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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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

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 NVT6d3prSXCxcITvd4l{KEG|c3H5 NYjvbJZYOC53LUKg{txO M4X0bFEzNTR6IHi= NHPXd2tFVVOR NGj3b45qdmS3Y3XzJIFxd3C2b4Ppd{BqdiCkb4ToJIRwe2VvIHHu[EB1cW2nLTDk[ZBmdmSnboSgcYFvdmW{ MXGyOVg3QTJzMB?=
H1650 MknvRZBweHSxc3nzJGF{e2G7 Moi3NE42NTJizszN MmDxNVIuPDhiaB?= NUn5eFAzTE2VTx?= MVjpcoR2[2W|IHHwc5B1d3OrczDpckBjd3SqIHTvd4UuKGGwZDD0bY1mNSCmZYDlcoRmdnRibXHucoVz NG\IUJUzPTh4OUKxNC=>
H1975 NYL1O3NLTnWwY4Tpc44hSXO|YYm= MXWwMlI2NTFizszN NFnyTIszPCCq M{jrVGROW09? MkP2bY5pcWKrdIOg[ZhxemW|c3nvckBw\iCjcH;weI9{cXNvcnXsZZRm\CCycn;0[YlvKEKlbD3YUEwhSmOuLUKsJJN2en[rdnnuMEBZUUGS NFrr[IMzPTh4OUKxNC=>
H1650 NEjrbJRHfW6ldHnvckBCe3OjeR?= MmjPNE4zPS1zIN88US=> NHrlcpYzPCCq MlHISG1UVw>? MVHpcohq[mm2czDlfJBz\XO|aX;uJI9nKGGyb4D0c5Nqey2{ZXzheIVlKHC{b4TlbY4hSmOuLWjMMEBD[2xvMjygd5Vzfmm4aX6sJHhKSVB? NY\rdXZQOjV6NkmyNVA>
H1975 MlHFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFn6NYsyKM7:TR?= MVK0PEBp M4rGVmROW09? Mnj0d4Vve2m2aYrld{Bk\WyuczD0c{B1cGViY4n0c5RwgGmlaYT5JI9nKGW{bH;0bY5q[g>? MVmyOVg3QTJzMB?=
H1650 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MormNUDPxE1? MUe0PEBp MVfEUXNQ NF\mWJB{\W6|aYTpfoV{KGOnbHzzJJRwKHSqZTDjfZRwfG:6aXPpeJkhd2ZiZYLsc5Rqdmmk NXflZ2dEOjV6NkmyNVA>
CD4+ T Mn\SSpVv[3Srb36gRZN{[Xl? NGq5W3UxNjBzLUGg{txO MnLoOFghcA>? M17wTmROW09? MnjqdoVlfWOnczD0bIUheGixc4Doc5J6dGG2aX;uJIxmfmWuczDv[kBLSUt{IHHu[EBUXEGWM9Mg MlHKNlU2PzJ3M{W=
Caco-2  MX7GeY5kfGmxbjDBd5NigQ>? MYGwMVEzOCEQvF2= MX63JI1qdg>? MVnpcohq[mm2czD0bIlidWmwZTD1dJRic2Vid3n0bEBidiCLQ{WwxsBw\iB{LkJCpOK2VQ>? NEHXTFQzPTB4M{[3Ni=>
Caco-2  MX3GeY5kfGmxbjDBd5NigQ>? NEPZR2syOC93MD:xNFAh|ryP NInPWnczKGh? M3r3UYRm[3KnYYPld{B1cGViZnz1fEBw\iCdM1jdeIhq[W2rbnWgZYNzd3O|IITo[UBud26xbHH5[ZIhf2m2aDDJR|UxKG:oIE[uOeKh|ryP NXnqb2o5OjVyNkO2O|I>
HEK293 MSR  MoHUSpVv[3Srb36gRZN{[Xl? M3\ZWlAuOTBizszN MYe3JI1qdg>? MUDpcohq[mm2czDoWGhVWjJid3n0bEBidiCLQ{WwxsBw\iBzLkNCpOK2VQ>? M4Wwb|I2ODZ|Nkey
MedB-1 NICyVmtHfW6ldHnvckBCe3OjeR?= MWSxM|Ih|ryP MWKyOEBp MnnP[IVkemWjc3XzJHNVSVR4IIDoc5NxcG:{eXzheIlwdiClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NX\BcXVIOjR7N{e2Olg>
U2940 M1PlS2Z2dmO2aX;uJGF{e2G7 MmLKNU8zKM7:TR?= NGD4PHczPCCq MXvk[YNz\WG|ZYOgV3RCXDZicHjvd5Bpd3K7bHH0bY9vKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> MmT5NlQ6Pzd4Nki=
K1106 NX6wOJduTnWwY4Tpc44hSXO|YYm= MYSxM|Ih|ryP MnPCNlQhcA>? MmO5[IVkemWjc3XzJHNVSVR4IIDoc5NxcG:{eXzheIlwdiClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NH;xPY4zPDl5N{[2PC=>
K562 NH3xZ2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzjc|VkOC1zIN88US=> NUCybY5PPzJiaB?= MVPpcohq[mm2czDLOVYzKGOnbHygdJJwdGmoZYLheIlwdiCjdDDobYdpKGOxbnPlcpRz[XSrb36= M{D0dVI1Pzd3M{C4
MDA-MB-468  MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTaUHF6OyEEtV2= NUjVU|lCPDhiaB?= M3;4dIVvcGGwY3XkJJNq[mOuNjDpcoR2[2WmIHzvd5Mhd2ZiY3XscEB3cWGkaXzpeJnDqA>? NE\hXYczPDZ4MkixPC=>
MDA-MB-468 M2DLNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3GRm41OC12IN88US=> M4T3[lQ5KGh? NXPyNIJyemW|dXz0d{B{cWewaX\pZ4FvfCCub4PzJI9nKH[rYXLpcIl1gSClb33wZZJm\CC2bzDSTU1DWEliYXzvcoU> NE\JUpEzPDZ4MkixPC=>
L428 NH3YWFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HoNlAuPSEQvF2= MXK0PEBp MVLpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 NH;VcJYzPDZzMEiyOy=>
KMH2 NHfZXXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1PpeVAuPSEQvF2= MnXqOFghcA>? Ml[2bY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= MnrLNlQ3OTB6Mke=
L1236 NFW3bIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLBVocxNTVizszN MlLvOFghcA>? M2DyUYlvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= NVHWTGtPOjR4MUC4Nlc>
SUPHD1 NEPpS2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvWSZhYOC13IN88US=> NXfUPJFHPDhiaB?= Mkn4bY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= M{njXVI1PjFyOEK3
HDLM2 M3Px[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\rTVExNTVizszN M3vQcFQ5KGh? NV3PbZU1cW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> MYWyOFYyODh{Nx?=
K1106P NGny[o1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPqW3IxNTVizszN MWi0PEBp NU\WS3ZocW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> NIf6d|gzPDZzMEiyOy=>
L428 NWLlfFJDSXCxcITvd4l{KEG|c3H5 NFzBVVUxNzBwNkK1M|EvOjVizszN NVjZTpk{PDhiaB?= NVqyVo5ncW6mdXPld{B1cGViYYDvdJRwe2m|wrC= MXmyOFYyODh{Nx?=
KMH2 MUDBdI9xfG:|aYOgRZN{[Xl? M2DLSlAwOC54MkWvNU4zPSEQvF2= M2niSVQ5KGh? NWLF[ZlLcW6mdXPld{B1cGViYYDvdJRwe2m|wrC= MYOyOFYyODh{Nx?=
L1236 MUPBdI9xfG:|aYOgRZN{[Xl? M1vneVAwOC54MkWvNU4zPSEQvF2= NF3zfVQ1QCCq NV7uW2ZrcW6mdXPld{B1cGViYYDvdJRwe2m|wrC= MWOyOFYyODh{Nx?=
SUPHD1 MlLORZBweHSxc3nzJGF{e2G7 MVmwM|AvPjJ3L{GuNlUh|ryP M3G4WFQ5KGh? NFLpZVBqdmS3Y3XzJJRp\SCjcH;weI9{cXQEoB?= M2PFSlI1PjFyOEK3
HDLM2 MnW3RZBweHSxc3nzJGF{e2G7 NYXk[3YzOC9yLk[yOU8yNjJ3IN88US=> M3frOFQ5KGh? MV;pcoR2[2W|IITo[UBieG:ydH;zbZPDqA>? M{Wyb|I1PjFyOEK3
K1106P MXHBdI9xfG:|aYOgRZN{[Xl? M2jZUVAwOC54MkWvNU4zPSEQvF2= MkLlOFghcA>? MX3pcoR2[2W|IITo[UBieG:ydH;zbZPDqA>? NWm3RXlUOjR4MUC4Nlc>
L428 NG\l[5RHfW6ldHnvckBCe3OjeR?= NVruZodpOC13IN88US=> Mnj5NlQhcA>? NX\wVI8{cW6qaXLpeJMhUkGNMj;TWGFVKHOrZ37hcIlv\w>? NFG3S2gzPDZzMEiyOy=>
KMH2 MUTGeY5kfGmxbjDBd5NigQ>? NWfoS3kxOC13IN88US=> NILZUnUzPCCq M4XzOYlvcGmkaYTzJGpCUzJxU2TBWEB{cWewYXzpcoc> MV6yOFYyODh{Nx?=
L1236 NHvaSI5HfW6ldHnvckBCe3OjeR?= M3znZVAuPSEQvF2= Mn3YNlQhcA>? MlSxbY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> NHn2PG0zPDZzMEiyOy=>
SUPHD1 M{Wx[mZ2dmO2aX;uJGF{e2G7 NF\lb4ExNTVizszN Mn3LNlQhcA>? MmXjbY5pcWKrdIOgTmFMOi:VVFHUJJNq\26jbHnu[y=> NGWyU4YzPDZzMEiyOy=>
HDLM2 MUfGeY5kfGmxbjDBd5NigQ>? NVfvS3QxOC13IN88US=> MWCyOEBp MWTpcohq[mm2czDKRWszN1OWQWSgd4lodmGuaX7n M1rSNlI1PjFyOEK3
K1106P MkjhSpVv[3Srb36gRZN{[Xl? M1jiRlAuPSEQvF2= MWKyOEBp MUjpcohq[mm2czDKRWszN1OWQWSgd4lodmGuaX7n M2fnZlI1PjFyOEK3
MM.1S  MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDabY1FUUN3ME2xMVMh|ryP NGfnRm4zPDV6NEGwNS=>
TpoR JAK2 WT MorMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTFwNDCoNU4{6oDVMT61LUDPxE1? NUXKWZhTOjR{NUG3PVA>
TpoR JAK2 V617F MkjuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfPTWM2OD1yLkigLFAvP+LCk{CuPUkh|ryP MUWyOFI2OTd7MB?=
TpoR W515L MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTWTWM2OD1yLkigLFAvP+LCk{GuNEkh|ryP M{m5TFI1OjVzN{mw
Bcr-abl NXXDeVB3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXPTWM2OD1{LkegLFIvOuLCk{OuN{kh|ryP MXuyOFI2OTd7MB?=
JAK2 TW M2nKVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjqW3FXUUN3ME2xMlghMDFwNfMAl|IvOylizszN NGTRNHUzPDJ3MUe5NC=>
JAK2 V617F Moj3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\heWlEPTB;MD62JEgxNjckgKOwMlcqKM7:TR?= NIjnW4ozPDJ3MUe5NC=>
MedB-1 NITacG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mki3OEDPxE1? MonaNlQwPDhxN{KgbC=> M17EfGROW09? MnixbY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> NWjKUXR6OjN6NUKzOlY>
K1106 NGfGSY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXSVFduPCEQvF2= MWWyOE81QC95MjDo NX7meXByTE2VTx?= M3fqNIlvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> NW\vU5dVOjN6NUKzOlY>
U2940 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPkbIN7PCEQvF2= MnvzNlQwPDhxN{KgbC=> NGXUdnVFVVOR NEDxSWJqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 MVeyN|g2OjN4Nh?=
FE-PD M1fNfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUfkfIVkOC5yNkOtOEDPxE1? M1W1VGlEPTB;OT61JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= NHO0eJIzOzN5Mk[2PS=>
HEL NWrCTWc1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\CZ|AvODZ|LUSg{txO NVntZms3UUN3ME2xMlUh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NXrPbVVjOjN|N{K2Olk>
K-562 M1exXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jHeFAvODZ|LUSg{txO NUe3cJFXUUN3ME2yMlUh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MVWyN|M4OjZ4OR?=
L-82 MnH0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPjS2QxNjB4Mz20JO69VQ>? MlnFTWM2OD1yLkm4JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= MmjwNlM{PzJ4Nkm=
MAC-1 M3nvRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\4NE4xPjNvNDFOwG0> M{nQS2lEPTB;MD61NkDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIRwe2ViZHXw[Y5l\W62bIm= NWPCRZQxOjN|N{K2Olk>
MAC-2A MmXyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfKWFUxNjB4Mz20JO69VQ>? MXXJR|UxRTBwNkmg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDkc5NmKGSncHXu[IVvfGy7 NHri[oMzOzN5Mk[2PS=>
MAC-2B NH\TeG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn:zNE4xPjNvNDFOwG0> NWT4T3g6UUN3ME2wMlU1KM7:TTygbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NYH6PXVNOjN|N{K2Olk>
MY-LA MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX2wMlA3Oy12IN88US=> M3PKeWlEPTB;Mj6xJO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= MYqyN|M4OjZ4OR?=
NC-NC MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYewMlA3Oy12IN88US=> M{OxN2lEPTB;MT6wJO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= NYXyNmRHOjN|N{K2Olk>
SE-AX NGK5UGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrDXYwxNjB4Mz20JO69VQ>? NV;w[I1HUUN3ME2xMlUh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NUXqWllzOjN|N{K2Olk>
SR-786 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVGwMlA3Oy12IN88US=> M37GbmlEPTB;ND62JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHig[I9{\SCmZYDlcoRmdnSueR?= M3PZfFI{Ozd{Nk[5
M-MOK  Ml:zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoD3NlUhyrWPwrC= MXyyOE81QC95MjDo MlrrSG1UVw>? M4rQTIlvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> Moj3NlE5PTNzNUe=
HEL M{e4cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTNyNTDuUS=> NU\XWldJOTh|OUS1OVQ>
Ba/F3 JAK2V617F MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjSb21KSzVyPUK3NEBvVQ>? Ml7wNVg{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]
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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]
+ 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 <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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    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