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.

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In DMSO USD 220 In stock
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USD 370 In stock
USD 570 In stock

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3 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.

    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

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 NUjCO|NrSXCxcITvd4l{KEG|c3H5 NVHYRolnOC53LUKg{txO NGTZcXMyOi12ODDo M3;Hb2ROW09? M1O0d4lv\HWlZYOgZZBweHSxc3nzJIlvKGKxdHig[I9{\S1iYX7kJJRqdWVvIHTldIVv\GWwdDDtZY5v\XJ? MnzXNlU5Pjl{MUC=
H1650 M4fXfWFxd3C2b4Ppd{BCe3OjeR?= MYewMlUuOiEQvF2= Mnv5NVIuPDhiaB?= NHrUOnFFVVOR MoK1bY5lfWOnczDhdI9xfG:|aYOgbY4h[m:2aDDkc5NmNSCjbnSgeIlu\S1iZHXw[Y5l\W62IH3hco5meg>? NH7SU5EzPTh4OUKxNC=>
H1975 NVXPT486TnWwY4Tpc44hSXO|YYm= MlrINE4zPS1zIN88US=> MX6yOEBp MmPBSG1UVw>? NYTaXG1{cW6qaXLpeJMh\XiycnXzd4lwdiCxZjDhdI9xfG:|aYOtdoVt[XSnZDDwdo91\WmwIFLjcE1ZVCxiQnPsMVItKHO3co\peolvNCC[SVHQ M2rEdVI2QDZ7MkGw
H1650 M3XQbmZ2dmO2aX;uJGF{e2G7 M4rie|AvOjVvMTFOwG0> M3;SSFI1KGh? MV3EUXNQ NVXqTHo5cW6qaXLpeJMh\XiycnXzd4lwdiCxZjDhdI9xfG:|aYOtdoVt[XSnZDDwdo91\WmwIFLjcE1ZVCxiQnPsMVItKHO3co\peolvNCC[SVHQ MonXNlU5Pjl{MUC=
H1975 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY[xJO69VQ>? NVrtZmp[PDhiaB?= NXL0bYhETE2VTx?= M1fj[JNmdnOrdHn6[ZMh[2WubIOgeI8hfGinIHP5eI91d3irY3n0fUBw\iCncnzveIlvcWJ? MX6yOVg3QTJzMB?=
H1650 M2XpPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\o[VEh|ryP NFf2S4g1QCCq MWrEUXNQ NIXMVIx{\W6|aYTpfoV{KGOnbHzzJJRwKHSqZTDjfZRwfG:6aXPpeJkhd2ZiZYLsc5Rqdmmk NUjPTFU6OjV6NkmyNVA>
CD4+ T NIfuToJHfW6ldHnvckBCe3OjeR?= MX[wMlAyNTFizszN NWTpUoZbPDhiaB?= NUXYTJdOTE2VTx?= M37aVpJm\HWlZYOgeIhmKHCqb4PwbI9zgWyjdHnvckBt\X[nbIOgc4YhUkGNMjDhcoQhW1SDVERCpC=> NWf5UJdLOjV3N{K1N|U>
Caco-2  NX;kdWV{TnWwY4Tpc44hSXO|YYm= M4D3[lAuOTJyIN88US=> NYHIcGVLPyCvaX6= MYHpcohq[mm2czD0bIlidWmwZTD1dJRic2Vid3n0bEBidiCLQ{WwxsBw\iB{LkJCpOK2VQ>? MlzVNlUxPjN4N{K=
Caco-2  M33vdmZ2dmO2aX;uJGF{e2G7 M{iwZ|ExNzVyL{GwNEDPxE1? MkTLNkBp NVjEUGY1\GWlcnXhd4V{KHSqZTDmcJV5KG:oIGuzTH11cGmjbXnu[UBi[3Kxc4OgeIhmKG2xbn;sZZlmeiC5aYToJGlEPTBib3[gOk42yqEQvF2= MUKyOVA3OzZ5Mh?=
HEK293 MSR  M4LScGZ2dmO2aX;uJGF{e2G7 NVvQcmxyOC1zMDFOwG0> NHfZc3M4KG2rbh?= Ml3VbY5pcWKrdIOgbHRJXFJ{IIfpeIgh[W5iSVO1NOKhd2ZiMT6yxsDDvU1? MlPGNlUxPjN4N{K=
MedB-1 NGjsO|hHfW6ldHnvckBCe3OjeR?= M2XkcFEwOiEQvF2= MkDBNlQhcA>? NFvRdIRl\WO{ZXHz[ZMhW1SDVE[gdIhwe3Cqb4L5cIF1cW:wIHPvcoNmdnS{YYTpc44h\GWyZX7k[Y51dHl? NFTMNZQzPDl5N{[2PC=>
U2940 NF3YO|hHfW6ldHnvckBCe3OjeR?= NVrOO3hkOS9{IN88US=> NXHSOGx4OjRiaB?= MmnQ[IVkemWjc3XzJHNVSVR4IIDoc5NxcG:{eXzheIlwdiClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 M4D2Z|I1QTd5Nk[4
K1106 NY\WTYhMTnWwY4Tpc44hSXO|YYm= NG\XT5IyNzJizszN NFvYSJYzPCCq MXTk[YNz\WG|ZYOgV3RCXDZicHjvd5Bpd3K7bHH0bY9vKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> NFLuRYIzPDl5N{[2PC=>
K562 MlHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nSeFAuOSEQvF2= M3W0S|czKGh? M1jYe4lvcGmkaYTzJGs2PjJiY3XscEBxem:uaX\ldoF1cW:wIHH0JIhq\2hiY3;uZ4VvfHKjdHnvci=> MXSyOFc4PTNyOB?=
MDA-MB-468  MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnpTIg3OyEEtV2= NFK3bos1QCCq NX34PJBT\W6qYX7j[YQhe2mkY3y2JIlv\HWlZXSgcI9{eyCxZjDj[YxtKH[rYXLpcIl1gcLi MoPyNlQ3PjJ6MUi=
MDA-MB-468 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7IVncxNTRizszN NWjyfYZlPDhiaB?= MUXy[ZN2dHS|IIPp[45q\mmlYX70JIxwe3Nib3[geoli[mmuaYT5JINwdXCjcnXkJJRwKFKLLVLQTUBidG:wZR?= MonTNlQ3PjJ6MUi=
L428 NGPFcWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2r6dlAuPSEQvF2= NEnVVpA1QCCq M330VolvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= M3r5RVI1PjFyOEK3
KMH2 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{mwcVAuPSEQvF2= M1L1Z|Q5KGh? M3TxXYlvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= MVmyOFYyODh{Nx?=
L1236 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWmwMVUh|ryP NXv2dVVEPDhiaB?= MlLtbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= NIW1d4czPDZzMEiyOy=>
SUPHD1 M3LnZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M372fFAuPSEQvF2= NFy5W5M1QCCq MV3pcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 M1nST|I1PjFyOEK3
HDLM2 NYPUPIRGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYWwMVUh|ryP MnXiOFghcA>? MofNbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= NFXsZnYzPDZzMEiyOy=>
K1106P MmH1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3i0UVAuPSEQvF2= M3zkNFQ5KGh? M1jUZolvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= NVzXTIxwOjR4MUC4Nlc>
L428 NGfzeXJCeG:ydH;zbZMhSXO|YYm= MV6wM|AvPjJ3L{GuNlUh|ryP MmTOOFghcA>? MVvpcoR2[2W|IITo[UBieG:ydH;zbZPDqA>? MknSNlQ3OTB6Mke=
KMH2 MXrBdI9xfG:|aYOgRZN{[Xl? M37IeFAwOC54MkWvNU4zPSEQvF2= NWXrW28yPDhiaB?= MVrpcoR2[2W|IITo[UBieG:ydH;zbZPDqA>? Ml\FNlQ3OTB6Mke=
L1236 NHeyRoxCeG:ydH;zbZMhSXO|YYm= MlzsNE8xNjZ{NT:xMlI2KM7:TR?= M1S0fFQ5KGh? MXzpcoR2[2W|IITo[UBieG:ydH;zbZPDqA>? NF;nXW4zPDZzMEiyOy=>
SUPHD1 NXW3NGRvSXCxcITvd4l{KEG|c3H5 MUCwM|AvPjJ3L{GuNlUh|ryP MmXpOFghcA>? Ml\SbY5lfWOnczD0bIUh[XCxcITvd4l{yqB? NGfPUW8zPDZzMEiyOy=>
HDLM2 MWjBdI9xfG:|aYOgRZN{[Xl? M3;mb|AwOC54MkWvNU4zPSEQvF2= MYe0PEBp M3XJeYlv\HWlZYOgeIhmKGGyb4D0c5Nqe8Li NIHFeFQzPDZzMEiyOy=>
K1106P MmW2RZBweHSxc3nzJGF{e2G7 M3;mclAwOC54MkWvNU4zPSEQvF2= MonwOFghcA>? MkG0bY5lfWOnczD0bIUh[XCxcITvd4l{yqB? MYiyOFYyODh{Nx?=
L428 NUSxbZo{TnWwY4Tpc44hSXO|YYm= NVrzZo5GOC13IN88US=> MlzPNlQhcA>? MYnpcohq[mm2czDKRWszN1OWQWSgd4lodmGuaX7n MUmyOFYyODh{Nx?=
KMH2 MV7GeY5kfGmxbjDBd5NigQ>? MlXONE02KM7:TR?= NFHNTJYzPCCq NVe2PJFjcW6qaXLpeJMhUkGNMj;TWGFVKHOrZ37hcIlv\w>? NInE[G4zPDZzMEiyOy=>
L1236 Mn36SpVv[3Srb36gRZN{[Xl? NU\sSFhpOC13IN88US=> M4DnNlI1KGh? NGrIW5lqdmirYnn0d{BLSUt{L2PURXQhe2mpbnHsbY5o MoS5NlQ3OTB6Mke=
SUPHD1 MWfGeY5kfGmxbjDBd5NigQ>? NX7iemFSOC13IN88US=> MV6yOEBp MlPybY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> MkD4NlQ3OTB6Mke=
HDLM2 M1fYV2Z2dmO2aX;uJGF{e2G7 NUnHUnpIOC13IN88US=> MYiyOEBp Mn;sbY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> MX:yOFYyODh{Nx?=
K1106P NEiwUnBHfW6ldHnvckBCe3OjeR?= M1z2W|AuPSEQvF2= MojpNlQhcA>? MWnpcohq[mm2czDKRWszN1OWQWSgd4lodmGuaX7n M3W1TVI1PjFyOEK3
MM.1S  M4rRVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUT3RYhsUUN3ME2xMVMh|ryP MWqyOFU5PDFyMR?=
TpoR JAK2 WT MnPoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3NOndKSzVyPUGuOEApOS5|4pETNU42MSEQvF2= MYWyOFI2OTd7MB?=
TpoR JAK2 V617F MoLtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTBwODCoNE446oDVMD65LUDPxE1? MX:yOFI2OTd7MB?=
TpoR W515L Mm\WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\lTWM2OD1yLkigLFAvP+LCk{GuNEkh|ryP NI\6fVQzPDJ3MUe5NC=>
Bcr-abl MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTJwNzCoNk4z6oDVMz6zLUDPxE1? M{DLWlI1OjVzN{mw
JAK2 TW M4TucGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnve3hLUUN3ME2xMlghMDFwNfMAl|IvOylizszN MlfFNlQzPTF5OUC=
JAK2 V617F NGjme4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DiR2lEPTB;MD62JEgxNjckgKOwMlcqKM7:TR?= NV73UpgzOjR{NUG3PVA>
MedB-1 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYG0JO69VQ>? MoS5NlQwPDhxN{KgbC=> MkjWSG1UVw>? Mn34bY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> NXuwfYpVOjN6NUKzOlY>
K1106 NGTyS4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PGU|Qh|ryP NFnsdVkzPC92OD:3NkBp NVHVWGs6TE2VTx?= M{PUV4lvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> MnvVNlM5PTJ|Nk[=
U2940 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfDR3NOPCEQvF2= Mn7PNlQwPDhxN{KgbC=> M3zkPGROW09? MormbY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> M2PhflI{QDV{M{[2
FE-PD NEPxOYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjDXFgxNjB4Mz20JO69VQ>? MYPJR|UxRTlwNTFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? MXeyN|M4OjZ4OR?=
HEL NYfD[JlvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWSwMlA3Oy12IN88US=> MmnpTWM2OD1zLkWg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 MY[yN|M4OjZ4OR?=
K-562 M1SxUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXqNE4xPjNvNDFOwG0> MojMTWM2OD1{LkWg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 MmDLNlM{PzJ4Nkm=
L-82 M1LtOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVuwMlA3Oy12IN88US=> MWjJR|UxRTBwOUig{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 NWH5e3VCOjN|N{K2Olk>
MAC-1 MlHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUf3c25VOC5yNkOtOEDPxE1? MYXJR|UxRTBwNUKg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 NFzNOpYzOzN5Mk[2PS=>
MAC-2A MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWWwMlA3Oy12IN88US=> M{HBTmlEPTB;MD62PUDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= M2nFWVI{Ozd{Nk[5
MAC-2B MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUmwMlA3Oy12IN88US=> MoToTWM2OD1yLkW0JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= M2TOPFI{Ozd{Nk[5
MY-LA NW\zVGJbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjMT5AxNjB4Mz20JO69VQ>? M4PnOWlEPTB;Mj6xJO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= NEnscHMzOzN5Mk[2PS=>
NC-NC NGnVb4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXiwMlA3Oy12IN88US=> NWf1ZnNoUUN3ME2xMlAh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MX6yN|M4OjZ4OR?=
SE-AX M{H5WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXSwMlA3Oy12IN88US=> NIXSfFVKSzVyPUGuOUDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= NWfocY9jOjN|N{K2Olk>
SR-786 MlXHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHJdlgxNjB4Mz20JO69VQ>? NW\sSZVnUUN3ME20MlYh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NFHIe5YzOzN5Mk[2PS=>
M-MOK  M2TGUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWqyOUDDvU4EoB?= NVrY[ndEOjRxNEivO|IhcA>? NWnNdHJ5TE2VTx?= M4LLTYlvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> M4rMPVIyQDV|MUW3
HEL NUjCR5BET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{S1VmlEPTB;M{C1JI5O Mn\1NVg{QTR3NUS=
Ba/F3 JAK2V617F MmnKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn30TWM2OD1{N{Cgcm0> NVTFdlBPOTh|OUS1OVQ>

... 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
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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
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  • 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
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  • 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 <1 mg/mL
Ethanol <1 mg/mL
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 Information

Molecular Weight 524.68
Formula

C27H36N6O3S

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

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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.

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