R406

Catalog No.S2194

R406 Chemical Structure

Molecular Weight(MW): 628.63

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. Phase 1.

Size Price Stock Quantity  
In DMSO USD 286 In stock
USD 120 In stock
USD 170 In stock
USD 270 In stock
USD 870 In stock
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Cited by 30 Publications

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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. 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 Mkf6SpVv[3Srb36gRZN{[Xl? MYexJO69VQ>? MYmzxsBp NH7mN2Rz\WS3Y3XzJI1q\3KjdHnvcuKh M4LnOVI3OjVzN{[x
U266 MmHtSpVv[3Srb36gRZN{[Xl? NF7Tc4QyKM7:TR?= M3vZc|PDqGh? MnrjdoVlfWOnczDtbYdz[XSrb39CpC=> M{jZT|I3OjVzN{[x
Jeko-1 NYjJN4Z6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mkn2OFghcA>? MVzJR|UxRTVwME[4NlYh|ryP MYGyOVg{PTd3NR?=
Mino Ml:3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;xSVQ5KGh? Ml3XTWM2OD13LkewPFU1KM7:TR?= MVSyOVg{PTd3NR?=
Jeko-1 M3nBd2Fxd3C2b4Ppd{BCe3OjeR?= NYHTUnRvPcLizszN NVfFXpFPOjRiaB?= M1PZR4lv\HWlZYOgNlUvOcLiwsJCpFMvOsLiJTDhdI9xfG:|aYO= MYmyOVg{PTd3NR?=
primary MCL NFnq[GRCeG:ydH;zbZMhSXO|YYm= M3uzeVIhyrWP NV7obJFIOjRiaB?= MmrwbY5kemWjc3XzJJNq\26rZnnjZY51dHliYYDvdJRwe2m|wrC= MlTRNlU{QDh|N{O=
PBMCs NX3Y[mhtS2WubDDWbYFjcWyrdImgRZN{[Xl? NYTkUo4yOC13MDFOwG0> NEXwW|QzPCCq MYrEUXNQ NWXXT3h3cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MVWyOVEzPzh4Mh?=
PBMCs NXnUSpY4TnWwY4Tpc44hSXO|YYm= MYi1JO69VQ>? NHzENoMyKGh? NV;oZ3NWTE2VTx?= MULk[YNz\WG|ZYOgeIhmKGOnbHygcYloemG2aX;u MVuyOVEzPzh4Mh?=
CFSE-CD4+ T  MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHXNE4xPjJ3LUGg{txO MVi0JIQ> NInCTWFjdG:la4OgdJJwdGmoZYLheIlwdiCxZjDHWmhFNWSncnn2[YQhS0R2K9MgWEBk\WyuczDhcoQhS0RzMXKrxsBk\Wyucx?= Mo\JNlQ3Pzl7OEK=
CFSE-CD11b+ M{PwdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2L5bVAvODZ{NT2xJO69VQ>? MmTuPEBl M3v2UIJtd2OtczDwdo9tcW[ncnH0bY9vKG:oIFfWTGQu\GW{aY\l[EBETDRtwrDUJINmdGy|IHHu[EBETDFzYjxCpINmdGy| M13VcVI1Pjd7OUiy
HMECs NE\2WG1HfW6ldHnvckBCe3OjeR?= MWqwMVExKM7:TR?= NH\WR3ozOCCvaX6= M{C0WolvcGmkaYTzJHZGT0Zvc4TpcZVt[XSnZDDy[Yxm[XOnIH;mJG5Q M{juW|I1OzJ7NUS0
AB5 NHXofY1CeG:ydH;zbZMhSXO|YYm= MlnmNE0zNjVizszN NUnWUmU1PDhiaB?= MWLEUXNQ NFOwS3BqdmS3Y3XzJIFxd3C2b4Ppdy=> MWGyN|M6QDlzMR?=
JB7 M3rsT2Fxd3C2b4Ppd{BCe3OjeR?= NHTWfYMxNTJwNTFOwG0> M2mze|Q5KGh? NFrhZYVFVVOR MmPWbY5lfWOnczDhdI9xfG:|aYO= MnzzNlM{QTh7MUG=
AB5 M3r3c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXKwMVIvPSEQvF2= MoXQOFghcA>? MWPEUXNQ MU\pcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 Mkf0NlM{QTh7MUG=
JB7 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml7zNE0zNjVizszN NGjYXFU1QCCq MXTEUXNQ NFjBVXFqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 MUGyN|M6QDlzMR?=
RL M4\afmZ2dmO2aX;uJGF{e2G7 M4fXelIvPS93IN88US=> MnfNNlQwPDhiaB?= M4DndGROW09? M2TlbYlv\HWlZYOgZUBxd3SnboSg[IVkemWjc3WgbY4hVU2SLUmgcXJPSSCneIDy[ZN{cW:w NFfaZnUzOTl{Nkm2OS=>
RL NGPoUnNHfW6ldHnvckBCe3OjeR?= NIPqXFkyNzJwNTFOwG0> M4Lzb|I1KGh? M3vTTGROW09? NWnNR|YyemWmdXPld{B1cGViYXP0bZZifGmxbjDv[kBCc3RiYX7kJJA4OFN4Sx?= M2LHU|IyQTJ4OU[1
platelet  MYnGeY5kfGmxbjDBd5NigQ>? MVWxxsDPxG1? M3HXXlUhdWmw MX\pcohq[mm2czDGZ:6{WkmLQT3t[YRq[XSnZDDwcIF1\WyndDDh[4dz\WejdHnvci=> NYDxcVY4OjF6NEi2PVQ>
platelet  NEfUUJZHfW6ldHnvckBCe3OjeR?= NF6wfmExNjB3L{GvNk42KM7:TR?= MX[1JI1qdg>? MnSybY5pcWKrdIOgeIhmKHOrZ37hcIlv\yCvZXPoZY5qe22|IHTve45{fHKnYX2gc4YhTmQQs2LJTWE> MWSyNVg1QDZ7NB?=
DoHH2 M3;mPGFxd3C2b4Ppd{BCe3OjeR?= MlviNE8{NzFyIN88US=> M3;DSVQ5KGh? M4jGWYlv\HWlZYOgZ4VtdCCmZXH0bEB{cWewaX\pZ4FvfGy7 NWfNWWdlOjB6N{W0NFg>
Jeko-1  M{nubGFxd3C2b4Ppd{BCe3OjeR?= M3;wSFAwOy9zMDFOwG0> MljEOFghcA>? NV7QZWRncW6mdXPld{Bk\WyuIHTlZZRpKHOrZ37p[olk[W62bIm= NGO1fW0zODh5NUSwPC=>
Raji  Mnu2RZBweHSxc3nzJGF{e2G7 NHXjcJcxNzNxMUCg{txO MVu0PEBp M{TUPYlv\HWlZYOgZ4VtdCCmZXH0bEB{cWewaX\pZ4FvfGy7 MmPUNlA5PzV2MEi=
DHL4 M3;tUGFxd3C2b4Ppd{BCe3OjeR?= MnLaNE8yNzRizszN MUS5OkBp Mn31bY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= MmXpNVgxODZ4OU[=
LY7 NX;vOZBySXCxcITvd4l{KEG|c3H5 NFjBSXExNzFxNDFOwG0> M4DoTVk3KGh? M4j1R4lv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= M3rRfFE5ODB4Nkm2
LY3 M1nHXmFxd3C2b4Ppd{BCe3OjeR?= M4fXV|AwOS92IN88US=> MUe5OkBp M1X5SYlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= M{\KWlE5ODB4Nkm2
DHL6 NFPEWFFCeG:ydH;zbZMhSXO|YYm= MnnUNE8yNzRizszN M1LXOFk3KGh? NV\pSVZ6cW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> NUfJdm9mOThyME[2PVY>
LY10 NXvTOIlFSXCxcITvd4l{KEG|c3H5 NITIcZExNzFxNDFOwG0> NX;VeWV6QTZiaB?= M2nGb4lv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NELGdlgyQDByNk[5Oi=>
DHL10 Mlj4RZBweHSxc3nzJGF{e2G7 MYmwM|EwPCEQvF2= MYe5OkBp MX;pcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MkjGNVgxODZ4OU[=
Wsu-NHL NYfhXnpoSXCxcITvd4l{KEG|c3H5 M3;BRlAwOS92IN88US=> M3TVZlk3KGh? MXnpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NX\4fYpEOThyME[2PVY>
LY18 M1XTVGFxd3C2b4Ppd{BCe3OjeR?= MlfsNE8yNzRizszN NFXKelU6PiCq MV7pcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NYTuO|dpOThyME[2PVY>
LY1 MXLBdI9xfG:|aYOgRZN{[Xl? NXKxcmhEOC9zL{Sg{txO NV60O41DQTZiaB?= NETzc2lqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 MWexPFAxPjZ7Nh?=
DHL8 MYfBdI9xfG:|aYOgRZN{[Xl? M2rXOFAwOS92IN88US=> M3H6RVk3KGh? MnH6bY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= MoS3NVgxODZ4OU[=
DHL4 Mo[yRZBweHSxc3nzJGF{e2G7 M2DHU|Qh|ryP M1HySlk3KGh? M4TXeYlv\HWlZYOgZ4xm[X[jZ3Wgc4Yh[2G|cHHz[ZMhQSCjbnSgN{wh[nW2IH7veEBk[XOyYYPlJFg> MnzrNVgxODZ4OU[=
DHL6 NVnIbZVUSXCxcITvd4l{KEG|c3H5 NIDic4I1KM7:TR?= MVe5OkBp NX\3TIx[cW6mdXPld{BkdGWjdnHn[UBw\iClYYPwZZNmeyB7IHHu[EA{NCCkdYSgco91KGOjc4Dhd4UhQA>? NFjxUGkyQDByNk[5Oi=>
LY3 MkjURZBweHSxc3nzJGF{e2G7 MmjPOEDPxE1? M1:zV|k3KGh? M4jT[4lv\HWlZYOgZ4xm[X[jZ3Wgc4Yh[2G|cHHz[ZMhQSCjbnSgN{wh[nW2IH7veEBk[XOyYYPlJFg> M3fPSlE5ODB4Nkm2
LY7 Mn62RZBweHSxc3nzJGF{e2G7 NWLoO|F3PCEQvF2= NXzhVmlMQTZiaB?= NYS0RZFCcW6mdXPld{BkdGWjdnHn[UBw\iClYYPwZZNmeyB7IHHu[EA{NCCkdYSgco91KGOjc4Dhd4UhQA>? MVqxPFAxPjZ7Nh?=
DHL4 M1fkTWZ2dmO2aX;uJGF{e2G7 NFr5RZI1KM7:TR?= NF;DOlUyPiCq NV;TVYZicW6qaXLpeJMhfG:waXOgRmxPUyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> NXr1VnZvOThyME[2PVY>
LY7 Ml3ISpVv[3Srb36gRZN{[Xl? NI\yZYk1KM7:TR?= MYKxOkBp M3zxXolvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u NXixXop1OThyME[2PVY>
LY3 M3XnZ2Z2dmO2aX;uJGF{e2G7 MXS0JO69VQ>? NHLDbocyPiCq M3niZ4lvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u M3rPWFE5ODB4Nkm2
DHL6 M4XX[mZ2dmO2aX;uJGF{e2G7 M{D3bFQh|ryP MVuxOkBp MlzmbY5pcWKrdIOgeI9vcWNiQlzOT{B1gXKxc3nu[UBxcG:|cHjvdplt[XSrb36= MkPnNVgxODZ4OU[=
LY10 MXTGeY5kfGmxbjDBd5NigQ>? MmfoOEDPxE1? MXWxOkBp NXLaSWlicW6qaXLpeJMhfG:waXOgRmxPUyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> NGPReJgyQDByNk[5Oi=>
Wsu-NHL Mm\wSpVv[3Srb36gRZN{[Xl? NFzOVlc1KM7:TR?= NF:5RlcyPiCq M{ThU4lvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u NFTyZYgyQDByNk[5Oi=>
LY18 M3XFRmZ2dmO2aX;uJGF{e2G7 NUexS5dwPCEQvF2= NXf5R|QzOTZiaB?= Mlu0bY5pcWKrdIOgeI9vcWNiQlzOT{B1gXKxc3nu[UBxcG:|cHjvdplt[XSrb36= MVGxPFAxPjZ7Nh?=

... Click to View More Cell Line Experimental Data

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

Animal Research:[1]
+ Expand
  • Animal Models: Arthritis is induced in C57BL/6 mice by intraperitoneal injection of 150 μL of pooled sera from adult K/BxN mice.
  • Formulation: 35% TPGS, 60% PEG 400, and 5% propylene glycol
  • 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 powder
in solvent
Synonyms N/A

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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.

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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.

Syk Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID