R406

Catalog No.S2194

For research use only.

R406 is a potent Syk inhibitor with IC50 of 41 nM in cell-free assays, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. R406 induces apoptosis. Phase 1.

R406 Chemical Structure

CAS No. 841290-81-1

Selleck's R406 has been cited by 82 publications

Purity & Quality Control

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Biological Activity

Description R406 is a potent Syk inhibitor with IC50 of 41 nM in cell-free assays, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. R406 induces apoptosis. Phase 1.
Features Lead drug candidate for rheumatoid arthritis.
Targets
Flt3 [1]
(Cell-free assay)
Syk [1]
(Cell-free assay)
41 nM
In vitro

R406 is a potent inhibitor of immunoglobulin E (IgE)- and IgG-mediated activation of Fc receptor signaling. R406 inhibits the anti-IgE-induced production and release of LTC4 and cytokines and chemokines, including TNFα, IL-8, and GM-CSF. R406 inhibits phosphorylation of Syk substrate linker for activation of T cells in mast cells and B-cell linker protein/SLP65 in B cells. R406 binds to the ATP binding pocket of Syk and inhibits its kinase activity as an ATP-competitive inhibitor with Ki of 30 nM. R406 blocks Syk-dependent FcR-mediated activation of monocytes/macrophages and neutrophils and Bcr-mediated activation of B lymphocytes. [1] R406 significantly induces chronic lymphocytic leukemia (CLL) cell apoptosis in nurselike cells cocultures and blocks CCL3 and CCL4 secretion by CLL cells in response to B-cell antigen receptor (Bcr) triggering. [2] R406 is a potent inhibitor of platelet signaling and functions initiated by FcγRIIA cross-linking by specific antibodies or by sera from HIT patients. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
AMO-1 NHv2VHpHfW6ldHnvckBCe3OjeR?= M1\PclEh|ryP NYizOW5YO8LiaB?= MnjIdoVlfWOnczDtbYdz[XSrb39CpC=> NGjFelc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkK1NVc3OSd-Mk[yOVE4PjF:L3G+
U266 MoD6SpVv[3Srb36gRZN{[Xl? MmHqNUDPxE1? NXz4cJZCO8LiaB?= M3zGO5Jm\HWlZYOgcYloemG2aX;uxsA> MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjJ3MUe2NUc,OjZ{NUG3OlE9N2F-
Jeko-1 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrQbHI1QCCq M{Pqd2lEPTB;NT6wOlgzPiEQvF2= NX;FSZpRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4N|U4PTVpPkK1PFM2PzV3PD;hQi=>
Mino MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPjUGN3PDhiaB?= MVHJR|UxRTVwN{C4OVQh|ryP MmDtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6M{W3OVUoRjJ3OEO1O|U2RC:jPh?=
Jeko-1 M1;xeGFxd3C2b4Ppd{BCe3OjeR?= M4fFdVXDqM7:TR?= M1\QWlI1KGh? NVvNepZKcW6mdXPld{AzPS5zwrFCteKhOy5{wrClJIFxd3C2b4Ppdy=> M2XxV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEO1O|U2Lz5{NUizOVc2PTxxYU6=
primary MCL MV;BdI9xfG:|aYOgRZN{[Xl? MoO0NkDDvU1? NXzWR5IzOjRiaB?= NX7Me5B1cW6lcnXhd4V{KHOrZ37p[olk[W62bImgZZBweHSxc3nzxsA> M4riVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{i4N|c{Lz5{NUO4PFM4OzxxYU6=
PBMCs MoTIR4VtdCCYaXHibYxqfHliQYPzZZk> NYLJdGJLOC13MDFOwG0> NHvSNGIzPCCq Mn7lSG1UVw>? NWXiUoVGcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= M1K2XFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MUK3PFYzLz5{NUGyO|g3OjxxYU6=
PBMCs Ml;BSpVv[3Srb36gRZN{[Xl? NFz6ZYI2KM7:TR?= NXW1b3VLOSCq NYTqO3lDTE2VTx?= MVnk[YNz\WG|ZYOgeIhmKGOnbHygcYloemG2aX;u NHXtc3c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUGyO|g3Oid-MkWxNlc5PjJ:L3G+
CFSE-CD4+ T  M4PneWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnhZlAxNjB4MkWtNUDPxE1? M1rHUVQh\A>? M2jPWIJtd2OtczDwdo9tcW[ncnH0bY9vKG:oIFfWTGQu\GW{aY\l[EBETDRtwrDUJINmdGy|IHHu[EBETDFzYjxCpINmdGy| NVnT[IR6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2O|k6QDJpPkK0Olc6QTh{PD;hQi=>
CFSE-CD11b+ MkXtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXjSoUxNjB4MkWtNUDPxE1? Mn\PPEBl NGnBfXljdG:la4OgdJJwdGmoZYLheIlwdiCxZjDHWmhFNWSncnn2[YQhS0R2K9MgWEBk\WyuczDhcoQhS0RzMXKrxsBk\Wyucx?= MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ5OUm4Nkc,OjR4N{m5PFI9N2F-
HMECs NH25e4RHfW6ldHnvckBCe3OjeR?= MUOwMVExKM7:TR?= NYPzcm1iOjBibXnu MX7pcohq[mm2czDWSWdHNXO2aX31cIF1\WRicnXs[YF{\SCxZjDOUy=> MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN{OUW0OEc,OjR|Mkm1OFQ9N2F-
AB5 MXPBdI9xfG:|aYOgRZN{[Xl? MoDoNE0zNjVizszN MnjYOFghcA>? NXLGTYlPTE2VTx?= NEHyfnJqdmS3Y3XzJIFxd3C2b4Ppdy=> M4P2cVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{m4PVEyLz5{M{O5PFkyOTxxYU6=
JB7 NYiwWWhZSXCxcITvd4l{KEG|c3H5 NVvjdHJnOC1{LkWg{txO MljNOFghcA>? M3LtVGROW09? M1q0S4lv\HWlZYOgZZBweHSxc3nz NFvzT|E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O5PFkyOSd-MkOzPVg6OTF:L3G+
AB5 NXL6NYpxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXLNo5IOC1{LkWg{txO MYS0PEBp NWfVXnV5TE2VTx?= NYnCfYdTcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> M2XCZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{m4PVEyLz5{M{O5PFkyOTxxYU6=
JB7 M2HxVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUWwMVIvPSEQvF2= MlPiOFghcA>? NH75OnFFVVOR M2fPbYlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= NWfhVW9pRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzPVg6OTFpPkKzN|k5QTFzPD;hQi=>
RL NYHBN3lKTnWwY4Tpc44hSXO|YYm= MlTVNk42NzVizszN M3;pdFI1NzR6IHi= NGPtNZNFVVOR M1TwSolv\HWlZYOgZUBxd3SnboSg[IVkemWjc3WgbY4hVU2SLUmgcXJPSSCneIDy[ZN{cW:w NFm3XIg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUmyOlk3PSd-MkG5NlY6PjV:L3G+
RL M1GzbmZ2dmO2aX;uJGF{e2G7 NGXHSoYyNzJwNTFOwG0> MXKyOEBp MoLISG1UVw>? Mm\FdoVlfWOnczD0bIUh[WO2aY\heIlwdiCxZjDBb5Qh[W6mIIC3NHM3Uw>? NWK0bY9ORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5NlY6PjVpPkKxPVI3QTZ3PD;hQi=>
platelet  MYLGeY5kfGmxbjDBd5NigQ>? NF\Yc2IyyqEQvH2= M1WzUFUhdWmw NELsVoFqdmirYnn0d{BH[87|UlnJRU1u\WSrYYTl[EBxdGG2ZXzleEBi\2e{ZXfheIlwdg>? MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTh2OE[5OEc,OjF6NEi2PVQ9N2F-
platelet  NV\QbJk6TnWwY4Tpc44hSXO|YYm= MVKwMlA2NzFxMj61JO69VQ>? Mn7sOUBucW5? M2n4Z4lvcGmkaYTzJJRp\SC|aXfuZYxqdmdibXXjbIFvcXOvczDkc5dve3S{ZXHtJI9nKE[lzsPSTWlC M{O1UVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOES4Olk1Lz5{MUi0PFY6PDxxYU6=
DoHH2 MW\BdI9xfG:|aYOgRZN{[Xl? NFzoPGkxNzNxMUCg{txO NHvUUHk1QCCq NGDzOYFqdmS3Y3XzJINmdGxiZHXheIghe2mpbnnmbYNidnSueR?= MkHWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB6N{W0NFgoRjJyOEe1OFA5RC:jPh?=
Jeko-1  NF;NUnNCeG:ydH;zbZMhSXO|YYm= NULDd2hkOC9|L{GwJO69VQ>? NV7rZ4Z1PDhiaB?= NVfWfo5ZcW6mdXPld{Bk\WyuIHTlZZRpKHOrZ37p[olk[W62bIm= MmGyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB6N{W0NFgoRjJyOEe1OFA5RC:jPh?=
Raji  MkLTRZBweHSxc3nzJGF{e2G7 NV\2cYRPOC9|L{GwJO69VQ>? MWG0PEBp NHTiT5NqdmS3Y3XzJINmdGxiZHXheIghe2mpbnnmbYNidnSueR?= NWn3eFQzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4O|U1ODhpPkKwPFc2PDB6PD;hQi=>
DHL4 MVfBdI9xfG:|aYOgRZN{[Xl? MYWwM|EwPCEQvF2= NWftOGJbQTZiaB?= NV:2bWwzcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> NUHNXFM3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUiwNFY3QTZpPkG4NFA3Pjl4PD;hQi=>
LY7 NW\6cVl{SXCxcITvd4l{KEG|c3H5 M2nxPVAwOS92IN88US=> MmjRPVYhcA>? MYXpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NV;ZNY1tRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUiwNFY3QTZpPkG4NFA3Pjl4PD;hQi=>
LY3 NIHQZWVCeG:ydH;zbZMhSXO|YYm= MnT2NE8yNzRizszN NV7GVpROQTZiaB?= MXHpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NYfKU29jRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUiwNFY3QTZpPkG4NFA3Pjl4PD;hQi=>
DHL6 NET0SmdCeG:ydH;zbZMhSXO|YYm= MUOwM|EwPCEQvF2= MU[5OkBp M1rqbIlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDByNk[5Okc,OThyME[2PVY9N2F-
LY10 MknyRZBweHSxc3nzJGF{e2G7 M2DNclAwOS92IN88US=> NWrEUmRGQTZiaB?= MoPpbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= M{TtTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6MEC2Olk3Lz5zOECwOlY6PjxxYU6=
DHL10 MmD6RZBweHSxc3nzJGF{e2G7 M2XZVVAwOS92IN88US=> M2TT[Fk3KGh? MVnpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NEnURYg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOECwOlY6Pid-MUiwNFY3QTZ:L3G+
Wsu-NHL M13xfWFxd3C2b4Ppd{BCe3OjeR?= NYGwcG1lOC9zL{Sg{txO MlrNPVYhcA>? NETPVoRqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDByNk[5Okc,OThyME[2PVY9N2F-
LY18 NGjoZ4RCeG:ydH;zbZMhSXO|YYm= NUfWZmo6OC9zL{Sg{txO MoCxPVYhcA>? NEPwSZZqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 M2jOe|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6MEC2Olk3Lz5zOECwOlY6PjxxYU6=
LY1 NFHXOldCeG:ydH;zbZMhSXO|YYm= NIjBUlYxNzFxNDFOwG0> MWm5OkBp M2ftUYlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= M{XYZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6MEC2Olk3Lz5zOECwOlY6PjxxYU6=
DHL8 NGDzeINCeG:ydH;zbZMhSXO|YYm= NGPYVowxNzFxNDFOwG0> M{CzXVk3KGh? NIPF[2NqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 Ml3lQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOThyME[2PVYoRjF6MEC2Olk3RC:jPh?=
DHL4 NWHEXWJwSXCxcITvd4l{KEG|c3H5 NVvSTY5vPCEQvF2= M3vTZlk3KGh? MX7pcoR2[2W|IHPs[YF3[WenIH;mJINie3Cjc3XzJFkh[W6mIEOsJIJ2fCCwb4SgZ4F{eGG|ZTC4 M1\vWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6MEC2Olk3Lz5zOECwOlY6PjxxYU6=
DHL6 M3[3[WFxd3C2b4Ppd{BCe3OjeR?= NYq5fmU{PCEQvF2= NIj2WFE6PiCq M4m3eIlv\HWlZYOgZ4xm[X[jZ3Wgc4Yh[2G|cHHz[ZMhQSCjbnSgN{wh[nW2IH7veEBk[XOyYYPlJFg> M3;QNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6MEC2Olk3Lz5zOECwOlY6PjxxYU6=
LY3 M1i2NGFxd3C2b4Ppd{BCe3OjeR?= Ml7WOEDPxE1? MVq5OkBp MWDpcoR2[2W|IHPs[YF3[WenIH;mJINie3Cjc3XzJFkh[W6mIEOsJIJ2fCCwb4SgZ4F{eGG|ZTC4 NX:x[XhWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUiwNFY3QTZpPkG4NFA3Pjl4PD;hQi=>
LY7 NUjMPWZuSXCxcITvd4l{KEG|c3H5 M4Cw[VQh|ryP NHjxOpo6PiCq M1fWT4lv\HWlZYOgZ4xm[X[jZ3Wgc4Yh[2G|cHHz[ZMhQSCjbnSgN{wh[nW2IH7veEBk[XOyYYPlJFg> M2\YN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6MEC2Olk3Lz5zOECwOlY6PjxxYU6=
DHL4 NFXwSFhHfW6ldHnvckBCe3OjeR?= M1LUbVQh|ryP NVXCdFN3OTZiaB?= NHjqeFlqdmirYnn0d{B1d26rYzDCUG5MKHS7cn;zbY5mKHCqb4PwbI9zgWyjdHnvci=> NV;EbXRZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUiwNFY3QTZpPkG4NFA3Pjl4PD;hQi=>
LY7 NVX6O5R1TnWwY4Tpc44hSXO|YYm= MVq0JO69VQ>? NHLHfWkyPiCq MoXRbY5pcWKrdIOgeI9vcWNiQlzOT{B1gXKxc3nu[UBxcG:|cHjvdplt[XSrb36= NYG1NppMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUiwNFY3QTZpPkG4NFA3Pjl4PD;hQi=>
LY3 MUTGeY5kfGmxbjDBd5NigQ>? NIjhbZE1KM7:TR?= M3f0UVE3KGh? MUnpcohq[mm2czD0c45q[yCETF7LJJR6em:|aX7lJJBpd3OyaH;yfYxifGmxbh?= NWP1[YxRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUiwNFY3QTZpPkG4NFA3Pjl4PD;hQi=>
DHL6 M3vkcWZ2dmO2aX;uJGF{e2G7 MUK0JO69VQ>? NYHWbHdOOTZiaB?= M3TjPIlvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u M3LRZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6MEC2Olk3Lz5zOECwOlY6PjxxYU6=
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THP1 MlvLSpVv[3Srb36gZZN{[Xl? M1r1fGlvcGmkaYTpc44hd2ZiU2nLJIlvKGi3bXHuJHRJWDFiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJGZk\XC|aXzvcnIyN0[lZ3HtcYFTNW2nZHnheIVlKHOrZ37hcIlv\yC{ZYPwc45{\XNuIFXDOVA:OC5zN{JOwG0v MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJ3N{KxN{c,OjJ{NUeyNVM9N2F-
B-cells NYPCPGhXTnWwY4Tpc44h[XO|YYm= MV[xJIhz NX;peG5yUW6qaXLpeIlwdiCxZjDTfYshcW5iYXzwbIFK\01vc4TpcZVt[XSnZDDoeY1idiCEIHPlcIx{KGG|c3Xzd4VlKGG|IFPEPFYh\XiycnXzd4lwdiCjZoTldkAyKGi{IHnuZ5Vj[XSrb36gZpkh\myxdzDjfZRwdWW2comsJGVEPTB;MD6zN|XPxE1w MkPnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR5N{m1NVQoRjJ2N{e5OVE1RC:jPh?=
Ramos Mo\tSpVv[3Srb36gZZN{[Xl? MVzJcohq[mm2aX;uJI9nKFO7azDpckBidnSrIFnnUU1{fGmvdXzheIVlKGi3bXHuJHJidW:|IHPlcIx{KGG|c3Xzd4VlKGG|IFLMUmsheGixc4Doc5J6dGG2aX;uJIJ6KGOnbHz1cIFzKGG|c3H5MEBKSzVyPUCuOFU4|ryPLh?= NYrlV4h3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3NlY5ODZpPkK0O|I3QDB4PD;hQi=>
Rec1 NGG0eHJHfW6ldHnvckBie3OjeR?= NULYd2w4Oi53IIXN MlHvOkBpenN? MmnGTY5pcWKrdHnvckBw\iCEVFugdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIGLlZ|Eh[2WubIOgZZQhOi53IIXNJIlv[3WkYYTl[EBnd3JiNjDodpMh[nliV3XzeIVzdiCkbH;0eIlv\yCvZYToc4Q> M3q2[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkKyPFc4Lz5{NUKyNlg4PzxxYU6=
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Rec1 NWPIZZFETnWwY4Tpc44h[XO|YYm= NIHCboczNjVidV2= M4\FcVYhcHK| Mn;RTY5pcWKrdHnvckBw\iCOeX6gdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIGLlZ|Eh[2WubIOgZZQhOi53IIXNJIlv[3WkYYTl[EBnd3JiNjDodpMh[nliV3XzeIVzdiCkbH;0eIlv\yCvZYToc4Q> NYLHNmNGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNlI5PzdpPkK1NlIzQDd5PD;hQi=>
SJ-GBM2 MlO0dWhVWyCjc4PhfS=> MkKydWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOMLVfCUVIh[2WubIO= NYLGT3BbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
A673 MYDxTHRUKGG|c3H5 NYnUTlVXeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFG2O|Mh[2WubIO= M170PFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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NB-EBc1 NGfSXnhyUFSVIHHzd4F6 MmPSdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE6ELVXCZ|Eh[2WubIO= NXH2[4hCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Saos-2 NYjPXVhLeUiWUzDhd5NigQ>? MnLGdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOjb4OtNkBk\Wyucx?= NES4XJA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
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Rh41 MlrldWhVWyCjc4PhfS=> MnfCdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqNEGgZ4VtdHN? MkPSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Assay
Methods Test Index PMID
Western blot p-RPS6 / T-RPS6 / p-4E-BP1 / T-4E-BP1 ; p-MEK / T-MEK / p-ERK / T-ERK ; p-c-RAF / T-c-RAF ; p-AKT / T-AKT / p-mTOR / T-mTOR 23535559
Growth inhibition assay Cell viability (U87, U251 cells) ; Cell viability (GSC lines) 31043589
In vivo R406 reduces cutaneous reverse passive Arthus reaction by approximately 86% at 5 mg/kg in prophylactic treated mice. R406 also shows efficacy in inhibiting paw inflammation in antibody-induced arthritis mouse models. [1] R406 does not adversely affect macrophage or neutrophil function in innate immune responses and has minimal functional immunotoxicity notwithstanding its lymphocytopenic effect. [4]

Protocol (from reference)

Animal Research:[1]
  • Animal Models: Arthritis is induced in C57BL/6 mice by intraperitoneal injection of 150 μL of pooled sera from adult K/BxN mice.
  • Dosages: 1 or 5 mg/kg
  • Administration: Administered orally
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(159.07 mM)
Water Insoluble
Ethanol 0 mg/mL
(0.0 mM)

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5%dmso+95%cornoil
For best results, use promptly after mixing.

6mg/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 628.63
Formula

C22H23FN6O5.C6H6O3S

CAS No. 841290-81-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1(C(=O)NC2=C(O1)C=CC(=N2)NC3=NC(=NC=C3F)NC4=CC(=C(C(=C4)OC)OC)OC)C.C1=CC=C(C=C1)S(=O)(=O)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01725230 Completed Drug: Fostamatinib|Drug: Rosuvastatin|Drug: Simvastatin Rheumatoid Arthritis AstraZeneca November 2012 Phase 1
NCT01598571 Completed Drug: Fostamatinib Healthy AstraZeneca May 2012 Phase 1
NCT01387308 Completed Drug: Fostamatinib Healthy AstraZeneca August 2011 Phase 1
NCT01355354 Completed Drug: Digoxin|Drug: Fostamatinib Healthy Volunteers|Rheumatoid Arthritis AstraZeneca June 2011 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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

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Frequently Asked Questions

Question 1:
What’s the difference between S1533 and S2194?

Answer:
S1533 and S2194 are two different forms of R406. S1533 is the free base form, containing only R406 molecule without a acid added to it. S2194 has an additional C6H6O3S acid on it which makes the molecule a salt form. The free base and salt forms have same biology activities. Free base has a lower molecular weight and salt form has a better solubility in DMSO.

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