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.

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In DMSO USD 286 In stock
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Cited by 32 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. 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 MoHQSpVv[3Srb36gRZN{[Xl? MmDtNUDPxE1? NFToUlc{yqCq NIXHRm1z\WS3Y3XzJI1q\3KjdHnvcuKh MnLTNlYzPTF5NkG=
U266 NHHGPFhHfW6ldHnvckBCe3OjeR?= NVK0NHNNOSEQvF2= NV3RSYV6O8LiaB?= NUKx[|Y{emWmdXPld{BucWe{YYTpc47DqA>? M2nMWlI3OjVzN{[x
Jeko-1 NUPMTpJoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnhZ4c1QCCq NF3XVWpKSzVyPUWuNFY5OjZizszN MWWyOVg{PTd3NR?=
Mino NV\JUpJPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYT0XGp[PDhiaB?= M4PiXmlEPTB;NT63NFg2PCEQvF2= M3fQRVI2QDN3N{W1
Jeko-1 MnPkRZBweHSxc3nzJGF{e2G7 NUn6VYxGPcLizszN NEjiR3czPCCq NWjKeJYxcW6mdXPld{AzPS5zwrFCteKhOy5{wrClJIFxd3C2b4Ppdy=> NWLMOXFWOjV6M{W3OVU>
primary MCL Moj2RZBweHSxc3nzJGF{e2G7 MlvGNkDDvU1? NYTafHRrOjRiaB?= M3LjOolv[3KnYYPld{B{cWewaX\pZ4FvfGy7IHHwc5B1d3Orc9Mg NUHjOWNIOjV|OEizO|M>
PBMCs NHXlPXBE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NFq2ZoMxNTVyIN88US=> MXSyOEBp MmHZSG1UVw>? M3;4TIlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NH[4TGUzPTF{N{i2Ni=>
PBMCs MnfJSpVv[3Srb36gRZN{[Xl? M17jb|Uh|ryP NIC4PFUyKGh? MkXvSG1UVw>? Moiz[IVkemWjc3XzJJRp\SClZXzsJI1q\3KjdHnvci=> MlXHNlUyOjd6NkK=
CFSE-CD4+ T  NUPGVGdXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXiybpI1OC5yNkK1MVEh|ryP NYrseGNOPCCm MnHwZoxw[2u|IIDyc4xq\mW{YYTpc44hd2ZiR2\ISE1l\XKrdnXkJGNFPCwEoGSgZ4VtdHNiYX7kJGNFOTGkK9MgZ4VtdHN? M1[xbVI1Pjd7OUiy
CFSE-CD11b+ NVTrPXlOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MViwMlA3OjVvMTFOwG0> NVv3UYhVQCCm NH61TnFjdG:la4OgdJJwdGmoZYLheIlwdiCxZjDHWmhFNWSncnn2[YQhS0R2K9MgWEBk\WyuczDhcoQhS0RzMXKrxsBk\Wyucx?= M2L2d|I1Pjd7OUiy
HMECs MnrpSpVv[3Srb36gRZN{[Xl? NUTtZWlqOC1zMDFOwG0> NWfJZ2tZOjBibXnu NYPMWY5tcW6qaXLpeJMhXkWJRj3zeIlufWyjdHXkJJJmdGWjc3Wgc4YhVk9? NH22dVIzPDN{OUW0OC=>
AB5 NXrmdIlXSXCxcITvd4l{KEG|c3H5 MlzSNE0zNjVizszN M2rOdFQ5KGh? NYXkNm01TE2VTx?= NV:xcppWcW6mdXPld{BieG:ydH;zbZM> NUj1SnZTOjN|OUi5NVE>
JB7 M1vxdGFxd3C2b4Ppd{BCe3OjeR?= MX6wMVIvPSEQvF2= MWK0PEBp MoLkSG1UVw>? NUnDW2JFcW6mdXPld{BieG:ydH;zbZM> MYqyN|M6QDlzMR?=
AB5 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3K5UFAuOi53IN88US=> M{T1W|Q5KGh? M2fyPWROW09? MlrNbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= NF\QcpEzOzN7OEmxNS=>
JB7 MkD5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLENE0zNjVizszN NUDXWIxyPDhiaB?= Mlu5SG1UVw>? MYTpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 NGDqR2gzOzN7OEmxNS=>
RL NFO4bXBHfW6ldHnvckBCe3OjeR?= NWLWO|lTOi53L{Wg{txO NXn3O25TOjRxNEigbC=> M4fL[2ROW09? MmXubY5lfWOnczDhJJBwfGWwdDDk[YNz\WG|ZTDpckBOVVBvOTDtVm5CKGW6cILld5Nqd25? M3\sZVIyQTJ4OU[1
RL MVHGeY5kfGmxbjDBd5NigQ>? Ml3qNU8zNjVizszN MknrNlQhcA>? NH\Oe2lFVVOR MUfy[YR2[2W|IITo[UBi[3SrdnH0bY9vKG:oIFHreEBidmRicEewV|ZM MV2yNVkzPjl4NR?=
platelet  M37tdGZ2dmO2aX;uJGF{e2G7 Mkf1NeKh|ryv NYfuZWVlPSCvaX6= NFLTeIJqdmirYnn0d{BH[87|UlnJRU1u\WSrYYTl[EBxdGG2ZXzleEBi\2e{ZXfheIlwdg>? NUi2U4hCOjF6NEi2PVQ>
platelet  NHrvUXlHfW6ldHnvckBCe3OjeR?= NV:xc3BSOC5yNT:xM|IvPSEQvF2= M1\FcFUhdWmw MmjxbY5pcWKrdIOgeIhmKHOrZ37hcIlv\yCvZXPoZY5qe22|IHTve45{fHKnYX2gc4YhTmQQs2LJTWE> MlLHNlE5PDh4OUS=
DoHH2 MmX4RZBweHSxc3nzJGF{e2G7 NXPjfVJsOC9|L{GwJO69VQ>? M2DIUFQ5KGh? NFy0epdqdmS3Y3XzJINmdGxiZHXheIghe2mpbnnmbYNidnSueR?= M3jUV|IxQDd3NEC4
Jeko-1  M4PwUmFxd3C2b4Ppd{BCe3OjeR?= NYLZUGM1OC9|L{GwJO69VQ>? NHK1bHU1QCCq MU\pcoR2[2W|IHPlcIwh\GWjdHigd4lodmmoaXPhcpRtgQ>? NIqyW|QzODh5NUSwPC=>
Raji  M4G4cWFxd3C2b4Ppd{BCe3OjeR?= NF\WSW4xNzNxMUCg{txO NVjw[ox1PDhiaB?= NHrG[YpqdmS3Y3XzJINmdGxiZHXheIghe2mpbnnmbYNidnSueR?= MYOyNFg4PTRyOB?=
DHL4 NYDvZYtQSXCxcITvd4l{KEG|c3H5 NF;2XnUxNzFxNDFOwG0> MlvzPVYhcA>? NF3ESXNqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 M4TvRVE5ODB4Nkm2
LY7 NWDWUW1MSXCxcITvd4l{KEG|c3H5 M3H2WVAwOS92IN88US=> NY\RdphDQTZiaB?= M4rGSIlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= MmPpNVgxODZ4OU[=
LY3 NWX3WXRJSXCxcITvd4l{KEG|c3H5 M2fneVAwOS92IN88US=> M4f5RVk3KGh? M{[wXIlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= MmDRNVgxODZ4OU[=
DHL6 NInSbmpCeG:ydH;zbZMhSXO|YYm= MoGyNE8yNzRizszN MUG5OkBp M1HMTYlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NH;PVIUyQDByNk[5Oi=>
LY10 MYrBdI9xfG:|aYOgRZN{[Xl? NIfMbW4xNzFxNDFOwG0> MYm5OkBp M4j0[Ylv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NWrpZ45bOThyME[2PVY>
DHL10 MUjBdI9xfG:|aYOgRZN{[Xl? MUmwM|EwPCEQvF2= NWDyRnFzQTZiaB?= MnvhbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= M2TudFE5ODB4Nkm2
Wsu-NHL NUW5WVg2SXCxcITvd4l{KEG|c3H5 NF3PNZYxNzFxNDFOwG0> NVq0c45ZQTZiaB?= NXTKV2t1cW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> MVuxPFAxPjZ7Nh?=
LY18 Ml;qRZBweHSxc3nzJGF{e2G7 MU[wM|EwPCEQvF2= NWDTZplLQTZiaB?= MlPWbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= NGrLN|cyQDByNk[5Oi=>
LY1 MnL0RZBweHSxc3nzJGF{e2G7 M1T1bFAwOS92IN88US=> M37leVk3KGh? NGHr[FFqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 M{TycVE5ODB4Nkm2
DHL8 MnTaRZBweHSxc3nzJGF{e2G7 M4LlOVAwOS92IN88US=> NI\5UFY6PiCq NFnvUVFqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NV7XOZFYOThyME[2PVY>
DHL4 MonGRZBweHSxc3nzJGF{e2G7 MXe0JO69VQ>? NF3seZk6PiCq MUHpcoR2[2W|IHPs[YF3[WenIH;mJINie3Cjc3XzJFkh[W6mIEOsJIJ2fCCwb4SgZ4F{eGG|ZTC4 MX2xPFAxPjZ7Nh?=
DHL6 NHezfmtCeG:ydH;zbZMhSXO|YYm= MmTvOEDPxE1? NVf2coVTQTZiaB?= M2LVc4lv\HWlZYOgZ4xm[X[jZ3Wgc4Yh[2G|cHHz[ZMhQSCjbnSgN{wh[nW2IH7veEBk[XOyYYPlJFg> MV2xPFAxPjZ7Nh?=
LY3 NYnSTXpZSXCxcITvd4l{KEG|c3H5 NY\NOFdbPCEQvF2= MWm5OkBp M1e2VYlv\HWlZYOgZ4xm[X[jZ3Wgc4Yh[2G|cHHz[ZMhQSCjbnSgN{wh[nW2IH7veEBk[XOyYYPlJFg> NIXYNYYyQDByNk[5Oi=>
LY7 NVzTTGNbSXCxcITvd4l{KEG|c3H5 NI\JTGg1KM7:TR?= NVjZO3pVQTZiaB?= M4rQbolv\HWlZYOgZ4xm[X[jZ3Wgc4Yh[2G|cHHz[ZMhQSCjbnSgN{wh[nW2IH7veEBk[XOyYYPlJFg> NGLZUVUyQDByNk[5Oi=>
DHL4 NFjGUlZHfW6ldHnvckBCe3OjeR?= Mmf5OEDPxE1? M3PpflE3KGh? MW\pcohq[mm2czD0c45q[yCETF7LJJR6em:|aX7lJJBpd3OyaH;yfYxifGmxbh?= NFTGfnMyQDByNk[5Oi=>
LY7 MXXGeY5kfGmxbjDBd5NigQ>? M{nibFQh|ryP MX:xOkBp M4fwOolvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u M1XvXFE5ODB4Nkm2
LY3 NF3H[VBHfW6ldHnvckBCe3OjeR?= MXS0JO69VQ>? MYqxOkBp NXrDNGc4cW6qaXLpeJMhfG:waXOgRmxPUyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> NGezXHYyQDByNk[5Oi=>
DHL6 MmnBSpVv[3Srb36gRZN{[Xl? M{XNblQh|ryP MmXlNVYhcA>? M1r4folvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u M4ntbFE5ODB4Nkm2
LY10 M2rPO2Z2dmO2aX;uJGF{e2G7 MmHMOEDPxE1? NYPOTnlHOTZiaB?= MWTpcohq[mm2czD0c45q[yCETF7LJJR6em:|aX7lJJBpd3OyaH;yfYxifGmxbh?= M1rJT|E5ODB4Nkm2
Wsu-NHL M3vPVmZ2dmO2aX;uJGF{e2G7 MYm0JO69VQ>? NUK3NWpxOTZiaB?= Mor3bY5pcWKrdIOgeI9vcWNiQlzOT{B1gXKxc3nu[UBxcG:|cHjvdplt[XSrb36= NXq4SII6OThyME[2PVY>
LY18 M2nZVWZ2dmO2aX;uJGF{e2G7 Ml7rOEDPxE1? M1zlb|E3KGh? MmLybY5pcWKrdIOgeI9vcWNiQlzOT{B1gXKxc3nu[UBxcG:|cHjvdplt[XSrb36= M4fw[FE5ODB4Nkm2

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-RPS6 / T-RPS6 / p-4E-BP1 / T-4E-BP1; 

PubMed: 23535559     


Four AML cell lines (a and b) were treated for 24 hours with vehicle versus R406. Western blots of (a) p-RPS6 (Ser240/244) and (b) p-4E-BP1 (Thr37/46).

p-MEK / T-MEK / p-ERK / T-ERK; 

PubMed: 23535559     


AML cell lines were treated with vehicle versus R406. Western blots of p-MEK1/2 (Ser217/221) and p-ERK1/2 (Thr202/Tyr204) are depicted. 

p-c-RAF / T-c-RAF; 

PubMed: 23535559     


Effect of SYK inhibition on c-RAF in AML cells. AML cells were grown in the presence of 4 μM R406 for the indicated times and assessed for activation of c-RAF and ERK1/2.

p-AKT / T-AKT / p-mTOR / T-mTOR; 

PubMed: 23535559     


Western blot of (a) p-AKT (Ser473) or (b) p-mTOR (Ser2448) in AML cell lines treated with R406 for 24 hours.

23535559
Growth inhibition assay
Cell viability (U87, U251 cells); 

PubMed: 31043589     


U87 and U251 were insensitive to R406, with a calculated IC50 of more than 1 mM for both cell lines.

Cell viability (GSC lines); 

PubMed: 31043589     


Incubation with R406 significantly reduced the cell viability of both GSC lines, with an IC50 of 0.75 μM for GSC-1 and 0.89 μM for GSC-2 respectively. 

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

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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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

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID