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 M3\SemFxd3C2b4Ppd{BCe3OjeR?= MmPaNE42NTJizszN NVTwe4p5OTJvNEigbC=> MnTPSG1UVw>? NF7UVJFqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCkb4ToJIRwe2VvIHHu[EB1cW2nLTDk[ZBmdmSnboSgcYFvdmW{ MknoNlU5Pjl{MUC=
H1650 M{ewOGFxd3C2b4Ppd{BCe3OjeR?= NVW4[XdrOC53LUKg{txO M1fxXVEzNTR6IHi= M4\VW2ROW09? NH3qVWJqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCkb4ToJIRwe2VvIHHu[EB1cW2nLTDk[ZBmdmSnboSgcYFvdmW{ M1;0elI2QDZ7MkGw
H1975 NF;MNplHfW6ldHnvckBCe3OjeR?= NYHwTo5tOC5{NT2xJO69VQ>? NXPhfIJEOjRiaB?= NGfzXm5FVVOR M3rabolvcGmkaYTzJIV5eHKnc4Ppc44hd2ZiYYDvdJRwe2m|LYLlcIF1\WRicILveIVqdiCEY3ytXGwtKEKlbD2yMEB{fXK4aY\pckwhYEmDUB?= Mk\kNlU5Pjl{MUC=
H1650 NGXUXopHfW6ldHnvckBCe3OjeR?= M4\YVlAvOjVvMTFOwG0> NUDHe|JEOjRiaB?= MYjEUXNQ NGf5eXNqdmirYnn0d{BmgHC{ZYPzbY9vKG:oIHHwc5B1d3Orcz3y[YxifGWmIIDyc5RmcW5iQnPsMXhNNCCEY3ytNkwhe3W{dnn2bY4tKFiLQWC= MYKyOVg3QTJzMB?=
H1975 NH;zZ3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLXSmt{OSEQvF2= NXTjR2M4PDhiaB?= NYXHZ4F{TE2VTx?= NH72Tmh{\W6|aYTpfoV{KGOnbHzzJJRwKHSqZTDjfZRwfG:6aXPpeJkhd2ZiZYLsc5Rqdmmk M3HBblI2QDZ7MkGw
H1650 NInxTINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PDTlEh|ryP NUnOTmRyPDhiaB?= M4LQWWROW09? MXzz[Y5{cXSrenXzJINmdGy|IITvJJRp\SCleYTveI95cWOrdImgc4Yh\XKub4Tpcolj M33EdFI2QDZ7MkGw
CD4+ T NYjHWVB6TnWwY4Tpc44hSXO|YYm= NHzhOGwxNjBzLUGg{txO M2X3O|Q5KGh? MmLFSG1UVw>? M{i4fZJm\HWlZYOgeIhmKHCqb4PwbI9zgWyjdHnvckBt\X[nbIOgc4YhUkGNMjDhcoQhW1SDVERCpC=> MVyyOVU4OjV|NR?=
Caco-2  NYnDfGFmTnWwY4Tpc44hSXO|YYm= M{npcVAuOTJyIN88US=> NESxU4I4KG2rbh?= M{HxPYlvcGmkaYTzJJRpcWGvaX7lJJVxfGGtZTD3bZRpKGGwIFnDOVDDqG:oIEKuNeKhyrWP NULIXIxPOjVyNkO2O|I>
Caco-2  M{THW2Z2dmO2aX;uJGF{e2G7 NXvMPWpzOTBxNUCvNVAxKM7:TR?= NUDabXRsOiCq NF7Y[Hhl\WO{ZXHz[ZMhfGinIH\seZghd2ZiW{PIYZRpcWGvaX7lJIFkem:|czD0bIUhdW:wb3zhfYVzKHerdHigTWM2OCCxZjC2MlXDqM7:TR?= NGjWR3czPTB4M{[3Ni=>
HEK293 MSR  Mki3SpVv[3Srb36gRZN{[Xl? MViwMVExKM7:TR?= M2rLSFchdWmw MVHpcohq[mm2czDoWGhVWjJid3n0bEBidiCLQ{WwxsBw\iBzLkNCpOK2VQ>? NG\mN|MzPTB4M{[3Ni=>
MedB-1 NEe5cnBHfW6ldHnvckBCe3OjeR?= M{X4flEwOiEQvF2= NWLITm15OjRiaB?= NHznem5l\WO{ZXHz[ZMhW1SDVE[gdIhwe3Cqb4L5cIF1cW:wIHPvcoNmdnS{YYTpc44h\GWyZX7k[Y51dHl? NG\DfmgzPDl5N{[2PC=>
U2940 MmL6SpVv[3Srb36gRZN{[Xl? NXmyZXNHOS9{IN88US=> NX;XXodlOjRiaB?= NIHWSFhl\WO{ZXHz[ZMhW1SDVE[gdIhwe3Cqb4L5cIF1cW:wIHPvcoNmdnS{YYTpc44h\GWyZX7k[Y51dHl? M1jXcVI1QTd5Nk[4
K1106 Mn3qSpVv[3Srb36gRZN{[Xl? NEDZenMyNzJizszN MlPYNlQhcA>? MYfk[YNz\WG|ZYOgV3RCXDZicHjvd5Bpd3K7bHH0bY9vKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> MWKyOFk4PzZ4OB?=
K562 NX;XOpNuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUKwMVEh|ryP NHe5V3A4OiCq NVjmZ21icW6qaXLpeJMhUzV4MjDj[YxtKHC{b3zp[oVz[XSrb36gZZQhcGmpaDDjc45k\W62cnH0bY9v M1XDPFI1Pzd3M{C4
MDA-MB-468  NYrtSoVjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYWzJOK2VQ>? MUC0PEBp Mm\R[Y5p[W6lZXSgd4lj[2x4IHnu[JVk\WRibH;zd{Bw\iClZXzsJJZq[WKrbHn0feKh M2LLdlI1PjZ{OEG4
MDA-MB-468 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUO2bW91OC12IN88US=> NWf5ZnJ5PDhiaB?= NUDXWYdDemW|dXz0d{B{cWewaX\pZ4FvfCCub4PzJI9nKH[rYXLpcIl1gSClb33wZZJm\CC2bzDSTU1DWEliYXzvcoU> MnHiNlQ3PjJ6MUi=
L428 NWfDO5ZIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jmdlAuPSEQvF2= MWG0PEBp MoXsbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= NIHPTWkzPDZzMEiyOy=>
KMH2 M3LCSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYCwMVUh|ryP NITYdGs1QCCq M1vhPIlvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= M2ntN|I1PjFyOEK3
L1236 Mm\IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoH0NE02KM7:TR?= M2jqXFQ5KGh? MkXjbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= NXHET3dCOjR4MUC4Nlc>
SUPHD1 M1PXdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXOwMVUh|ryP NVvJXpRTPDhiaB?= NVrKZ5o6cW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> M{S1clI1PjFyOEK3
HDLM2 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DUWFAuPSEQvF2= MnftOFghcA>? NWHudnA2cW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> MmXINlQ3OTB6Mke=
K1106P NWDzPJhKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUWwSox4OC13IN88US=> NVzodYxtPDhiaB?= Mo\WbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= M33DN|I1PjFyOEK3
L428 NYn0TmtOSXCxcITvd4l{KEG|c3H5 MVewM|AvPjJ3L{GuNlUh|ryP NX;WU|NUPDhiaB?= NGXRZm5qdmS3Y3XzJJRp\SCjcH;weI9{cXQEoB?= MlTVNlQ3OTB6Mke=
KMH2 MXnBdI9xfG:|aYOgRZN{[Xl? MlLRNE8xNjZ{NT:xMlI2KM7:TR?= NHTXTGI1QCCq NXTEUFBPcW6mdXPld{B1cGViYYDvdJRwe2m|wrC= NHTLTVgzPDZzMEiyOy=>
L1236 M4rjd2Fxd3C2b4Ppd{BCe3OjeR?= M4O2TlAwOC54MkWvNU4zPSEQvF2= MYq0PEBp NHjnWVVqdmS3Y3XzJJRp\SCjcH;weI9{cXQEoB?= NUfaemhxOjR4MUC4Nlc>
SUPHD1 MXHBdI9xfG:|aYOgRZN{[Xl? NE\YSFExNzBwNkK1M|EvOjVizszN NUK4SYhFPDhiaB?= M1ruPIlv\HWlZYOgeIhmKGGyb4D0c5Nqe8Li MV[yOFYyODh{Nx?=
HDLM2 M360NWFxd3C2b4Ppd{BCe3OjeR?= NIS3T4UxNzBwNkK1M|EvOjVizszN M1r4UFQ5KGh? MXfpcoR2[2W|IITo[UBieG:ydH;zbZPDqA>? NX;GeYE5OjR4MUC4Nlc>
K1106P M1HIZ2Fxd3C2b4Ppd{BCe3OjeR?= NFXTU4MxNzBwNkK1M|EvOjVizszN MXG0PEBp Mo\EbY5lfWOnczD0bIUh[XCxcITvd4l{yqB? MoTNNlQ3OTB6Mke=
L428 M{XCcmZ2dmO2aX;uJGF{e2G7 NWK3Roh{OC13IN88US=> MmjaNlQhcA>? M4HaTIlvcGmkaYTzJGpCUzJxU2TBWEB{cWewYXzpcoc> MVmyOFYyODh{Nx?=
KMH2 M2XjcWZ2dmO2aX;uJGF{e2G7 Ml3LNE02KM7:TR?= NF\ucZEzPCCq NX7CO2tGcW6qaXLpeJMhUkGNMj;TWGFVKHOrZ37hcIlv\w>? M3\kW|I1PjFyOEK3
L1236 MVvGeY5kfGmxbjDBd5NigQ>? NFLnco8xNTVizszN NH3sS5QzPCCq M1\2cIlvcGmkaYTzJGpCUzJxU2TBWEB{cWewYXzpcoc> NVjXUYRqOjR4MUC4Nlc>
SUPHD1 MUPGeY5kfGmxbjDBd5NigQ>? MXSwMVUh|ryP MWCyOEBp NWj1So1JcW6qaXLpeJMhUkGNMj;TWGFVKHOrZ37hcIlv\w>? MnHwNlQ3OTB6Mke=
HDLM2 NHHmSHhHfW6ldHnvckBCe3OjeR?= NH3wVo8xNTVizszN MoDTNlQhcA>? MmrQbY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> MXGyOFYyODh{Nx?=
K1106P MWPGeY5kfGmxbjDBd5NigQ>? NWLEXnhFOC13IN88US=> Mmf1NlQhcA>? MkXIbY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> M1PXdFI1PjFyOEK3
MM.1S  NXnlNlF{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfuNIxKUUN3ME2xMVMh|ryP MWeyOFU5PDFyMR?=
TpoR JAK2 WT Mnr5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjyO5JXUUN3ME2xMlQhMDFwM,MAl|EvPSlizszN NVrHclF2OjR{NUG3PVA>
TpoR JAK2 V617F Mof4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLPTWM2OD1yLkigLFAvP+LCk{CuPUkh|ryP MVWyOFI2OTd7MB?=
TpoR W515L M3;1cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTBwODCoNE446oDVMT6wLUDPxE1? Mnn0NlQzPTF5OUC=
Bcr-abl M37SUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTJwNzCoNk4z6oDVMz6zLUDPxE1? NGOwOm4zPDJ3MUe5NC=>
JAK2 TW MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTFwODCoNU426oDVMj6zLUDPxE1? NXfnXIxTOjR{NUG3PVA>
JAK2 V617F NELVZodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTBwNjCoNE436oDVMD63LUDPxE1? M1zUcVI1OjVzN{mw
