Fedratinib (SAR302503, TG101348)

Catalog No.S2736

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.

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Fedratinib (SAR302503, TG101348) Chemical Structure

Fedratinib (SAR302503, TG101348) Chemical Structure
Molecular Weight: 524.68

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JAK Inhibitors with Unique Features

Product Information

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  • Research Area
  • Inhibition Profile
  • Combination Therapy
    Combination Therapy

Product Description

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. Phase 2.
Targets JAK2 [1]
(Cell-free assay)
JAK2 (V617F) [1]
(Cell-free assay)
FLT3 [1]
(Cell-free assay)
RET [1]
(Cell-free assay)
IC50 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
H1975M4HNTWFxd3C2b4Ppd{BCe3OjeR?=NFfyTIUxNjVvMjFOwG0>NInJRlMyOi12ODDoMXTEUXNQNYLVUXRucW6mdXPld{BieG:ydH;zbZMhcW5iYn;0bEBld3OnLTDhcoQhfGmvZT2g[IVx\W6mZX70JI1idm6nch?=M1XOVVI2QDZ7MkGw
H1650MYPBdI9xfG:|aYOgRZN{[Xl?NWi5UYVbOC53LUKg{txOM4DJclEzNTR6IHi=NX7aeHNoTE2VTx?=MUDpcoR2[2W|IHHwc5B1d3OrczDpckBjd3SqIHTvd4UuKGGwZDD0bY1mNSCmZYDlcoRmdnRibXHucoVzMnrBNlU5Pjl{MUC=
H1975NGnSeHZHfW6ldHnvckBCe3OjeR?=MkTlNE4zPS1zIN88US=>MUeyOEBpMorTSG1UVw>?M2f3bolvcGmkaYTzJIV5eHKnc4Ppc44hd2ZiYYDvdJRwe2m|LYLlcIF1\WRicILveIVqdiCEY3ytXGwtKEKlbD2yMEB{fXK4aY\pckwhYEmDUB?=MmXLNlU5Pjl{MUC=
H1650NH;mXI9HfW6ldHnvckBCe3OjeR?=M3rxPFAvOjVvMTFOwG0>M2HBOFI1KGh?MYLEUXNQNIHN[HRqdmirYnn0d{BmgHC{ZYPzbY9vKG:oIHHwc5B1d3Orcz3y[YxifGWmIIDyc5RmcW5iQnPsMXhNNCCEY3ytNkwhe3W{dnn2bY4tKFiLQWC=NF\zTIgzPTh4OUKxNC=>
H1975NXrSTWQ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MVuxJO69VQ>?NGTqVZQ1QCCqMUHEUXNQNUXuOFRme2Wwc3n0bZpmeyClZXzsd{B1dyC2aHWgZ5l1d3SxeHnjbZR6KG:oIHXycI91cW6rYh?=NIDUV4ozPTh4OUKxNC=>
H1650MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MmHKNUDPxE1?M3XrVVQ5KGh?M{C2XmROW09?M1;tfpNmdnOrdHn6[ZMh[2WubIOgeI8hfGinIHP5eI91d3irY3n0fUBw\iCncnzveIlvcWJ?NEe1ZoQzPTh4OUKxNC=>
CD4+ TM3zjbGZ2dmO2aX;uJGF{e2G7NHnYdGQxNjBzLUGg{txOMXW0PEBpNHnNTVBFVVORMnHKdoVlfWOnczD0bIUheGixc4Doc5J6dGG2aX;uJIxmfmWuczDv[kBLSUt{IHHu[EBUXEGWM9MgM3G1XlI2PTd{NUO1
Caco-2 MoDESpVv[3Srb36gRZN{[Xl?NIjPfYoxNTF{MDFOwG0>NF\o[GQ4KG2rbh?=NVPlWVdNcW6qaXLpeJMhfGirYX3pcoUhfXC2YXvlJJdqfGhiYX6gTWM2OMLib3[gNk4yyqEEtV2=M1zlfFI2ODZ|Nkey
Caco-2 MlXoSpVv[3Srb36gRZN{[Xl?M4jLUFExNzVyL{GwNEDPxE1?MX2yJIg>NF[2cpZl\WO{ZXHz[ZMhfGinIH\seZghd2ZiW{PIYZRpcWGvaX7lJIFkem:|czD0bIUhdW:wb3zhfYVzKHerdHigTWM2OCCxZjC2MlXDqM7:TR?=MmrENlUxPjN4N{K=
HEK293 MSR Ml;PSpVv[3Srb36gRZN{[Xl?NVjsXXhvOC1zMDFOwG0>NYPvVJVJPyCvaX6=NWS0UmFicW6qaXLpeJMhcFSKVGKyJJdqfGhiYX6gTWM2OMLib3[gNU4zyqEEtV2=NGf4XHYzPTB4M{[3Ni=>
MedB-1NYT0UpF5TnWwY4Tpc44hSXO|YYm=M1T5W|EwOiEQvF2=MXiyOEBpNUjOVJhi\GWlcnXhd4V{KFOWQWS2JJBpd3OyaH;yfYxifGmxbjDjc45k\W62cnH0bY9vKGSncHXu[IVvfGy7NV7HdW86OjR7N{e2Olg>
U2940MV\GeY5kfGmxbjDBd5NigQ>?MoTrNU8zKM7:TR?=NHLQXGMzPCCqNEjGRY9l\WO{ZXHz[ZMhW1SDVE[gdIhwe3Cqb4L5cIF1cW:wIHPvcoNmdnS{YYTpc44h\GWyZX7k[Y51dHl?M2S5VlI1QTd5Nk[4
K1106NXL4OIRXTnWwY4Tpc44hSXO|YYm=NYD1dGJkOS9{IN88US=>MXWyOEBpNIXGe4tl\WO{ZXHz[ZMhW1SDVE[gdIhwe3Cqb4L5cIF1cW:wIHPvcoNmdnS{YYTpc44h\GWyZX7k[Y51dHl?Mn3ZNlQ6Pzd4Nki=
K562NXrUR|FWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MV[wMVEh|ryPM4fsSlczKGh?NEfMN4hqdmirYnn0d{BMPTZ{IHPlcIwheHKxbHnm[ZJifGmxbjDheEBpcWeqIHPvcoNmdnS{YYTpc44>NXT2eWR6OjR5N{WzNFg>
MDA-MB-468 MkP6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M2jHXlMhyrWPMX60PEBpNUiwZo1r\W6qYX7j[YQhe2mkY3y2JIlv\HWlZXSgcI9{eyCxZjDj[YxtKH[rYXLpcIl1gcLiNXLGdm5vOjR4NkK4NVg>
MDA-MB-468NGKwbmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NYfMR|lnOC12IN88US=>Mn;1OFghcA>?M3fFUZJme3WudIOgd4lodmmoaXPhcpQhdG:|czDv[kB3cWGkaXzpeJkh[2:vcHHy[YQhfG9iUlmtRnBKKGGub37lNGDwR4wzPDZ4MkixPC=>
L428M{\OZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7MVqwMVUh|ryPNYLt[3VKPDhiaB?=NXvUfo9wcW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=>MleyNlQ3OTB6Mke=
KMH2MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M3KwZ|AuPSEQvF2=MnzOOFghcA>?MWfpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7NHLPRYIzPDZzMEiyOy=>
L1236M{DnbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M2TDPFAuPSEQvF2=NVHyZlFVPDhiaB?=NW\aR3pjcW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=>M4ryVlI1PjFyOEK3
SUPHD1MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NFLQXVIxNTVizszNNHzrR5Q1QCCqNVfNUHF2cW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=>NFrSfW4zPDZzMEiyOy=>
HDLM2NYPqcldMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MmLwNE02KM7:TR?=MUm0PEBpNWTjfpBIcW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=>NGjuPFUzPDZzMEiyOy=>
K1106PM3jZbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NHj2XHAxNTVizszNNIe1c4o1QCCqMonDbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?=NVK0WWZ3OjR4MUC4Nlc>
L428MYPBdI9xfG:|aYOgRZN{[Xl?M3TFUlAwOC54MkWvNU4zPSEQvF2=NX\aO|NmPDhiaB?=MlT3bY5lfWOnczD0bIUh[XCxcITvd4l{yqB?M4TrWFI1PjFyOEK3
KMH2MmHKRZBweHSxc3nzJGF{e2G7NILi[oYxNzBwNkK1M|EvOjVizszNMmP0OFghcA>?NXrEZYdlcW6mdXPld{B1cGViYYDvdJRwe2m|wrC=M4rQZVI1PjFyOEK3
L1236Mlj2RZBweHSxc3nzJGF{e2G7M4r4elAwOC54MkWvNU4zPSEQvF2=MnXPOFghcA>?MkjJbY5lfWOnczD0bIUh[XCxcITvd4l{yqB?NEHoOXQzPDZzMEiyOy=>
SUPHD1NYnqZZdXSXCxcITvd4l{KEG|c3H5NX\UdmxKOC9yLk[yOU8yNjJ3IN88US=>NFjDNIY1QCCqMUXpcoR2[2W|IITo[UBieG:ydH;zbZPDqA>?NWXWSXJKOjR4MUC4Nlc>
HDLM2MWXBdI9xfG:|aYOgRZN{[Xl?MYmwM|AvPjJ3L{GuNlUh|ryPNXy4O5VIPDhiaB?=NFjTN2lqdmS3Y3XzJJRp\SCjcH;weI9{cXQEoB?=MnniNlQ3OTB6Mke=
K1106PNIP2VpBCeG:ydH;zbZMhSXO|YYm=MlS2NE8xNjZ{NT:xMlI2KM7:TR?=MlzBOFghcA>?MmribY5lfWOnczD0bIUh[XCxcITvd4l{yqB?MUGyOFYyODh{Nx?=
L428MX\GeY5kfGmxbjDBd5NigQ>?M1HJO|AuPSEQvF2=NWm5OGR[OjRiaB?=MUHpcohq[mm2czDKRWszN1OWQWSgd4lodmGuaX7nM2XndlI1PjFyOEK3
KMH2M1TI[2Z2dmO2aX;uJGF{e2G7M3fpPVAuPSEQvF2=M3zOdlI1KGh?M33CZYlvcGmkaYTzJGpCUzJxU2TBWEB{cWewYXzpcoc>M3LjPFI1PjFyOEK3
L1236MYrGeY5kfGmxbjDBd5NigQ>?NEXubGgxNTVizszNMmL0NlQhcA>?MXHpcohq[mm2czDKRWszN1OWQWSgd4lodmGuaX7nMWKyOFYyODh{Nx?=
SUPHD1MUXGeY5kfGmxbjDBd5NigQ>?NX\pUIU5OC13IN88US=>MWOyOEBpMl\CbY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=>NHrtdFUzPDZzMEiyOy=>
HDLM2NIrydnZHfW6ldHnvckBCe3OjeR?=NU\lc5VrOC13IN88US=>NIXw[oEzPCCqNVvhR|d3cW6qaXLpeJMhUkGNMj;TWGFVKHOrZ37hcIlv\w>?MYGyOFYyODh{Nx?=
K1106PMVXGeY5kfGmxbjDBd5NigQ>?MYKwMVUh|ryPMlzqNlQhcA>?NHrmWXBqdmirYnn0d{BLSUt{L2PURXQhe2mpbnHsbY5oMnTpNlQ3OTB6Mke=
MM.1S M4fwNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MmW0TWM2OD1zLUOg{txONGPXTFMzPDV6NEGwNS=>
TpoR JAK2 WTM4nYOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MVrJR|UxRTFwNDCoNU4{6oDVMT61LUDPxE1?MVOyOFI2OTd7MB?=
TpoR JAK2 V617FM{XEVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NVzoS|VnUUN3ME2wMlghMDBwN,MAl|AvQSlizszNNXW0fJhDOjR{NUG3PVA>
TpoR W515LMVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NXXmTWUzUUN3ME2wMlghMDBwN,MAl|EvOClizszNMViyOFI2OTd7MB?=
Bcr-ablMmLzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?Mk\lTWM2OD1{LkegLFIvOuLCk{OuN{kh|ryPNIL6[GEzPDJ3MUe5NC=>
JAK2 TWNYPLZmh2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NVnkOFdnUUN3ME2xMlghMDFwNfMAl|IvOylizszNNVnzXVdOOjR{NUG3PVA>
JAK2 V617FMlX0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MojGTWM2OD1yLk[gLFAvPuLCk{CuO{kh|ryPMl;mNlQzPTF5OUC=
MedB-1M4HJNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M3PnN|Qh|ryPMl:yNlQwPDhxN{KgbC=>MWDEUXNQM3HITolvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk>MlLONlM5PTJ|Nk[=
K1106M4GyO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7NVvl[4J{PCEQvF2=MYqyOE81QC95MjDoNUDWS49qTE2VTx?=MnvObY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=>NGnkc2czOzh3MkO2Oi=>
U2940NH65TW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MXu0JO69VQ>?Mn20NlQwPDhxN{KgbC=>MlvOSG1UVw>?MYPpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5MUKyN|g2OjN4Nh?=
FE-PDNGXzTYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NXHKbog5OC5yNkOtOEDPxE1?MYPJR|UxRTlwNTFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl?NHrGPXkzOzN5Mk[2PS=>
HELM4XRcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NIrXN|ExNjB4Mz20JO69VQ>?MXzJR|UxRTFwNTFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl?NVvwZoJQOjN|N{K2Olk>
K-562Ml7ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NFnBT2MxNjB4Mz20JO69VQ>?NY\KTlJPUUN3ME2yMlUh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5MW[yN|M4OjZ4OR?=
L-82MlzwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MVKwMlA3Oy12IN88US=>NWLtXG9ZUUN3ME2wMlk5KM7:TTygbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=>NUD6bmJFOjN|N{K2Olk>
MAC-1M{PPNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NFfk[nIxNjB4Mz20JO69VQ>?MkWyTWM2OD1yLkWyJO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?=NILkWHEzOzN5Mk[2PS=>
MAC-2AM2WxPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M3rU[FAvODZ|LUSg{txONWjmfVFXUUN3ME2wMlY6KM7:TTygbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=>MUeyN|M4OjZ4OR?=
MAC-2BMV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M1X3RlAvODZ|LUSg{txOMl\rTWM2OD1yLkW0JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?=M3:4VVI{Ozd{Nk[5
MY-LAM3fodGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NXLJTY1OOC5yNkOtOEDPxE1?NYLrWFM2UUN3ME2yMlEh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5M{fFWFI{Ozd{Nk[5
NC-NCMnOzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MnXuNE4xPjNvNDFOwG0>Mkn2TWM2OD1zLkCg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7MnXWNlM{PzJ4Nkm=
SE-AXNY[0fFVsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MWewMlA3Oy12IN88US=>NGX1dG9KSzVyPUGuOUDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm=MXKyN|M4OjZ4OR?=
SR-786MoPqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?Mm\ONE4xPjNvNDFOwG0>NWDQfIxSUUN3ME20MlYh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5MlX6NlM{PzJ4Nkm=
M-MOK M3\zNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MnvrNlUhyrWPwrC=M4DGZVI1NzR6L{eyJIg>NGPTSIpFVVORMWfpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5MkDoNlE5PTNzNUe=
HELMVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M3jzRmlEPTB;M{C1JI5ONUX2VG9POTh|OUS1OVQ>
Ba/F3 JAK2V617FMWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NWDpdJNkUUN3ME2yO|Ahdk1?NFX4cW4yQDN7NEW1OC=>

... Click to View More Cell Line Experimental Data

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]
Features

Protocol(Only for 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 Assay: [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.

Animal Study: [1]

Animal Models C57BL/6 mice injected intravenously with whole bone marrow expressing JAK2V617F
Formulation Dissolved in DMSO, and diluted in saline
Dosages ~120 mg/kg
Administration Oral gavage twice daily (b.i.d.)

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Wernig G, et al. Cancer Cell, 2008, 13(4), 311-320.

[2] Geron I, et al. Cancer Cell, 2008, 13(4), 321-330.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-23)

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

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Chemical Information

Download Fedratinib (SAR302503, TG101348) SDF
Molecular Weight (MW) 524.68
Formula

C27H36N6O3S

CAS No. 936091-26-8
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 100 mg/mL (190.59 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 1% DMSO+30% polyethylene glycol+1% Tween 80 30 mg/mL
* <1 mg/ml means slightly soluble or 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 Name N-tert-butyl-3-(5-methyl-2-(4-(2-(pyrrolidin-1-yl)ethoxy)phenylamino)pyrimidin-4-ylamino)benzenesulfonamide

Customer Product Validation(3)


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Rating
Source Blood 2014 123(20), 3175-84. Fedratinib (SAR302503, TG101348) purchased from Selleck
Method Colony-forming assay
Cell Lines Mutant fetal liver R2 cells
Concentrations 500 nM
Incubation Time
Results To test whether this altered signaling pathway in Rcor-/- erythroid cells contributed to their generation of myeloid colonies, the Jak/Stat pathway was blocked with a specific Jak2 inhibitor, TG101348. TG101348 reduced the number of myeloid colonies formed by mutant cells by 40%.

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Source Cancer Gene Ther 2013 20, 582-9. Fedratinib (SAR302503, TG101348) purchased from Selleck
Method microscope imaging
Cell Lines SCC25 cells
Concentrations 1 nM
Incubation Time 24 h
Results Cells were treated with the respective inhibitors at indicated concentrations for 24 h before infection by VSV-GFP (MOI of 0.5). Viral spread, as indicated by GFP expression,was significantly increased in treated cells compared with cells that did not receive drug treatment

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Source Claude HAAN Université du Luxembour. Fedratinib (SAR302503, TG101348) purchased from Selleck
Method Western blot
Cell Lines HEL cells
Concentrations 0.25-1 μM
Incubation Time 3 h
Results TG101348 treatment resulted in a reduction of STAT5 phosphorylation in a concentration-dependent manner.

Tech Support

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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