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 89 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 NWjsOlFoTnWwY4Tpc44hSXO|YYm= MkLjNUDPxE1? Ml\1N:KhcA>? Ml7rdoVlfWOnczDtbYdz[XSrb39CpC=> MoLGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ{NUG3OlEoRjJ4MkWxO|YyRC:jPh?=
U266 NWWxPHJFTnWwY4Tpc44hSXO|YYm= M{nrN|Eh|ryP M4rzcVPDqGh? NXnnT3AxemWmdXPld{BucWe{YYTpc47DqA>? MlvvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ{NUG3OlEoRjJ4MkWxO|YyRC:jPh?=
Jeko-1 NInZSllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDZRoZYPDhiaB?= M3;uemlEPTB;NT6wOlgzPiEQvF2= NGGz[o89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUizOVc2PSd-MkW4N|U4PTV:L3G+
Mino NUe4U2FsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojoOFghcA>? NWjLXnVbUUN3ME21MlcxQDV2IN88US=> NYn3VpdqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4N|U4PTVpPkK1PFM2PzV3PD;hQi=>
Jeko-1 Ml3uRZBweHSxc3nzJGF{e2G7 MV[1xsDPxE1? MojPNlQhcA>? MmCybY5lfWOnczCyOU4yyqEEsdMgN{4zyqBnIHHwc5B1d3Orcx?= MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh|NUe1OUc,OjV6M{W3OVU9N2F-
primary MCL M3rrRmFxd3C2b4Ppd{BCe3OjeR?= M2DoWFIhyrWP NX;Qc284OjRiaB?= MXXpcoNz\WG|ZYOgd4lodmmoaXPhcpRtgSCjcH;weI9{cXQEoB?= NXPZV41[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzPFg{PzNpPkK1N|g5Ozd|PD;hQi=>
PBMCs NWTOfWh[S2WubDDWbYFjcWyrdImgRZN{[Xl? NYq2fYd1OC13MDFOwG0> MmDnNlQhcA>? M3vjfmROW09? NGjxenlqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NGC5e2M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUGyO|g3Oid-MkWxNlc5PjJ:L3G+
PBMCs M1X3UWZ2dmO2aX;uJGF{e2G7 NGrXNYc2KM7:TR?= MoO2NUBp M4[yO2ROW09? Mmfm[IVkemWjc3XzJJRp\SClZXzsJI1q\3KjdHnvci=> M4Pv[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MUK3PFYzLz5{NUGyO|g3OjxxYU6=
CFSE-CD4+ T  NYDNdXBtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXUXXAxNjB4MkWtNUDPxE1? M3m3XFQh\A>? MWDicI9kc3NicILvcIln\XKjdHnvckBw\iCJVljEMYRmemm4ZXSgR2Q1M8LiVDDj[YxteyCjbnSgR2QyOWJtwrDj[Yxtew>? MnjNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4N{m5PFIoRjJ2Nke5PVgzRC:jPh?=
CFSE-CD11b+ MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\xZ|AvODZ{NT2xJO69VQ>? NHzzSnA5KGR? NHvpTYpjdG:la4OgdJJwdGmoZYLheIlwdiCxZjDHWmhFNWSncnn2[YQhS0R2K9MgWEBk\WyuczDhcoQhS0RzMXKrxsBk\Wyucx?= M3rFNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2Nke5PVgzLz5{NE[3PVk5OjxxYU6=
HMECs NH3uT5hHfW6ldHnvckBCe3OjeR?= MmrpNE0yOCEQvF2= NYfDcmRKOjBibXnu MVHpcohq[mm2czDWSWdHNXO2aX31cIF1\WRicnXs[YF{\SCxZjDOUy=> NYjEW3Z4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzNlk2PDRpPkK0N|I6PTR2PD;hQi=>
AB5 MUDBdI9xfG:|aYOgRZN{[Xl? M2Ky[VAuOi53IN88US=> MUK0PEBp MYTEUXNQ MUnpcoR2[2W|IHHwc5B1d3Orcx?= MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN7OEmxNUc,OjN|OUi5NVE9N2F-
JB7 NIfjUnBCeG:ydH;zbZMhSXO|YYm= MlO1NE0zNjVizszN NXfseZg5PDhiaB?= MlTsSG1UVw>? M4rFOolv\HWlZYOgZZBweHSxc3nz NH3FOo49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O5PFkyOSd-MkOzPVg6OTF:L3G+
AB5 M2H3dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3v0[VAuOi53IN88US=> MWm0PEBp MULEUXNQ M1jyOIlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= M{jmUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{m4PVEyLz5{M{O5PFkyOTxxYU6=
JB7 NWnH[5hVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jZNFAuOi53IN88US=> MYC0PEBp MkHKSG1UVw>? NGnzSI1qdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 MoDqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|OUi5NVEoRjJ|M{m4PVEyRC:jPh?=
RL MXTGeY5kfGmxbjDBd5NigQ>? NUXBZmZSOi53L{Wg{txO M2rLS|I1NzR6IHi= MljZSG1UVw>? MkP1bY5lfWOnczDhJJBwfGWwdDDk[YNz\WG|ZTDpckBOVVBvOTDtVm5CKGW6cILld5Nqd25? NH7abHA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUmyOlk3PSd-MkG5NlY6PjV:L3G+
RL MYjGeY5kfGmxbjDBd5NigQ>? NITudnMyNzJwNTFOwG0> NHPiTJgzPCCq M1PGWmROW09? MkDBdoVlfWOnczD0bIUh[WO2aY\heIlwdiCxZjDBb5Qh[W6mIIC3NHM3Uw>? MonDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF7Mk[5OlUoRjJzOUK2PVY2RC:jPh?=
platelet  NXzoZ5dnTnWwY4Tpc44hSXO|YYm= NX6xXot6OcLizszt M4XwclUhdWmw M{XzTIlvcGmkaYTzJGZk|rOUSVnBMY1m\GmjdHXkJJBt[XSnbHX0JIFo\3KnZ3H0bY9v M2Xl[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOES4Olk1Lz5{MUi0PFY6PDxxYU6=
platelet  NHn0WIJHfW6ldHnvckBCe3OjeR?= NGS2WnMxNjB3L{GvNk42KM7:TR?= M1nOT|UhdWmw MkTGbY5pcWKrdIOgeIhmKHOrZ37hcIlv\yCvZXPoZY5qe22|IHTve45{fHKnYX2gc4YhTmQQs2LJTWE> M{fn[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOES4Olk1Lz5{MUi0PFY6PDxxYU6=
DoHH2 NG\6TYNCeG:ydH;zbZMhSXO|YYm= M37abVAwOy9zMDFOwG0> MlHMOFghcA>? M37FRolv\HWlZYOgZ4VtdCCmZXH0bEB{cWewaX\pZ4FvfGy7 M4DYXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOEe1OFA5Lz5{MEi3OVQxQDxxYU6=
Jeko-1  MWDBdI9xfG:|aYOgRZN{[Xl? NYT3PXZPOC9|L{GwJO69VQ>? MYi0PEBp NEHOcpBqdmS3Y3XzJINmdGxiZHXheIghe2mpbnnmbYNidnSueR?= M{nvfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOEe1OFA5Lz5{MEi3OVQxQDxxYU6=
Raji  Mn\yRZBweHSxc3nzJGF{e2G7 NHrhVGoxNzNxMUCg{txO MorDOFghcA>? MY\pcoR2[2W|IHPlcIwh\GWjdHigd4lodmmoaXPhcpRtgQ>? MkXFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB6N{W0NFgoRjJyOEe1OFA5RC:jPh?=
DHL4 MnTzRZBweHSxc3nzJGF{e2G7 Ml73NE8yNzRizszN M{XlOlk3KGh? NUDPc2locW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> NYPwXZlMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUiwNFY3QTZpPkG4NFA3Pjl4PD;hQi=>
LY7 NVjD[5RrSXCxcITvd4l{KEG|c3H5 NGO5dVYxNzFxNDFOwG0> MnLMPVYhcA>? M{fKeYlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NWnaW2xZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUiwNFY3QTZpPkG4NFA3Pjl4PD;hQi=>
LY3 MmOwRZBweHSxc3nzJGF{e2G7 M1jLO|AwOS92IN88US=> Mm[5PVYhcA>? M2fUUYlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= M1vn[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6MEC2Olk3Lz5zOECwOlY6PjxxYU6=
DHL6 NXzsOYV4SXCxcITvd4l{KEG|c3H5 MVmwM|EwPCEQvF2= NF23OFU6PiCq NFzuV3VqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NX;xOZlrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUiwNFY3QTZpPkG4NFA3Pjl4PD;hQi=>
LY10 NF;DU3FCeG:ydH;zbZMhSXO|YYm= MoS0NE8yNzRizszN NX\WNWU2QTZiaB?= M4LEbYlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NW\NeWpHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUiwNFY3QTZpPkG4NFA3Pjl4PD;hQi=>
DHL10 MlHZRZBweHSxc3nzJGF{e2G7 M1[1WVAwOS92IN88US=> NIWyfIw6PiCq Mn\NbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= M3rBblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6MEC2Olk3Lz5zOECwOlY6PjxxYU6=
Wsu-NHL NFvqZ3pCeG:ydH;zbZMhSXO|YYm= NHLPdnQxNzFxNDFOwG0> NUTreFl2QTZiaB?= MkLKbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= NF3TOXE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOECwOlY6Pid-MUiwNFY3QTZ:L3G+
LY18 MWfBdI9xfG:|aYOgRZN{[Xl? NHX2dHkxNzFxNDFOwG0> NHzDUGo6PiCq NGe5UodqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDByNk[5Okc,OThyME[2PVY9N2F-
LY1 NXXhSo5lSXCxcITvd4l{KEG|c3H5 M4\MWFAwOS92IN88US=> M2KzNlk3KGh? NFjpXHlqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 MoXoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOThyME[2PVYoRjF6MEC2Olk3RC:jPh?=
DHL8 NUfjT2dFSXCxcITvd4l{KEG|c3H5 MVGwM|EwPCEQvF2= MXq5OkBp MlzmbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= M33TbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6MEC2Olk3Lz5zOECwOlY6PjxxYU6=
DHL4 MXjBdI9xfG:|aYOgRZN{[Xl? MXe0JO69VQ>? MknpPVYhcA>? MlTnbY5lfWOnczDjcIVifmGpZTDv[kBk[XOyYYPld{A6KGGwZDCzMEBjfXRibn;0JINie3Cjc3WgPC=> NVXDc3lLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUiwNFY3QTZpPkG4NFA3Pjl4PD;hQi=>
DHL6 M2m0OmFxd3C2b4Ppd{BCe3OjeR?= NGi0O3E1KM7:TR?= NWrKS|luQTZiaB?= NHvLdGlqdmS3Y3XzJINt\WG4YXflJI9nKGOjc4Dhd4V{KDliYX7kJFMtKGK3dDDuc5Qh[2G|cHHz[UA5 NH35TYo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOECwOlY6Pid-MUiwNFY3QTZ:L3G+
LY3 MWLBdI9xfG:|aYOgRZN{[Xl? NHHVV4c1KM7:TR?= MlrjPVYhcA>? MmDvbY5lfWOnczDjcIVifmGpZTDv[kBk[XOyYYPld{A6KGGwZDCzMEBjfXRibn;0JINie3Cjc3WgPC=> MojOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOThyME[2PVYoRjF6MEC2Olk3RC:jPh?=
LY7 NFLQeINCeG:ydH;zbZMhSXO|YYm= M1O3c|Qh|ryP MX:5OkBp NYTQe4FocW6mdXPld{BkdGWjdnHn[UBw\iClYYPwZZNmeyB7IHHu[EA{NCCkdYSgco91KGOjc4Dhd4UhQA>? NWm0OJV5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUiwNFY3QTZpPkG4NFA3Pjl4PD;hQi=>
DHL4 MUXGeY5kfGmxbjDBd5NigQ>? M3OwRlQh|ryP NYjVV5BXOTZiaB?= MonTbY5pcWKrdIOgeI9vcWNiQlzOT{B1gXKxc3nu[UBxcG:|cHjvdplt[XSrb36= NXXGU4c3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUiwNFY3QTZpPkG4NFA3Pjl4PD;hQi=>
LY7 NWC5VFdRTnWwY4Tpc44hSXO|YYm= M4K4bVQh|ryP MYOxOkBp M3nDSolvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u NYT2Z2tzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUiwNFY3QTZpPkG4NFA3Pjl4PD;hQi=>
LY3 NV7lSIRFTnWwY4Tpc44hSXO|YYm= MkTDOEDPxE1? M{fyWVE3KGh? NFP5VIRqdmirYnn0d{B1d26rYzDCUG5MKHS7cn;zbY5mKHCqb4PwbI9zgWyjdHnvci=> MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDByNk[5Okc,OThyME[2PVY9N2F-
DHL6 Mn3kSpVv[3Srb36gRZN{[Xl? MX[0JO69VQ>? Mn;4NVYhcA>? NV:yVZJGcW6qaXLpeJMhfG:waXOgRmxPUyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> NIi2ZoM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOECwOlY6Pid-MUiwNFY3QTZ:L3G+
LY10 NVn0THU5TnWwY4Tpc44hSXO|YYm= NVzxUldvPCEQvF2= NF\SVGYyPiCq MYTpcohq[mm2czD0c45q[yCETF7LJJR6em:|aX7lJJBpd3OyaH;yfYxifGmxbh?= MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDByNk[5Okc,OThyME[2PVY9N2F-
Wsu-NHL NULIUWRsTnWwY4Tpc44hSXO|YYm= M1;mSFQh|ryP NF3Yd4EyPiCq NYP3bpg6cW6qaXLpeJMhfG:waXOgRmxPUyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> NYe1UXR{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUiwNFY3QTZpPkG4NFA3Pjl4PD;hQi=>
LY18 NHzmPJJHfW6ldHnvckBCe3OjeR?= MkDFOEDPxE1? Mk\3NVYhcA>? NWnuU3VqcW6qaXLpeJMhfG:waXOgRmxPUyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> NWX3XY9bRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUiwNFY3QTZpPkG4NFA3Pjl4PD;hQi=>
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SK-N-SH M4q2OGZ2dmO2aX;uJIF{e2G7 M3;hWWlvcGmkaYTpc44hd2ZiUnX0JIlvKGi3bXHuJHNMNU5vU1igZ4VtdHNuIFXDOVA:OC5yON88UU4> NVPremsxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyOVczOTNpPkKyNlU4OjF|PD;hQi=>
mouse bone marrow cells M{DvVGZ2dmO2aX;uJIF{e2G7 MYXJcohq[mm2aX;uJI9nKEmOMzDk[ZBmdmSnboSgdJJwdGmoZYLheIlwdiCrbjDDOVcwSjF4IH3veZNmKGKxbnWgcYFzem:5IHPlcIx{KHW|aX7nJHs{UF22aIntbYRqdmViYomgcIlyfWmmIIPjbY51cWyuYYTpc44h[2:3boTpcoctKEmFNUC9NE4yPDgQvF2u MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd{NkiwOkc,OjR5Mk[4NFY9N2F-
B-cells NFjFOXdHfW6ldHnvckBie3OjeR?= MWOxJIhz MXPJcohq[mm2aX;uJI9nKFO7azDpckBidHCqYVnnUU1{fGmvdXzheIVlKGi3bXHuJGIh[2WubIOgZZN{\XO|ZXSgZZMh[2WubDDwdo9tcW[ncnH0bY9vKGGodHXyJFEhcHJiaX7jeYJifGmxbjDifUBndG:5IHP5eI9u\XS{eTygSWM2OD1yLkG1Ne69VS5? Mn;KQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR5N{m1NVQoRjJ2N{e5OVE1RC:jPh?=
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B-cells Mnv5SpVv[3Srb36gZZN{[Xl? MV2xJIhz MYrJcohq[mm2aX;uJI9nKFO7azDpckBidHCqYVnnUU1{fGmvdXzheIVlKGi3bXHuJGIh[2WubIOgZZN{\XO|ZXSgZZMhS0R6NjDlfJBz\XO|aX;uJIFnfGW{IEGgbJIhcW6ldXLheIlwdiCkeTDmcI94KGO7dH;t[ZRzgSxiRVO1NF0xNjN|Nd88UU4> NEPUPII9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEe3PVUyPCd-MkS3O|k2OTR:L3G+
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Rec1 MULGeY5kfGmxbjDhd5NigQ>? M4Phd|IvPSC3TR?= NGLjdIE3KGi{cx?= MkP3TY5pcWKrdHnvckBw\iCEVFugdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIGLlZ|Eh[2WubIOgZZQhOi53IIXNJIlv[3WkYYTl[EBnd3JiNjDodpMh[nliV3XzeIVzdiCkbH;0eIlv\yCvZYToc4Q> MnjWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{MkK4O|coRjJ3MkKyPFc4RC:jPh?=
Rec1 NVfYZ20yTnWwY4Tpc44h[XO|YYm= MVqyMlUhfU1? NEjjbZM3KGi{cx?= Mn;BTY5pcWKrdHnvckBw\iCVeXugdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIGLlZ|Eh[2WubIOgZZQhOi53IIXNJIlv[3WkYYTl[EBnd3JiNjDodpMh[nliV3XzeIVzdiCkbH;0eIlv\yCvZYToc4Q> MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ{Mki3O{c,OjV{MkK4O|c9N2F-
Rec1 NHXt[odHfW6ldHnvckBie3OjeR?= M3X0R|IvPSC3TR?= MorNOkBpenN? M37XS2lvcGmkaYTpc44hd2ZiTInuJJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDS[YMyKGOnbHzzJIF1KDJwNTD1UUBqdmO3YnH0[YQh\m:{IE[gbJJ{KGK7IGfld5Rmem5iYnzveJRqdmdibXX0bI9l M{jrUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkKyPFc4Lz5{NUKyNlg4PzxxYU6=
SJ-GBM2 NEPpVZpyUFSVIHHzd4F6 MYPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0pvR1LNNkBk\Wyucx?= MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
A673 M13nfJFJXFNiYYPzZZk> NX3PVoxGeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFG2O|Mh[2WubIO= MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-MC NHrlR5RyUFSVIHHzd4F6 Mm\adWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO= NHPDVW89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
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Saos-2 NFvudYZyUFSVIHHzd4F6 MmTpdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOjb4OtNkBk\Wyucx?= Mn63QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
OHS-50 NXvUPJRWeUiWUzDhd5NigQ>? NIPDSm1yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiT1jTMVUxKGOnbHzz M1zldlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh41 NGPDS2NyUFSVIHHzd4F6 NVHYR3BJeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLoOFEh[2WubIO= M1jGclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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

Solubility (25°C)

In vitro

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

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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