MedB-1 MnTHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn[xOEDPxE1? M33INFI1NzR6L{eyJIg> NWDCVVl{TE2VTx?= NGi3dHVqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 MX[yN|g2OjN4Nh?=
K1106 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zLWVQh|ryP NH;MXFEzPC92OD:3NkBp M2\sTGROW09? MlzGbY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> NXPtXJFoOjN6NUKzOlY>
U2940 M{DGVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4W2WVQh|ryP NWC2RWJ3OjRxNEivO|IhcA>? NUDNTpdoTE2VTx?= MmntbY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> MVuyN|g2OjN4Nh?=
FE-PD NVmx[5doT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYSwMlA3Oy12IN88US=> MnPJTWM2OD17LkWg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 MWWyN|M4OjZ4OR?=
HEL NEW5WXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrXcmUxNjB4Mz20JO69VQ>? MlHETWM2OD1zLkWg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 MXKyN|M4OjZ4OR?=
K-562 M1fpOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWewMlA3Oy12IN88US=> NEDUXWlKSzVyPUKuOUDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= Mli3NlM{PzJ4Nkm=
L-82 MkTuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnzwNE4xPjNvNDFOwG0> MmPLTWM2OD1yLkm4JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= NEXmZ3YzOzN5Mk[2PS=>
MAC-1 MnG4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXGwMlA3Oy12IN88US=> MkjZTWM2OD1yLkWyJO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= M1fTUFI{Ozd{Nk[5
MAC-2A MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HSS|AvODZ|LUSg{txO NVX5N5dTUUN3ME2wMlY6KM7:TTygbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> M4W3R|I{Ozd{Nk[5
MAC-2B NXTDRYR3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDlZ4V3OC5yNkOtOEDPxE1? M4W1N2lEPTB;MD61OEDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= Mk[yNlM{PzJ4Nkm=
MY-LA M3XLVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjjV5MxNjB4Mz20JO69VQ>? NGThOlJKSzVyPUKuNUDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= M3PFb|I{Ozd{Nk[5
NC-NC NImzR5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M335dFAvODZ|LUSg{txO M{XBOmlEPTB;MT6wJO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= MnL1NlM{PzJ4Nkm=
SE-AX MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknCNE4xPjNvNDFOwG0> MlTYTWM2OD1zLkWg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 NGT2cHkzOzN5Mk[2PS=>
SR-786 NWDTW5lLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVewMlA3Oy12IN88US=> MmTMTWM2OD12Lk[g{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 MnnyNlM{PzJ4Nkm=
M-MOK  MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjjS3BFOjViwsXNxsA> NE[zfVIzPC92OD:3NkBp NI\XUYNFVVOR Mnm3bY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> NGPzVIEzOTh3M{G1Oy=>
HEL NF3kVIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mon0TWM2OD1|MEWgcm0> M2HqelE5Ozl2NUW0
Ba/F3 JAK2V617F MkLpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjXTWM2OD1{N{Cgcm0> MYCxPFM6PDV3NB?=

... 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 slightly soluble or insoluble
Ethanol slightly soluble or 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
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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID