kg
  • Administration: 口服,每天两次
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 100 mg/mL (190.59 mM)
Water Insoluble
Ethanol Insoluble

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 524.68
化学式

C27H36N6O3S

CAS号 936091-26-8
储存条件 粉状
溶于溶剂
别名 SAR302503

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
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 Unknown status 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
NCT01523171 Completed Drug: SAR302503 Hematopoietic Neoplasm Sanofi April 2012 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID