Fedratinib (SAR302503, TG101348)

Catalog No.S2736

Fedratinib (SAR302503, TG101348) Chemical Structure

Molecular Weight(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.

Size Price Stock Quantity  
In DMSO USD 220 In stock
USD 110 In stock
USD 170 In stock
USD 370 In stock
USD 570 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

4 Customer Reviews

  • 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.

Purity & Quality Control

Choose Selective JAK Inhibitors

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)
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 Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
H1975 NYT5XGo2SXCxcITvd4l{KEG|c3H5 MUOwMlUuOiEQvF2= NVSxfGgzOTJvNEigbC=> MYLEUXNQ NUPXfGd5cW6mdXPld{BieG:ydH;zbZMhcW5iYn;0bEBld3OnLTDhcoQhfGmvZT2g[IVx\W6mZX70JI1idm6nch?= M2f6[|I2QDZ7MkGw
H1650 NYTxVY4ySXCxcITvd4l{KEG|c3H5 MmC0NE42NTJizszN MXyxNk01QCCq M4ThZmROW09? MoHnbY5lfWOnczDhdI9xfG:|aYOgbY4h[m:2aDDkc5NmNSCjbnSgeIlu\S1iZHXw[Y5l\W62IH3hco5meg>? M3\NblI2QDZ7MkGw
H1975 M{L1emZ2dmO2aX;uJGF{e2G7 Mn3sNE4zPS1zIN88US=> Ml7YNlQhcA>? NF\zW4hFVVOR NWHWTG1ZcW6qaXLpeJMh\XiycnXzd4lwdiCxZjDhdI9xfG:|aYOtdoVt[XSnZDDwdo91\WmwIFLjcE1ZVCxiQnPsMVItKHO3co\peolvNCC[SVHQ MX[yOVg3QTJzMB?=
H1650 NV\yTpZOTnWwY4Tpc44hSXO|YYm= NWrtVGk4OC5{NT2xJO69VQ>? NI\udXIzPCCq MX3EUXNQ NHr2Z5NqdmirYnn0d{BmgHC{ZYPzbY9vKG:oIHHwc5B1d3Orcz3y[YxifGWmIIDyc5RmcW5iQnPsMXhNNCCEY3ytNkwhe3W{dnn2bY4tKFiLQWC= NVPOZWp7OjV6NkmyNVA>
H1975 NULxdVVTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HHelEh|ryP NXL4NotvPDhiaB?= MoS5SG1UVw>? M2C5U5NmdnOrdHn6[ZMh[2WubIOgeI8hfGinIHP5eI91d3irY3n0fUBw\iCncnzveIlvcWJ? M{\O[VI2QDZ7MkGw
H1650 M3;Kb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXmxJO69VQ>? NX[y[o84PDhiaB?= NY\JO|B4TE2VTx?= M2Lnc5NmdnOrdHn6[ZMh[2WubIOgeI8hfGinIHP5eI91d3irY3n0fUBw\iCncnzveIlvcWJ? MXKyOVg3QTJzMB?=
CD4+ T M2rMNWZ2dmO2aX;uJGF{e2G7 MoDQNE4xOS1zIN88US=> MWW0PEBp NI[zVJlFVVOR M4PVSpJm\HWlZYOgeIhmKHCqb4PwbI9zgWyjdHnvckBt\X[nbIOgc4YhUkGNMjDhcoQhW1SDVERCpC=> MUGyOVU4OjV|NR?=
Caco-2  NESxbnhHfW6ldHnvckBCe3OjeR?= NY\ibmk4OC1zMkCg{txO Ml;aO{BucW5? MV;pcohq[mm2czD0bIlidWmwZTD1dJRic2Vid3n0bEBidiCLQ{WwxsBw\iB{LkJCpOK2VQ>? Mn;lNlUxPjN4N{K=
Caco-2  MXfGeY5kfGmxbjDBd5NigQ>? NYf5TI02OTBxNUCvNVAxKM7:TR?= M1;ISFIhcA>? MmfN[IVkemWjc3XzJJRp\SCobIX4JI9nKFt|SG30bIlidWmwZTDhZ5Jwe3NidHjlJI1wdm:uYYnldkB4cXSqIFnDOVAhd2ZiNj61xsDPxE1? M37ncVI2ODZ|Nkey
HEK293 MSR  MlG3SpVv[3Srb36gRZN{[Xl? M3zseVAuOTBizszN M2r2XVchdWmw M3zsOIlvcGmkaYTzJIhVUFSUMjD3bZRpKGGwIFnDOVDDqG:oIEGuNuKhyrWP NEHKXoYzPTB4M{[3Ni=>
MedB-1 MonjSpVv[3Srb36gRZN{[Xl? MUGxM|Ih|ryP Mn;oNlQhcA>? NI\ScIdl\WO{ZXHz[ZMhW1SDVE[gdIhwe3Cqb4L5cIF1cW:wIHPvcoNmdnS{YYTpc44h\GWyZX7k[Y51dHl? NELSW|UzPDl5N{[2PC=>
U2940 M2nnVmZ2dmO2aX;uJGF{e2G7 M{j0Z|EwOiEQvF2= MWmyOEBp MYPk[YNz\WG|ZYOgV3RCXDZicHjvd5Bpd3K7bHH0bY9vKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> NWe3fVdtOjR7N{e2Olg>
K1106 M1;QPGZ2dmO2aX;uJGF{e2G7 NIrLSlMyNzJizszN MmXNNlQhcA>? MXTk[YNz\WG|ZYOgV3RCXDZicHjvd5Bpd3K7bHH0bY9vKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> M{TZZ|I1QTd5Nk[4
K562 NIjzZmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PlcVAuOSEQvF2= MlK5O|IhcA>? MVPpcohq[mm2czDLOVYzKGOnbHygdJJwdGmoZYLheIlwdiCjdDDobYdpKGOxbnPlcpRz[XSrb36= M{TId|I1Pzd3M{C4
MDA-MB-468  NEDINm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmr6N{DDvU1? NH3u[mg1QCCq MlPw[Y5p[W6lZXSgd4lj[2x4IHnu[JVk\WRibH;zd{Bw\iClZXzsJJZq[WKrbHn0feKh MVyyOFY3OjhzOB?=
MDA-MB-468 M1;1NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\ONE01KM7:TR?= MoixOFghcA>? M4CyepJme3WudIOgd4lodmmoaXPhcpQhdG:|czDv[kB3cWGkaXzpeJkh[2:vcHHy[YQhfG9iUlmtRnBKKGGub37l MX[yOFY3OjhzOB?=
L428 NFrBPXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvDNE02KM7:TR?= MmXTOFghcA>? MWDpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 Ml\jNlQ3OTB6Mke=
KMH2 NWnDTm06T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWGwMVUh|ryP MYC0PEBp MVvpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 MkfoNlQ3OTB6Mke=
L1236 NWD2Oo1YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fD[|AuPSEQvF2= NWPPbIFRPDhiaB?= M2LHVolvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= NFTwcWkzPDZzMEiyOy=>
SUPHD1 M1n5[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknRNE02KM7:TR?= M2XRVVQ5KGh? M33IeolvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= MXWyOFYyODh{Nx?=
HDLM2 MkfhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPKNWw2OC13IN88US=> NEHMXJY1QCCq MojlbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= NHfq[WgzPDZzMEiyOy=>
K1106P NV:1fmVrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfxNHkxNTVizszN M3P5eFQ5KGh? NHPVcoFqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 NI\ZW|EzPDZzMEiyOy=>
L428 M360[GFxd3C2b4Ppd{BCe3OjeR?= NWnMUGZbOC9yLk[yOU8yNjJ3IN88US=> NELkbHc1QCCq M{PxPYlv\HWlZYOgeIhmKGGyb4D0c5Nqe8Li M{C3U|I1PjFyOEK3
KMH2 NH7HVnJCeG:ydH;zbZMhSXO|YYm= NX7RNo9JOC9yLk[yOU8yNjJ3IN88US=> NWXnSZk4PDhiaB?= NE\DWJNqdmS3Y3XzJJRp\SCjcH;weI9{cXQEoB?= MYmyOFYyODh{Nx?=
L1236 M3H2OmFxd3C2b4Ppd{BCe3OjeR?= MlTPNE8xNjZ{NT:xMlI2KM7:TR?= NIPJ[GE1QCCq MUTpcoR2[2W|IITo[UBieG:ydH;zbZPDqA>? MmrlNlQ3OTB6Mke=
SUPHD1 MWjBdI9xfG:|aYOgRZN{[Xl? NH72PIoxNzBwNkK1M|EvOjVizszN MYS0PEBp MYPpcoR2[2W|IITo[UBieG:ydH;zbZPDqA>? MkHQNlQ3OTB6Mke=
HDLM2 M3;XdmFxd3C2b4Ppd{BCe3OjeR?= MlnENE8xNjZ{NT:xMlI2KM7:TR?= MUS0PEBp NG\KOZdqdmS3Y3XzJJRp\SCjcH;weI9{cXQEoB?= Mni4NlQ3OTB6Mke=
K1106P NYfYfZRbSXCxcITvd4l{KEG|c3H5 M4WwWlAwOC54MkWvNU4zPSEQvF2= M{joWlQ5KGh? MlTObY5lfWOnczD0bIUh[XCxcITvd4l{yqB? MlrENlQ3OTB6Mke=
L428 M3;BW2Z2dmO2aX;uJGF{e2G7 NY[2UIZpOC13IN88US=> NHPsXJczPCCq NEXiXm9qdmirYnn0d{BLSUt{L2PURXQhe2mpbnHsbY5o M370UlI1PjFyOEK3
KMH2 M3P1b2Z2dmO2aX;uJGF{e2G7 MnPRNE02KM7:TR?= M{LkRVI1KGh? MkDIbY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> NEjzTZEzPDZzMEiyOy=>
L1236 NUnsTGwxTnWwY4Tpc44hSXO|YYm= NFu1XHcxNTVizszN NHK5SYszPCCq MkDwbY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> NHHVToczPDZzMEiyOy=>
SUPHD1 MXfGeY5kfGmxbjDBd5NigQ>? MoHnNE02KM7:TR?= MVOyOEBp MnfSbY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> MVOyOFYyODh{Nx?=
HDLM2 NYjQOWRjTnWwY4Tpc44hSXO|YYm= MUGwMVUh|ryP M{K1PFI1KGh? MVfpcohq[mm2czDKRWszN1OWQWSgd4lodmGuaX7n NF\O[5ozPDZzMEiyOy=>
K1106P Mo\ySpVv[3Srb36gRZN{[Xl? Mlq1NE02KM7:TR?= NIiyWpkzPCCq NFXwOWtqdmirYnn0d{BLSUt{L2PURXQhe2mpbnHsbY5o Mn3oNlQ3OTB6Mke=
MM.1S  NXTr[I5QT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2WyXWlEPTB;MT2zJO69VQ>? NEnDU|EzPDV6NEGwNS=>
TpoR JAK2 WT NFv4TYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jnOmlEPTB;MT60JEgyNjQkgKOxMlUqKM7:TR?= NGLaUG4zPDJ3MUe5NC=>
TpoR JAK2 V617F NIDITGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1PHWmlEPTB;MD64JEgxNjgkgKOwMlkqKM7:TR?= MViyOFI2OTd7MB?=
TpoR W515L NG[1PVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnrTWM2OD1yLkigLFAvP+LCk{GuNEkh|ryP MXKyOFI2OTd7MB?=
Bcr-abl NI\ifo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTJwNzCoNk4z6oDVMz6zLUDPxE1? NV\QdWU2OjR{NUG3PVA>
JAK2 TW MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\QcWVyUUN3ME2xMlghMDFwNfMAl|IvOylizszN NGPt[VgzPDJ3MUe5NC=>
JAK2 V617F MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfpV2VKSzVyPUCuOkApOC544pETNE44MSEQvF2= NFvy[3IzPDJ3MUe5NC=>
MedB-1 M2W3UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFq4dpI1KM7:TR?= NGX5NYozPC92OD:3NkBp MknuSG1UVw>? M3XiPIlvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> MoH5NlM5PTJ|Nk[=
K1106 M33VTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYC0JO69VQ>? MnrGNlQwPDhxN{KgbC=> MnHWSG1UVw>? M2r2R4lvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> NXq5XnJmOjN6NUKzOlY>
U2940 NV[yPG1PT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DkSVQh|ryP NX;JSopWOjRxNEivO|IhcA>? NYPhOmtOTE2VTx?= M2fjV4lvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> M3XCO|I{QDV{M{[2
FE-PD NVfJZodrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXvNE4xPjNvNDFOwG0> NVT1SJR[UUN3ME25MlUh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NUHyZoIzOjN|N{K2Olk>
HEL NGDvUXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTUfGIxNjB4Mz20JO69VQ>? M2D5eGlEPTB;MT61JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= NXntTXZvOjN|N{K2Olk>
K-562 NF3UeWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoSyNE4xPjNvNDFOwG0> MV;JR|UxRTJwNTFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? MUKyN|M4OjZ4OR?=
L-82 NGHjU4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfyeVIxNjB4Mz20JO69VQ>? MnnsTWM2OD1yLkm4JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= NV3KWWpbOjN|N{K2Olk>
MAC-1 M13le2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHKNE4xPjNvNDFOwG0> NUHhelg1UUN3ME2wMlUzKM7:TTygbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NHnqXlIzOzN5Mk[2PS=>
MAC-2A M3fNTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILYfYQxNjB4Mz20JO69VQ>? M4P4VWlEPTB;MD62PUDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= NGTPTI8zOzN5Mk[2PS=>
MAC-2B NV\tNWFET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zIXFAvODZ|LUSg{txO MVTJR|UxRTBwNUSg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 NF\XUYQzOzN5Mk[2PS=>
MY-LA NWm1O2NwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XQU|AvODZ|LUSg{txO MWHJR|UxRTJwMTFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? NUTCNopSOjN|N{K2Olk>
NC-NC M3\0fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWCwMlA3Oy12IN88US=> NUDSXpV2UUN3ME2xMlAh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NUfIW49qOjN|N{K2Olk>
SE-AX MoDnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUG4fIhMOC5yNkOtOEDPxE1? M1\veGlEPTB;MT61JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= MYGyN|M4OjZ4OR?=
SR-786 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rJWFAvODZ|LUSg{txO MkC1TWM2OD12Lk[g{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 M2jCUFI{Ozd{Nk[5
M-MOK  MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvVNlUhyrWPwrC= M{i0UFI1NzR6L{eyJIg> MkLFSG1UVw>? NYPjOIJ6cW6qaXLpeJMh[2WubDDndo94fGhidHnt[UBl\XCnbnTlcpRtgQ>? MoXXNlE5PTNzNUe=
HEL MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PNc2lEPTB;M{C1JI5O MX2xPFM6PDV3NB?=
Ba/F3 JAK2V617F NIi2UohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mli1TWM2OD1{N{Cgcm0> MnftNVg{QTR3NUS=

... 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]

Protocol

Kinase Assay:[1]
+ Expand

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 Research:[1]
+ Expand
  • 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.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • 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.)
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (190.59 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order:
1% DMSO+30% polyethylene glycol+1% Tween 80
For best results, use promptly after mixing.
30 mg/mL

* 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 Information

Molecular Weight 524.68
Formula

C27H36N6O3S

CAS No. 936091-26-8
Storage powder
in solvent
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • 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):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

JAK Signaling Pathway Map

JAK Inhibitors with Unique Features

Related JAK Products

Tags: buy Fedratinib (SAR302503, TG101348) | Fedratinib (SAR302503, TG101348) supplier | purchase Fedratinib (SAR302503, TG101348) | Fedratinib (SAR302503, TG101348) cost | Fedratinib (SAR302503, TG101348) manufacturer | order Fedratinib (SAR302503, TG101348) | Fedratinib (SAR302503, TG101348) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID