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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USD 170 In stock
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Cited by 36 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 MX\GeY5kfGmxbjDBd5NigQ>? MYqxJO69VQ>? NG\CfZQ{yqCq M3HRZ5Jm\HWlZYOgcYloemG2aX;uxsA> MVSyOlI2OTd4MR?=
U266 MlrESpVv[3Srb36gRZN{[Xl? MljjNUDPxE1? M{XWWFPDqGh? M3eyc5Jm\HWlZYOgcYloemG2aX;uxsA> NYDJeZF3OjZ{NUG3OlE>
Jeko-1 MonnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XyNVQ5KGh? NF;1N3NKSzVyPUWuNFY5OjZizszN MXeyOVg{PTd3NR?=
Mino M3nROWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnifVRMPDhiaB?= M3LmSWlEPTB;NT63NFg2PCEQvF2= M{TKNFI2QDN3N{W1
Jeko-1 NVnmTJI6SXCxcITvd4l{KEG|c3H5 NEC0b3U2yqEQvF2= MXeyOEBp NHPsVo5qdmS3Y3XzJFI2NjIEoNMxxsA{NjMEoDWgZZBweHSxc3nz MYOyOVg{PTd3NR?=
primary MCL NHe2TVFCeG:ydH;zbZMhSXO|YYm= NHTvb|AzKML3TR?= M1\5[FI1KGh? Ml;ibY5kemWjc3XzJJNq\26rZnnjZY51dHliYYDvdJRwe2m|wrC= Mm\qNlU{QDh|N{O=
PBMCs MoPMR4VtdCCYaXHibYxqfHliQYPzZZk> M1PxS|AuPTBizszN MnXMNlQhcA>? NGHEeYRFVVOR NEnrS|FqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MoTVNlUyOjd6NkK=
PBMCs NH;meFJHfW6ldHnvckBCe3OjeR?= MoXkOUDPxE1? M1;URVEhcA>? NVXBV3VRTE2VTx?= MV7k[YNz\WG|ZYOgeIhmKGOnbHygcYloemG2aX;u MUeyOVEzPzh4Mh?=
CFSE-CD4+ T  NVrEUIZWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vJN|AvODZ{NT2xJO69VQ>? NIHPeXg1KGR? NXnTTmVP[myxY3vzJJBzd2yrZnXyZZRqd25ib3[gS3ZJTC2mZYLpeoVlKEOGNDxCpHQh[2WubIOgZY5lKEOGMUHiL:Kh[2WubIO= NHfTOpAzPDZ5OUm4Ni=>
CFSE-CD11b+ MmjVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTIZ3NkOC5yNkK1MVEh|ryP MV:4JIQ> MUnicI9kc3NicILvcIln\XKjdHnvckBw\iCJVljEMYRmemm4ZXSgR2Q1M8LiVDDj[YxteyCjbnSgR2QyOWJtwrDj[Yxtew>? MX[yOFY4QTl6Mh?=
HMECs MnrFSpVv[3Srb36gRZN{[Xl? MW[wMVExKM7:TR?= MnflNlAhdWmw M37sVIlvcGmkaYTzJHZGT0Zvc4TpcZVt[XSnZDDy[Yxm[XOnIH;mJG5Q MmS5NlQ{Ojl3NES=
AB5 NFT3ZmhCeG:ydH;zbZMhSXO|YYm= NWLqbpJqOC1{LkWg{txO MV:0PEBp MmOxSG1UVw>? MkD2bY5lfWOnczDhdI9xfG:|aYO= M1jad|I{Ozl6OUGx
JB7 MlT5RZBweHSxc3nzJGF{e2G7 NHLWPXgxNTJwNTFOwG0> MlHDOFghcA>? NVWwN5BoTE2VTx?= MkXBbY5lfWOnczDhdI9xfG:|aYO= NXPtV3lnOjN|OUi5NVE>
AB5 NEDzZYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\wNE0zNjVizszN M3XGOlQ5KGh? NVXiToRJTE2VTx?= MWTpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 MnrFNlM{QTh7MUG=
JB7 Mme5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jPSVAuOi53IN88US=> NFjyTlE1QCCq M{LwOmROW09? M1PxPIlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= M2P4ZlI{Ozl6OUGx
RL NGTCUpNHfW6ldHnvckBCe3OjeR?= M36xWlIvPS93IN88US=> NWTa[oJbOjRxNEigbC=> NXvVZYpxTE2VTx?= M2XteYlv\HWlZYOgZUBxd3SnboSg[IVkemWjc3WgbY4hVU2SLUmgcXJPSSCneIDy[ZN{cW:w NFjuUYYzOTl{Nkm2OS=>
RL NIHIdlVHfW6ldHnvckBCe3OjeR?= M3PVcFEwOi53IN88US=> MV[yOEBp NFHyfJBFVVOR M{XUNZJm\HWlZYOgeIhmKGGldHn2ZZRqd25ib3[gRYt1KGGwZDDwO|BUPkt? NVT5VXR4OjF7Mk[5OlU>
platelet  M4j2e2Z2dmO2aX;uJGF{e2G7 NG\VfW0yyqEQvH2= NXjqe|V7PSCvaX6= MV7pcohq[mm2czDGZ:6{WkmLQT3t[YRq[XSnZDDwcIF1\WyndDDh[4dz\WejdHnvci=> MUSyNVg1QDZ7NB?=
platelet  NV7Y[mY2TnWwY4Tpc44hSXO|YYm= MkHLNE4xPS9zL{KuOUDPxE1? MWi1JI1qdg>? NFXyR3RqdmirYnn0d{B1cGVic3nncoFtcW6pIH3lZ4hidmm|bYOg[I94dnO2cnXhcUBw\iCIY98zVmlKSQ>? NVnFZ|B5OjF6NEi2PVQ>
DoHH2 NE\TXHBCeG:ydH;zbZMhSXO|YYm= NGjYbIMxNzNxMUCg{txO NYjwT2Z7PDhiaB?= NU[0dVRKcW6mdXPld{Bk\WyuIHTlZZRpKHOrZ37p[olk[W62bIm= NYHvZ5duOjB6N{W0NFg>
Jeko-1  Mmr2RZBweHSxc3nzJGF{e2G7 M{LQcVAwOy9zMDFOwG0> M4DUOFQ5KGh? MkPGbY5lfWOnczDj[YxtKGSnYYToJJNq\26rZnnjZY51dHl? M2rqXlIxQDd3NEC4
Raji  MULBdI9xfG:|aYOgRZN{[Xl? NIPv[|ExNzNxMUCg{txO MoPiOFghcA>? NF2zemdqdmS3Y3XzJINmdGxiZHXheIghe2mpbnnmbYNidnSueR?= NGrmZYUzODh5NUSwPC=>
DHL4 M3TaXWFxd3C2b4Ppd{BCe3OjeR?= NVjsZoRDOC9zL{Sg{txO NVe4eopDQTZiaB?= M3nSdYlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= Mnf5NVgxODZ4OU[=
LY7 Mlv2RZBweHSxc3nzJGF{e2G7 MkjLNE8yNzRizszN NEfXfY06PiCq M4jOSIlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= M3\MclE5ODB4Nkm2
LY3 NVTDb4RySXCxcITvd4l{KEG|c3H5 MV6wM|EwPCEQvF2= NF60boE6PiCq M2rYNYlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NWf1TXA2OThyME[2PVY>
DHL6 MVvBdI9xfG:|aYOgRZN{[Xl? MoDkNE8yNzRizszN MUe5OkBp MUfpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 M3vzRlE5ODB4Nkm2
LY10 MlLJRZBweHSxc3nzJGF{e2G7 NInBXIUxNzFxNDFOwG0> M1HmVVk3KGh? M2rjWYlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NXnQ[FFQOThyME[2PVY>
DHL10 NWH5OJZ4SXCxcITvd4l{KEG|c3H5 MoTINE8yNzRizszN M2\LZlk3KGh? MY\pcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NXnyO5RCOThyME[2PVY>
Wsu-NHL NGrmb|BCeG:ydH;zbZMhSXO|YYm= MnHsNE8yNzRizszN Mn\sPVYhcA>? M4CweIlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NXyyd4N{OThyME[2PVY>
LY18 M{HFfGFxd3C2b4Ppd{BCe3OjeR?= MmjaNE8yNzRizszN MlvwPVYhcA>? M4jEbIlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= MmfWNVgxODZ4OU[=
LY1 MYfBdI9xfG:|aYOgRZN{[Xl? NYDhd2VJOC9zL{Sg{txO NUDkc5RkQTZiaB?= MWLpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MmnLNVgxODZ4OU[=
DHL8 NFPIe|VCeG:ydH;zbZMhSXO|YYm= M1;qfFAwOS92IN88US=> MnvBPVYhcA>? NIDwOYRqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NVjWNoQzOThyME[2PVY>
DHL4 MmfmRZBweHSxc3nzJGF{e2G7 M1Hw[VQh|ryP M1zqVFk3KGh? MWLpcoR2[2W|IHPs[YF3[WenIH;mJINie3Cjc3XzJFkh[W6mIEOsJIJ2fCCwb4SgZ4F{eGG|ZTC4 MX6xPFAxPjZ7Nh?=
DHL6 NE\CSY5CeG:ydH;zbZMhSXO|YYm= NFHJXZo1KM7:TR?= M2HIdVk3KGh? NGfw[ItqdmS3Y3XzJINt\WG4YXflJI9nKGOjc4Dhd4V{KDliYX7kJFMtKGK3dDDuc5Qh[2G|cHHz[UA5 MYmxPFAxPjZ7Nh?=
LY3 MX7BdI9xfG:|aYOgRZN{[Xl? MlzxOEDPxE1? NH7lZWk6PiCq M3PSVolv\HWlZYOgZ4xm[X[jZ3Wgc4Yh[2G|cHHz[ZMhQSCjbnSgN{wh[nW2IH7veEBk[XOyYYPlJFg> MlnlNVgxODZ4OU[=
LY7 MUjBdI9xfG:|aYOgRZN{[Xl? NVTyfXQ3PCEQvF2= M3nWVlk3KGh? NFr4SGtqdmS3Y3XzJINt\WG4YXflJI9nKGOjc4Dhd4V{KDliYX7kJFMtKGK3dDDuc5Qh[2G|cHHz[UA5 MWqxPFAxPjZ7Nh?=
DHL4 Mo\BSpVv[3Srb36gRZN{[Xl? NFHKNFU1KM7:TR?= NIjzfm8yPiCq M3TpZolvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u MnrpNVgxODZ4OU[=
LY7 Mlz2SpVv[3Srb36gRZN{[Xl? M4HSWlQh|ryP M4S3U|E3KGh? MoL1bY5pcWKrdIOgeI9vcWNiQlzOT{B1gXKxc3nu[UBxcG:|cHjvdplt[XSrb36= MXqxPFAxPjZ7Nh?=
LY3 MWfGeY5kfGmxbjDBd5NigQ>? NUDUcWdyPCEQvF2= NEnXVWEyPiCq MlT5bY5pcWKrdIOgeI9vcWNiQlzOT{B1gXKxc3nu[UBxcG:|cHjvdplt[XSrb36= M1XUWFE5ODB4Nkm2
DHL6 MkHjSpVv[3Srb36gRZN{[Xl? M{HielQh|ryP NGPycIIyPiCq NXXJV3Y1cW6qaXLpeJMhfG:waXOgRmxPUyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> MV6xPFAxPjZ7Nh?=
LY10 MmnuSpVv[3Srb36gRZN{[Xl? MWO0JO69VQ>? MVOxOkBp MVzpcohq[mm2czD0c45q[yCETF7LJJR6em:|aX7lJJBpd3OyaH;yfYxifGmxbh?= NWnOXYpkOThyME[2PVY>
Wsu-NHL MlW2SpVv[3Srb36gRZN{[Xl? MmDWOEDPxE1? NWHXSoM6OTZiaB?= NVnnXmNIcW6qaXLpeJMhfG:waXOgRmxPUyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> MWqxPFAxPjZ7Nh?=
LY18 NH\CSJBHfW6ldHnvckBCe3OjeR?= MWW0JO69VQ>? M{TjNVE3KGh? NGDV[mlqdmirYnn0d{B1d26rYzDCUG5MKHS7cn;zbY5mKHCqb4PwbI9zgWyjdHnvci=> MkPoNVgxODZ4OU[=

... 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]
- Collapse
  • 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.

Syk Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID