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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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 M2TJNWFxd3C2b4Ppd{BCe3OjeR?= NHTBdooxNjVvMjFOwG0> M3m0VFEzNTR6IHi= M4XqWWROW09? NXLqVIhxcW6mdXPld{BieG:ydH;zbZMhcW5iYn;0bEBld3OnLTDhcoQhfGmvZT2g[IVx\W6mZX70JI1idm6nch?= MmjUNlU5Pjl{MUC=
H1650 M4rQOmFxd3C2b4Ppd{BCe3OjeR?= NEfzWpExNjVvMjFOwG0> MXmxNk01QCCq NIH5bopFVVOR NV3PUplycW6mdXPld{BieG:ydH;zbZMhcW5iYn;0bEBld3OnLTDhcoQhfGmvZT2g[IVx\W6mZX70JI1idm6nch?= NF3NbVMzPTh4OUKxNC=>
H1975 MoHxSpVv[3Srb36gRZN{[Xl? NHHmT2IxNjJ3LUGg{txO M3zId|I1KGh? NFnkUGZFVVOR MVjpcohq[mm2czDlfJBz\XO|aX;uJI9nKGGyb4D0c5Nqey2{ZXzheIVlKHC{b4TlbY4hSmOuLWjMMEBD[2xvMjygd5Vzfmm4aX6sJHhKSVB? MlLLNlU5Pjl{MUC=
H1650 NETvR4JHfW6ldHnvckBCe3OjeR?= M4LnSlAvOjVvMTFOwG0> MWqyOEBp NFLDNZBFVVOR NETMU5BqdmirYnn0d{BmgHC{ZYPzbY9vKG:oIHHwc5B1d3Orcz3y[YxifGWmIIDyc5RmcW5iQnPsMXhNNCCEY3ytNkwhe3W{dnn2bY4tKFiLQWC= NV6yUpNNOjV6NkmyNVA>
H1975 NIGwRWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYq0XJp4OSEQvF2= Mnu2OFghcA>? Mmm1SG1UVw>? NVX4PYEye2Wwc3n0bZpmeyClZXzsd{B1dyC2aHWgZ5l1d3SxeHnjbZR6KG:oIHXycI91cW6rYh?= NY\iVnJ4OjV6NkmyNVA>
H1650 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYqxJO69VQ>? NInsOGE1QCCq MmjCSG1UVw>? MUTz[Y5{cXSrenXzJINmdGy|IITvJJRp\SCleYTveI95cWOrdImgc4Yh\XKub4Tpcolj NGryPGEzPTh4OUKxNC=>
CD4+ T NI\qXnlHfW6ldHnvckBCe3OjeR?= MoHiNE4xOS1zIN88US=> MVO0PEBp MVvEUXNQ MmPHdoVlfWOnczD0bIUheGixc4Doc5J6dGG2aX;uJIxmfmWuczDv[kBLSUt{IHHu[EBUXEGWM9Mg MofwNlU2PzJ3M{W=
Caco-2  NETuRZFHfW6ldHnvckBCe3OjeR?= MoPtNE0yOjBizszN Mn3FO{BucW5? MYfpcohq[mm2czD0bIlidWmwZTD1dJRic2Vid3n0bEBidiCLQ{WwxsBw\iB{LkJCpOK2VQ>? MWOyOVA3OzZ5Mh?=
Caco-2  MUHGeY5kfGmxbjDBd5NigQ>? M{HMcVExNzVyL{GwNEDPxE1? M{e1Z|IhcA>? NIfMfGtl\WO{ZXHz[ZMhfGinIH\seZghd2ZiW{PIYZRpcWGvaX7lJIFkem:|czD0bIUhdW:wb3zhfYVzKHerdHigTWM2OCCxZjC2MlXDqM7:TR?= NWrkOJlbOjVyNkO2O|I>
HEK293 MSR  NWPEbII5TnWwY4Tpc44hSXO|YYm= MUiwMVExKM7:TR?= MnzQO{BucW5? NWLL[JlTcW6qaXLpeJMhcFSKVGKyJJdqfGhiYX6gTWM2OMLib3[gNU4zyqEEtV2= MWKyOVA3OzZ5Mh?=
MedB-1 MX;GeY5kfGmxbjDBd5NigQ>? NWjWSoJkOS9{IN88US=> M3;FVlI1KGh? M{fVfoRm[3KnYYPld{BUXEGWNjDwbI9{eGixconsZZRqd25iY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? M2fYNFI1QTd5Nk[4
U2940 NWPTOmpZTnWwY4Tpc44hSXO|YYm= M4DCNVEwOiEQvF2= MmPDNlQhcA>? MmW1[IVkemWjc3XzJHNVSVR4IIDoc5NxcG:{eXzheIlwdiClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NH;Z[WkzPDl5N{[2PC=>
K1106 MlKwSpVv[3Srb36gRZN{[Xl? MkjKNU8zKM7:TR?= MYOyOEBp M1TTOIRm[3KnYYPld{BUXEGWNjDwbI9{eGixconsZZRqd25iY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? MoT0NlQ6Pzd4Nki=
K562 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3nzdVAuOSEQvF2= MUC3NkBp NHmyPXdqdmirYnn0d{BMPTZ{IHPlcIwheHKxbHnm[ZJifGmxbjDheEBpcWeqIHPvcoNmdnS{YYTpc44> NX[wbpk6OjR5N{WzNFg>
MDA-MB-468  NVfBfIVTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nqW|MhyrWP MkLOOFghcA>? M{myTIVvcGGwY3XkJJNq[mOuNjDpcoR2[2WmIHzvd5Mhd2ZiY3XscEB3cWGkaXzpeJnDqA>? NYDRZXJXOjR4NkK4NVg>
MDA-MB-468 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVuwMVQh|ryP M{KxRlQ5KGh? NXrJ[JFEemW|dXz0d{B{cWewaX\pZ4FvfCCub4PzJI9nKH[rYXLpcIl1gSClb33wZZJm\CC2bzDSTU1DWEliYXzvcoU> NVL3b3I6OjR4NkK4NVg>
L428 MmDLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NET2cWQxNTVizszN NUTpcGpQPDhiaB?= M2LF[4lvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= MlXrNlQ3OTB6Mke=
KMH2 NH;NO29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTLN2RLOC13IN88US=> NWnKNGZlPDhiaB?= M1jsVYlvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= M3LwVFI1PjFyOEK3
L1236 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPQWmkzOC13IN88US=> MmHCOFghcA>? MXzpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 NX3adVh7OjR4MUC4Nlc>
SUPHD1 MnvQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TaeFAuPSEQvF2= Mmn6OFghcA>? NUG1fFJNcW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> MVuyOFYyODh{Nx?=
HDLM2 M1vKR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonsNE02KM7:TR?= NEfzNYc1QCCq NHPz[plqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 NW\rPIc1OjR4MUC4Nlc>
K1106P NF33eWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrZNE02KM7:TR?= M2DmWlQ5KGh? MUHpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 M3nhTlI1PjFyOEK3
L428 MlHVRZBweHSxc3nzJGF{e2G7 Mnm5NE8xNjZ{NT:xMlI2KM7:TR?= NUHjOpp3PDhiaB?= M{HlVYlv\HWlZYOgeIhmKGGyb4D0c5Nqe8Li MWeyOFYyODh{Nx?=
KMH2 M3LNVWFxd3C2b4Ppd{BCe3OjeR?= M17PNVAwOC54MkWvNU4zPSEQvF2= MkmyOFghcA>? MoG5bY5lfWOnczD0bIUh[XCxcITvd4l{yqB? NXzYSW1wOjR4MUC4Nlc>
L1236 M17uSGFxd3C2b4Ppd{BCe3OjeR?= M4fXXFAwOC54MkWvNU4zPSEQvF2= MYm0PEBp NEHpe|dqdmS3Y3XzJJRp\SCjcH;weI9{cXQEoB?= M{fmelI1PjFyOEK3
SUPHD1 NV\sZndMSXCxcITvd4l{KEG|c3H5 NEjJXpUxNzBwNkK1M|EvOjVizszN Mny1OFghcA>? M2fLWolv\HWlZYOgeIhmKGGyb4D0c5Nqe8Li MlTUNlQ3OTB6Mke=
HDLM2 NXL3dHdHSXCxcITvd4l{KEG|c3H5 M2exU|AwOC54MkWvNU4zPSEQvF2= NXvNSJplPDhiaB?= NX\tV3VicW6mdXPld{B1cGViYYDvdJRwe2m|wrC= MU[yOFYyODh{Nx?=
K1106P MYTBdI9xfG:|aYOgRZN{[Xl? NXfpZ|BwOC9yLk[yOU8yNjJ3IN88US=> NH;QTo41QCCq M4LS[Ilv\HWlZYOgeIhmKGGyb4D0c5Nqe8Li M{DV[|I1PjFyOEK3
L428 M3q2cGZ2dmO2aX;uJGF{e2G7 MUCwMVUh|ryP NYi3cWViOjRiaB?= NFPm[4VqdmirYnn0d{BLSUt{L2PURXQhe2mpbnHsbY5o MUKyOFYyODh{Nx?=
KMH2 NVG4NFFrTnWwY4Tpc44hSXO|YYm= MlS4NE02KM7:TR?= NEezVHozPCCq MlvubY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> MlL4NlQ3OTB6Mke=
L1236 M3HwXmZ2dmO2aX;uJGF{e2G7 MoXZNE02KM7:TR?= Mo\5NlQhcA>? Ml;xbY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> NUHLN2lFOjR4MUC4Nlc>
SUPHD1 MYDGeY5kfGmxbjDBd5NigQ>? NVrYeWo4OC13IN88US=> MW[yOEBp MV\pcohq[mm2czDKRWszN1OWQWSgd4lodmGuaX7n MUKyOFYyODh{Nx?=
HDLM2 Mn[4SpVv[3Srb36gRZN{[Xl? M1f0VlAuPSEQvF2= NYHLNGpVOjRiaB?= MWrpcohq[mm2czDKRWszN1OWQWSgd4lodmGuaX7n M1TuZlI1PjFyOEK3
K1106P NHnF[mVHfW6ldHnvckBCe3OjeR?= NITsc|QxNTVizszN M{nHb|I1KGh? NHfsO3NqdmirYnn0d{BLSUt{L2PURXQhe2mpbnHsbY5o MnjmNlQ3OTB6Mke=
MM.1S  NV[yeoZvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmOzTWM2OD1zLUOg{txO Mn\TNlQ2QDRzMEG=
TpoR JAK2 WT MkPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTFwNDCoNU4{6oDVMT61LUDPxE1? M37CR|I1OjVzN{mw
TpoR JAK2 V617F MlvQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nPTGlEPTB;MD64JEgxNjgkgKOwMlkqKM7:TR?= MmLtNlQzPTF5OUC=
TpoR W515L MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYXVR3JbUUN3ME2wMlghMDBwN,MAl|EvOClizszN NV3lWHNwOjR{NUG3PVA>
Bcr-abl NHf3bJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\0cppKSzVyPUKuO{ApOi5{4pETN{4{MSEQvF2= M2jO[|I1OjVzN{mw
JAK2 TW M4flV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjvSGlVUUN3ME2xMlghMDFwNfMAl|IvOylizszN M2PSdVI1OjVzN{mw
JAK2 V617F M2jDWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTBwNjCoNE436oDVMD63LUDPxE1? M2nPRVI1OjVzN{mw
MedB-1 NFvFOZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLVOEDPxE1? M{jaUlI1NzR6L{eyJIg> NV\EXnU6TE2VTx?= MnvhbY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> NFHwXJAzOzh3MkO2Oi=>
K1106 NWqxd3RWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrrRmE1KM7:TR?= M1zrWVI1NzR6L{eyJIg> M1HiUGROW09? MU\pcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 M{TDbVI{QDV{M{[2
U2940 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHjOEDPxE1? MUGyOE81QC95MjDo NFnNZm1FVVOR MnLUbY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> MlXhNlM5PTJ|Nk[=
FE-PD MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHaSJRFOC5yNkOtOEDPxE1? MlrpTWM2OD17LkWg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 Mn;iNlM{PzJ4Nkm=
HEL NYPDSVdbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTnNE4xPjNvNDFOwG0> MoniTWM2OD1zLkWg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 M4\zN|I{Ozd{Nk[5
K-562 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrVV3kxNjB4Mz20JO69VQ>? NV;KSWZmUUN3ME2yMlUh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MYqyN|M4OjZ4OR?=
L-82 NFfTXoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1K0VVAvODZ|LUSg{txO NICxPWtKSzVyPUCuPVgh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 M1qyUVI{Ozd{Nk[5
MAC-1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLHNE4xPjNvNDFOwG0> NUjnRo5YUUN3ME2wMlUzKM7:TTygbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NYDJepZGOjN|N{K2Olk>
MAC-2A M17Od2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYKwMlA3Oy12IN88US=> MV7JR|UxRTBwNkmg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 NX21XFlwOjN|N{K2Olk>
MAC-2B M1jqPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXiwMlA3Oy12IN88US=> M{O4ZmlEPTB;MD61OEDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= NG\KU5kzOzN5Mk[2PS=>
MY-LA MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUL1[2FsOC5yNkOtOEDPxE1? M3fjbmlEPTB;Mj6xJO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= NFH2VGUzOzN5Mk[2PS=>
NC-NC NFnzS3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn73NE4xPjNvNDFOwG0> MXTJR|UxRTFwMDFOwG0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHTvd4Uh\GWyZX7k[Y51dHl? NF75VJUzOzN5Mk[2PS=>
SE-AX MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jrNFAvODZ|LUSg{txO NXfpb5BvUUN3ME2xMlUh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MUmyN|M4OjZ4OR?=
SR-786 NY\Te|ZiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYq3fW1mOC5yNkOtOEDPxE1? M3nyc2lEPTB;ND62JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= NIrFTWozOzN5Mk[2PS=>
M-MOK  MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHy[XBYOjViwsXNxsA> M2\0e|I1NzR6L{eyJIg> NGXzZ|NFVVOR NHXK[ZBqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 NInoO5ozOTh3M{G1Oy=>
HEL MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInwNIpKSzVyPUOwOUBvVQ>? NW\lRW94OTh|OUS1OVQ>
Ba/F3 JAK2V617F M1njTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljiTWM2OD1{N{Cgcm0> MUOxPFM6PDV3NB?=

... 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]
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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:[1]
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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:[1]
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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 Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
1% DMSO+30% polyethylene glycol+1% Tween 80
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
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.

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JAK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID